Research

Jump to: Review

30 pages, 42384 KiB

Open AccessArticle

In Silico Prediction, Characterization and Molecular Docking Studies on New Benzamide Derivatives

by Roxana Roman, Lucia Pintilie, Diana Nuță, Speranța Avram, Catalin Buiu, Catalina Sogor and Carmen Limban

Processes 2023, 11(2), 479; https://doi.org/10.3390/pr11020479 - 05 Feb 2023

Cited by 5 | Viewed by 2759

Abstract

Recent research papers have confirmed the prevalence of microorganisms resistant to numerous antimicrobial agents, leading to spreading infections, extended hospitalizations, and increased mortality rates. The amplifying factors stimulate the need to discover new molecules able to cut off the developing resistance of pathogens [...] Read more.

Recent research papers have confirmed the prevalence of microorganisms resistant to numerous antimicrobial agents, leading to spreading infections, extended hospitalizations, and increased mortality rates. The amplifying factors stimulate the need to discover new molecules able to cut off the developing resistance of pathogens against medicines. The current study presents a molecular docking procedure applied on 15 new pyridine–thiourea derivatives in order to test their activities against S. aureus and E. coli. The protein crystal structures were obtained from the Protein Data Bank (PDB). Processes such as geometry optimization, molecular properties (log P, polarizability, E HOMO, E LUMO, area and volume of the molecules, and ovality), drug-likeness, pharmacokinetic and pharmacogenomic profiles, and molecular docking studies are discussed in the present research. The approach involved the determination of the molecular properties for each chemical structure by using the Spartan 14 software, followed by the evaluation of their binding affinity through a specific docking score with the aid of the CLC Drug Discovery Workbench. Each studied compound established hydrogen bonds with the selected receptors, leading to suitable docking scores and increasing the chances of the compound being considered for further investigation. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

9 pages, 546 KiB

Open AccessArticle

Comparative Analysis of Clinical and Epidemiological Characteristics in Patients with SARI Confirmed as Influenza or COVID-19 Admitted in a Tertiary Care Hospital in Bucharest, Romania

by Bianca Georgiana Enciu (Milcu), Anca Cristina Drăgănescu, Daniela Pițigoi, Oana Săndulescu, Maria Dorina Crăciun, Anuța Bilașco, Anca Streinu-Cercel, Adrian Streinu-Cercel, Dragoș Florea, Victor Daniel Miron and Victoria Aramă

Processes 2022, 10(2), 327; https://doi.org/10.3390/pr10020327 - 08 Feb 2022

Cited by 1 | Viewed by 1764

Abstract

The COVID-19 pandemic has influenced the epidemiology of other respiratory pathogens, and this was most evident in the 2020–2021 season, which was characterized by a low circulation of influenza viruses. We aim to present a comparative analysis of clinical and epidemiological characteristics of [...] Read more.

The COVID-19 pandemic has influenced the epidemiology of other respiratory pathogens, and this was most evident in the 2020–2021 season, which was characterized by a low circulation of influenza viruses. We aim to present a comparative analysis of clinical and epidemiological characteristics of 2018–2019 influenza cases and 2020–2021 COVID-19 cases, hospitalized at a tertiary infectious diseases hospital in Bucharest. We used data collected from patients admitted for severe acute respiratory infection (SARI) and subsequently confirmed with either influenza or COVID-19. During the 2018–2019 season, 208 patients over 18 years of age were confirmed with influenza (median age = 53 years, 59.6% were female) and 6.7% had been vaccinated against influenza. The most frequent symptoms were fever (97.1%) and cough (94.7%), and 77.4% had at least one chronic condition. 90.4% received influenza antiviral therapy. During the 2020–2021 season, 191 patients were confirmed with COVID-19 (median age = 56 years, 67% were male). The most frequent symptoms were cough (85.9%) and fever (80.6%), and 75.9% had at least one chronic condition. This analysis highlights the main similarities and differences between influenza and COVID-19 and could help to optimize the management of cases. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

13 pages, 3478 KiB

Open AccessArticle

(S)-5-Methylmellein Isolated from an Endogenous Lichen Fungus Rosellinia corticium as a Potent Inhibitor of Human Monoamine Oxidase A

by Geum-Seok Jeong, Eun-Young Lee, Myung-Gyun Kang, Sang-Jip Nam, Daeui Park and Hoon Kim

Processes 2022, 10(1), 166; https://doi.org/10.3390/pr10010166 - 14 Jan 2022

Cited by 5 | Viewed by 1714

Abstract

In this study, the inhibitory activities against human monoamine oxidases (hMAOs) were evaluated using a library of 195 endogenous lichen fungi from Ukraine. Among them, the extract ELF68 of the endogenous fungus Rosellinia corticium from the lichen Pseudevernia furfuracea (L.) Zopf. exhibited the [...] Read more.

In this study, the inhibitory activities against human monoamine oxidases (hMAOs) were evaluated using a library of 195 endogenous lichen fungi from Ukraine. Among them, the extract ELF68 of the endogenous fungus Rosellinia corticium from the lichen Pseudevernia furfuracea (L.) Zopf. exhibited the strongest inhibitory activity against hMAO-A. Using the activity-guided method, (S)-5-methylmellein (5MM) was isolated from the extract and had an IC₅₀ value of 5.31 µM for hMAO-A with a lower potency for hMAO-B (IC₅₀ = 9.15 µM). Compound 5MM also moderately inhibited acetylcholinesterase (IC₅₀ = 27.07 µM) but very weakly inhibited butyrylcholinesterase and β-secretase. Compound 5MM had a K_i value of 2.45 μM and was a reversible competitive inhibitor of hMAO-A. A molecular docking study predicted that (S)-5MM showed higher binding affinity for hMAO-A (−6.8 kcal/mol) than hMAO-B (−6.4 kcal/mol). Its isomer, (R)-5MM, exhibited lower binding affinities for hMAO-A (−6.6 kcal/mol) and hMAO-B (−5.2 kcal/mol), compared to (S)-5MM. The S-form interacted with hMAO-A through hydrogen bonding with the Phe208 residue (distance: 1.972 Å), while the R-form interacted with the Asn181 residue (2.375 Å). The results of an in silico pharmacokinetic analysis indicated that 5MM did not violate Lipinski’s five rules and showed high gastrointestinal absorption and blood–brain barrier permeability. These results suggest that 5MM can be considered a candidate in the treatment of neuropsychiatric disorders, such as depression and cardiovascular disease. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

9 pages, 443 KiB

Open AccessFeature PaperArticle

Differentially Expressed Genes Correlated with Fibrosis in a Rat Model of Chronic Partial Bladder Outlet Obstruction

by Yuan-Shuo Hsueh, Hui Hua Chang, Shun-Yao Ko, Yi-Pai Lin and Wei-Yu Lin

Processes 2021, 9(12), 2219; https://doi.org/10.3390/pr9122219 - 09 Dec 2021

Viewed by 1943

Abstract

Chronic partial bladder outlet obstruction (PBOO) is a prevalent clinical problem that may result from multiple etiologies. PBOO may be a secondary condition to various anatomical and functional abnormalities. Bladder fibrosis is the worst outcome of PBOO. However, gene alterations and the mechanism [...] Read more.

Chronic partial bladder outlet obstruction (PBOO) is a prevalent clinical problem that may result from multiple etiologies. PBOO may be a secondary condition to various anatomical and functional abnormalities. Bladder fibrosis is the worst outcome of PBOO. However, gene alterations and the mechanism of fibrosis development after PBOO onset are not clear. Therefore, we aimed to investigate gene expression alterations during chronic PBOO. A rat model of PBOO was established and validated by a significant increase in rat bladder weight. The bladder samples were further analyzed by microarray, and differentially expressed genes (DEGs) that are more related to PBOO compared with the control genes were selected. The data showed that 16 significantly upregulated mRNAs and 3 significantly downregulated mRNAs are involved in fibrosis. Moreover, 13 significantly upregulated mRNAs and 12 significantly downregulated mRNAs are related to TGFB signaling. Twenty-two significantly upregulated mRNAs and nine significantly downregulated mRNAs are related to the extracellular matrix. The genes with differential expressions greater than four-fold included Grem1, Thbs1, Col8a1, Itga5, Tnc, Lox, Timp1, Col4a1, Col4a2, Bhlhe40, Itga1, Tgfb3, and Gadd45b. The gene with a differential expression less than a quarter-fold was Thbs2. These findings show the potential roles of these genes in the physiology of PBOO. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

7 pages, 550 KiB

Open AccessArticle

Effect of a Symbiotic Mixture on Fecal Microbiota in Pediatric Patients Suffering of Functional Abdominal Pain Disorders

by Cristina Adriana Becheanu, Roxana Elena Smădeanu and Iulia Florentina Ţincu

Processes 2021, 9(12), 2157; https://doi.org/10.3390/pr9122157 - 29 Nov 2021

Cited by 2 | Viewed by 1864

Abstract

(1) Background: Functional abdominal pain disorders (FAPDs) represent one of the main etiologies of chronic abdominal pain in the pediatric population. A wide spectrum of probiotic or prebiotic mixtures has been evaluated in trials regarding benefits in patients with FAPDs, mainly in the [...] Read more.

(1) Background: Functional abdominal pain disorders (FAPDs) represent one of the main etiologies of chronic abdominal pain in the pediatric population. A wide spectrum of probiotic or prebiotic mixtures has been evaluated in trials regarding benefits in patients with FAPDs, mainly in the adult population. (2) Methods: This study was interested in evaluating the effect of oral supplementation with a symbiotic mixture on intestinal microbiota in children with functional dyspepsia (FD), irritable bowel syndrome with diarrhea (IBS-D), and irritable bowel syndrome with constipation (IBS-C). A combination of six bacterial strains (Lactobacillus rhamnosus R0011, Lactibacillus casei R0215, Bifidobacterium lactis BI-04, Lactobacillus acidophilus La-14, Bifidobacterium longum BB536, Lactobacillus plantarum R1012) and 210 mg of fructo-oligosaccharides-inulin were administered orally, daily, for 12 weeks and patients were scored for severity of symptoms and fecal microbiota before and after the treatment. (3) Results: The proportion of patients with adequate symptom relief was higher in the IBS-D than in the IBS-C group; however, the difference was not statistically significant (74.4% vs. 61.9%, p = 0.230). There was an increasing proportion of bacterial genera associated with health benefits, for both IBS-C and IBS-D (IBS-C: 31.1 ± 16.7% vs. 47.7 ± 13.5%, p = 0.01; IBS-D: 35.8 ± 16.2% vs. 44.1 ± 15.1%, p = 0.01). (4) Conclusions: Administration of a symbiotic preparation resulted in significant changes to the microbiota and gastrointestinal symptoms in patients with FAPDs. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

20 pages, 22674 KiB

Open AccessEditor’s ChoiceArticle

Development and Optimization of Chitosan-Hydroxypropyl Methylcellulose In Situ Gelling Systems for Ophthalmic Delivery of Bupivacaine Hydrochloride

by Lăcrămioara Popa, Mihaela Violeta Ghica, Roxana Popescu, Teodora Irimia and Cristina-Elena Dinu-Pîrvu

Processes 2021, 9(10), 1694; https://doi.org/10.3390/pr9101694 - 22 Sep 2021

Cited by 8 | Viewed by 2528

Abstract

The aim of this study was the development and optimization of chitosan and hydroxypropyl methylcellulose (HPMC) in situ gelling systems, loaded with bupivacaine hydrochloride for topical ocular administration. This study is based on the properties of two polymers: chitosan, which has mucoadhesive action [...] Read more.

The aim of this study was the development and optimization of chitosan and hydroxypropyl methylcellulose (HPMC) in situ gelling systems, loaded with bupivacaine hydrochloride for topical ocular administration. This study is based on the properties of two polymers: chitosan, which has mucoadhesive action and is a pH-sensitive polymer, but also the cellulose derivative hydroxypropyl methylcellulose, a thermosensitive polymer which has mucoadhesive properties and increases the viscosity of systems. The analysis and optimization of in situ gelling systems were performed based on an experimental design and response surface methodology. The following formulation parameters were considered: X₁ = chitosan concentration (0.5%, 1%), X₂ = HPMC E 5 LV concentration (2%, 5%) and X₃ = Chitosan/HPMC E 5 LV ratio (1/1, 2/1). In addition, the parameters to be optimized were represented by the contact angle (CA (°)), viscosity and cumulative percentage of bupivacaine hydrochloride released in vitro. The results indicate that the designed in situ gelling systems are suitable for bupivacaine prolonged ophthalmic release and overcome the principal disadvantages of the liquid’s ocular formulations. An immediate therapeutic effect corresponding to ocular anesthetic installation was assured in the first stage: burst bupivacaine release. In the second phase, the gradual drug release was assured for over 6 h. This drug release profile, together with the corresponding rheological profile and a collection of superficial properties for good ocular adhesion balanced with an adequate hydrophilic character, assured the desired quality of the attributes for the proposed systems. The system, based on chitosan 1%, HPMC E 5 LV 5% and a 1/1 polymer ratio, could be a solution for the proposed formulation of in situ gelling colloidal systems, since the viscosity of the system was within the range of the optimal viscosity of the eye, and the amount of bupivacaine hydrochloride released after 6 h was the highest at 69.55%. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

8 pages, 396 KiB

Open AccessArticle

Cost-Efficacy of Antiretroviral Regimens Recommended in Treatment-Naive HIV-Infected Adults. A Single Center Experience

by Raluca Jipa, Iulia Nedelcu, Eliza Manea, Anca Damalan and Adriana Hristea

Processes 2021, 9(6), 956; https://doi.org/10.3390/pr9060956 - 28 May 2021

Viewed by 1956

Abstract

We aimed to assess the prescription trends of combined antiretroviral therapy (cART) in one infectious diseases department and the cost-efficacy (C/E) of different regimens used in treatment-naïve patients. The C/E was assessed with a software application developed by a group of researchers in [...] Read more.

We aimed to assess the prescription trends of combined antiretroviral therapy (cART) in one infectious diseases department and the cost-efficacy (C/E) of different regimens used in treatment-naïve patients. The C/E was assessed with a software application developed by a group of researchers in Spain. The efficacy was already calculated in the application. The costs included the local cost of antiretrovirals and other direct costs specific to our institution. In the software application, the C/E reference regimen was ABC/3TC/DTG. In total, 181 HIV-infected patients were diagnosed and initiated cART during 2015–2019. The proportion of patients treated with integrase-strand transfer inhibitor (INSTI)-based regimens increased from 2015–2018 (54%) to the end of 2019 (81%). The relative C/E ranged from 0.90 to 1.28 for the evaluated INSTI-based regimens. Among INSTI-based regimens, ABC/3TC/DTG and TAF/FTC/EVG/c are the regimens with similar efficacy and relative C/E. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

27 pages, 6355 KiB

Open AccessArticle

Liposomes with Caffeic Acid: Morphological and Structural Characterisation, Their Properties and Stability in Time

by Ioana Lavinia Dejeu, Laura Grațiela Vicaș, Tunde Jurca, Alin Cristian Teușdea, Mariana Eugenia Mureșan, Luminița Fritea, Paula Svera, Gianina Adela Gabor, George Emanuiel Dejeu, Octavian Adrian Maghiar, Anca Salomea Bodea, Annamaria Pallag and Eleonora Marian

Processes 2021, 9(6), 912; https://doi.org/10.3390/pr9060912 - 22 May 2021

Cited by 7 | Viewed by 3572

Abstract

Medical and pharmaceutical research has shown that liposomes are very efficient in transporting drugs to targets. In this study, we prepared six liposome formulas, three in which we entrapped caffeic acid (CA), and three with only phospholipids and without CA. Determination of entrapment [...] Read more.

Medical and pharmaceutical research has shown that liposomes are very efficient in transporting drugs to targets. In this study, we prepared six liposome formulas, three in which we entrapped caffeic acid (CA), and three with only phospholipids and without CA. Determination of entrapment efficiency (EE) showed that regardless of the phospholipids used, the percentage of CA entrapment was up to 76%. The characterization of the liposomes was performed using Dynamic Light Scattering (DLS), Atomic Force Microscopy (AFM), zeta potential and polydispersity and showed that about 75–99% of the liposomes had dimensions between 40 ± 0.55–500 ± 1.45 nm. The size and zeta potential of liposomes were influenced by the type of phospholipid used to obtain them. CA release from liposomes was performed using a six-cell Franz diffusion system, and it was observed that the release of entrapped CA occurs gradually, the highest amount occurring in the first eight hours (over 80%), after which the release is much reduced. Additionally, the time stability of the obtained liposomes was analysed using univariate and multivariate statistical analysis. Therefore, liposomes offer great potential in CA entrapment. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

14 pages, 2706 KiB

Open AccessArticle

Development and Evaluation of Fluoxetine Fast Dissolving Films: An Alternative for Noncompliance in Pediatric Patients

by Emőke-Margit Rédai, Paula Antonoaea, Nicoleta Todoran, Robert Alexandru Vlad, Magdalena Bîrsan, Anamaria Tătaru and Adriana Ciurba

Processes 2021, 9(5), 778; https://doi.org/10.3390/pr9050778 - 28 Apr 2021

Cited by 4 | Viewed by 2785

Abstract

The most used pharmaceutical formulations for children are syrups, suppositories, soft chewable capsules, and mini-tablets. Administrating them might create an administration discomfort. This study aimed to develop and evaluate orodispersible films (ODFs) for pediatric patients in which the fluoxetine (FX) is formulated in [...] Read more.

The most used pharmaceutical formulations for children are syrups, suppositories, soft chewable capsules, and mini-tablets. Administrating them might create an administration discomfort. This study aimed to develop and evaluate orodispersible films (ODFs) for pediatric patients in which the fluoxetine (FX) is formulated in the polymeric matrix. Six FX fast dissolving films (10 mg FX/ODF), FX1, FX2, FX3, FX4, FX5, and FX6, were prepared by solvent casting technique. In the composition of the ODFs, the concentration of the hydroxypropyl methylcellulose and the concentration of the propylene glycol were varied. Each formulation of fluoxetine ODF was evaluated by determining the tensile strength, folding endurance, disintegration, behavior in the controlled humidity and temperature conditions, and adhesiveness. All the obtained results were compared with the results obtained for six ODFs prepared without FX. The disintegration time of the FX ODFs was of maximum 88 s for FX2. Via the in vitro releasing study of the FX from the ODFs it was noticed that FX1 and FX2 allow a better release of the drug 99.98 ± 3.81% and 97.67 ± 3.85% being released within 15 min. From the obtained results it was also confirmed that FX ODFs were found to follow first-order release kinetic. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

13 pages, 2764 KiB

Open AccessArticle

Preparation and Characterization of Two Different Liposomal Formulations with Bioactive Natural Extract for Multiple Applications

by Florina Miere (Groza), Simona Ioana Vicas, Adrian Vasile Timar, Mariana Ganea, Mihaela Zdrinca, Simona Cavalu, Luminita Fritea, Laura Vicas, Mariana Muresan, Annamaria Pallag and Luciana Dobjanschi

Processes 2021, 9(3), 432; https://doi.org/10.3390/pr9030432 - 27 Feb 2021

Cited by 35 | Viewed by 3311

Abstract

Liposomes continue to attract great interest due to their increased bioavailability in the body and because the substances encapsulated are protected while maintaining their effectiveness. The aim of this study is to obtain “giant” liposomes by lipid film hydration using a preparation formula [...] Read more.

Liposomes continue to attract great interest due to their increased bioavailability in the body and because the substances encapsulated are protected while maintaining their effectiveness. The aim of this study is to obtain “giant” liposomes by lipid film hydration using a preparation formula with two different phospholipids, phosphatidylcholine (PC) and phosphatidylserine (PS). Firstly, the macro- and microscopic characterization, total phenols content and antioxidant capacity of the plant Stellaria media (L.) Vill. were assessed. Then, Stellaria media (L.) Vill. extract was encapsulated in both formulations (PCE and PSE) and the liposomes were characterized according to their morphology, size distribution and Zeta potential using optical microscopy and dynamic light scattering. The encapsulation efficiency (EE%) was determined using the Folin–Ciocalteu method and the values of both formulations were compared. PC and PCE liposomes with a diameter between 712 and 1000 nm and PS and PSE liposomes with a diameter between 58 and 1000 nm were obtained. The values EE% of Stellaria media (L.) Vill. extract for PCE and PSE were 92.09% and 84.25%, respectively. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

22 pages, 2945 KiB

Open AccessArticle

Evaluation of Dissolution Profiles of a Newly Developed Solid Oral Immediate-Release Formula Containing Alpha-Lipoic Acid

by Anca Lucia Pop, Simona Crișan, Maria Bârcă, Anne-Marie Ciobanu, Valentin Nicolae Varlas, Coriolan Pop, Mariana-Ana Pali, Dumitru Cauni, Emma Adriana Ozon, Denisa Udeanu, Simona Trifu and Bogdana Adriana Năsui

Processes 2021, 9(1), 176; https://doi.org/10.3390/pr9010176 - 19 Jan 2021

Cited by 14 | Viewed by 8149

Abstract

Alpha-lipoic acid (ALA, thioctic acid), a naturally-occurring essential dithiol compound, has become a common ingredient in many pharmaceutical and food supplement products (FSP), used in oxidative stress-dependent pathologies; oral bioavailability of ALA is limited by pharmacokinetic particularities that reduce its therapeutic efficacy-reduced solubility, [...] Read more.

Alpha-lipoic acid (ALA, thioctic acid), a naturally-occurring essential dithiol compound, has become a common ingredient in many pharmaceutical and food supplement products (FSP), used in oxidative stress-dependent pathologies; oral bioavailability of ALA is limited by pharmacokinetic particularities that reduce its therapeutic efficacy-reduced solubility, lack of gastric stability and hepatic degradation, doubled by formulation hinders. The objectives were to develop a solid oral 600 mg ALA FSP to obtain an optimal pharmaceutical profile compared to a reference listed drug (RLD) with a similarity factor f₂ 50. A comparative dissolution study was performed; an HPLC method was used for ALA quantification. After planning combinatory simulations (formulation stage), two prototype formulas (#1 and #2) were manufactured and further optimized by adjusting ALA physical characteristics and the excipients quantities (#3 and #4) in order to achieve the Quality Target Product Profile. A misshapen of ALA’s in vitro release was observed for #3 Formula (f₂ = 31.6); the optimal profile was obtained for Formula #4 (f₂ = 58.5). A simple quantitative formula is not enough to assure good ALA bioavailability; the formulation needs multiple compounding modulations under physicochemical compatibility algorithms, with multiple dissolution profiles testing back-ups. It is essential to ensure a formulation with an in vitro dissolution comparable with the RLD, allowing the compound to reach its target level to assure the optimum claimed antioxidant activity of ALA at the cellular level, even for food supplement formulations. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

21 pages, 3977 KiB

Open AccessArticle

Topical Biocompatible Fluconazole-Loaded Microemulsions Based on Essential Oils and Sucrose Esters: Formulation Design Based on Pseudo-Ternary Phase Diagrams and Physicochemical Characterization

by Lavinia Vlaia, Georgeta Coneac, Ana Maria Muţ, Ioana Olariu, Vicenţiu Vlaia, Dan Florin Anghel, Monica Elisabeta Maxim, Amadeus Dobrescu, Mircea Hîrjău and Dumitru Lupuleasa

Processes 2021, 9(1), 144; https://doi.org/10.3390/pr9010144 - 13 Jan 2021

Cited by 14 | Viewed by 3731

Abstract

To initiate our research into the development of biocompatiîle gelled-microemulsions based on essential oils (EOs) and sucrose esters (SEs) for the topical delivery of fluconazole, this formulation study investigated the usefulness of two relatively harmless natural non-ionic surfactants from the group of SEs [...] Read more.

To initiate our research into the development of biocompatiîle gelled-microemulsions based on essential oils (EOs) and sucrose esters (SEs) for the topical delivery of fluconazole, this formulation study investigated the usefulness of two relatively harmless natural non-ionic surfactants from the group of SEs (sucrose laurate and stearate) to form, in the presence of antifungal EOs, stable, isotropic microemulsions effective on fluconazole solubilization. Fluconazole’s solubility in EO significantly depended on their chemical composition, showing higher values for cinnamon, oregano and clove essential oils, further selected as oil phase components for microemulsion formulations. The phase behavior of several EO–isopropyl miristate/SE–isopropanol/water systems was assessed through pseudo-ternary phase diagrams constructed by microplate dilution technique. The hydrocarbon chain length of the SE and EO type strongly influenced the size of the microemulsion region in the pseudo-ternary phase diagrams. Ten microemulsion formulations containing 2% fluconazole, 6% or 10% oil mixture of EO–isopropyl myristate in 1:1 ratio, 45% SE-isopropanol mixture and water, were selected and evaluated for physicochemical properties (droplet size, polydispersity, viscosity, refractive index, zeta potential and pH). All formulations were physicochemically acceptable, but viscosity enhancement and further in vitro and in vivo tests are required for the development of biocompatible, clinically safe and effective fluconazole topical preparations. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Graphical abstract

13 pages, 3057 KiB

Open AccessArticle

Polymeric Films Containing Tenoxicam as Prospective Transdermal Drug Delivery Systems: Design and Characterization

by Adriana Ciurba, Paula Antonoaea, Nicoleta Todoran, Emőke Rédai, Robert Alexandru Vlad, Anamaria Tătaru, Daniela-Lucia Muntean and Magdalena Bîrsan

Processes 2021, 9(1), 136; https://doi.org/10.3390/pr9010136 - 11 Jan 2021

Cited by 7 | Viewed by 2448

Abstract

The administration of drugs via transdermal therapeutic systems has become an attractive form of therapeutic approach, considering its advantages and the high patient compliance achieved, making them a viable alternative, especially in the treatment of chronic diseases. The purpose of our study was [...] Read more.

The administration of drugs via transdermal therapeutic systems has become an attractive form of therapeutic approach, considering its advantages and the high patient compliance achieved, making them a viable alternative, especially in the treatment of chronic diseases. The purpose of our study was the development of polymer-based films containing tenoxicam (TX) and the analysis of dissolution kinetics. Auxiliary substances represent an important part of pharmaceutical forms, so during the first stage, TX and excipient compatibility were verified. Fourier Transform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC) analyses were performed on TX and on physical mixtures of TX-HPMC_E5 and TX-HPMC_15kcP. Three polymeric films of TX (TX₁, TX₂, and TX₃) were prepared using a solvent evaporation technique. Release studies were done at 32 °C ± 1 °C with a Franz diffusion cell. The results of the DSC and FT-IR analyses demonstrated the compatibility of the active substance with the two matrix-forming polymers. The results obtained in the release studies of TX from the proposed polymeric films suggested a pH-dependent behavior in all three polymeric films. At pH 5.5, flux values were between 8.058 ± 0.125 μg·cm⁻²·h⁻¹ and 10.850 ± 0.380 μg·cm⁻²·h⁻¹; and at pH 7.4, between 10.990 ± 0.2.490 μg·cm⁻²·h⁻¹ and 53.140 ± 0.196 μg·cm⁻²·h⁻¹. The Korsmeyer–Peppas model described a non-Fickian transport mechanism. The n values varied between 0.63–0.7 at pH 5.5 and 0.73–0.86 at pH 7.4, which suggested a diffusion depending on the matrix hydration and polymer relaxation. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

25 pages, 32267 KiB

Open AccessArticle

Physico-Chemical and Pharmaco-Technical Characterization of Inclusion Complexes Formed by Rutoside with β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin Used to Develop Solid Dosage Forms

by Teodora Balaci, Bruno Velescu, Oana Karampelas, Adina Magdalena Musuc, George Mihai Nițulescu, Emma Adriana Ozon, Georgiana Nițulescu, Cerasela Elena Gîrd, Catalina Fița and Dumitru Lupuliasa

Processes 2021, 9(1), 26; https://doi.org/10.3390/pr9010026 - 24 Dec 2020

Cited by 16 | Viewed by 2595

Abstract

The aim of our study was to obtain rutoside (RUT) inclusion complexes in β-cyclodextrin (β-CD) and in hydroxypropyl-β-cyclodextrin (HP-β-CD), in a 1:1 molar ratio, using the lyophilization method of complexation in solution. The complexes were confirmed and characterized, in comparison with the raw [...] Read more.

The aim of our study was to obtain rutoside (RUT) inclusion complexes in β-cyclodextrin (β-CD) and in hydroxypropyl-β-cyclodextrin (HP-β-CD), in a 1:1 molar ratio, using the lyophilization method of complexation in solution. The complexes were confirmed and characterized, in comparison with the raw materials and their simple physical mixtures, by SEM, DSC, and FT-IR analyses. The antioxidant activity of the compounds was assessed by using the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) and 2’-azino-bis(3-ethylbenzothiazolin-6-sulfonic) acid (ABTS) radicals, determining the radical scavenging activity, and by ferric reducing antioxidant power (FRAP) assay. The results revealed superior antioxidant ability for the inclusion complexes towards rutoside alone. The inclusion complexes were used as active ingredients in formulations of immediate-release tablets. The preformulation studies were performed on the powders for direct compression obtained after mixing the active ingredients with the excipients (Avicel PH 102, Polyplasdone XL-10, magnesium stearate, and talc). The materials were assessed for particle size, flowability, compressibility, and moisture content, establishing they are suitable for a direct compression process. The tablets were characterized regarding their pharmaco-technical properties and the results proved that the formulations lead to high-quality delivery systems, showing a good mechanical resistance with a low friability, excellent disintegration times, and satisfying dissolution rate. The performances were very similar for both formulations and the physico-mechanical properties of the tablets are not influenced by type of the used cyclodextrin, but the RUT- HP-β-CD tablets presented a higher dissolution rate. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

12 pages, 256 KiB

Open AccessArticle

Pharmacoeconomic Analysis of Hemophilia Care in Romania

by Petre Serban, Brigitha Vlaicu, Margit Serban, Cristina Emilia Ursu, Adina Traila, Cristian Jinca, Jenel Marian Patrascu, Daniel Andrei, Andrei Kozma and Teodora Smaranda Arghirescu

Processes 2020, 8(12), 1676; https://doi.org/10.3390/pr8121676 - 18 Dec 2020

Viewed by 2132

Abstract

Hemophilia, a congenital X linked disease, has the serious burden of bleeding, requiring life-long replacement with coagulation factors (CF). In the present day, there is a continuously improving treatment for this condition. Objective: Our observational, cross-sectional study aims at finding out whether a [...] Read more.

Hemophilia, a congenital X linked disease, has the serious burden of bleeding, requiring life-long replacement with coagulation factors (CF). In the present day, there is a continuously improving treatment for this condition. Objective: Our observational, cross-sectional study aims at finding out whether a prophylactic replacement with CF is affordable from the point of view of its cost-effectiveness in our country. Material and methods: A cohort of 122 persons with hemophilia were included in this patient-reported outcome survey, and they answered a questionnaire consisting of 56 items, focused on 4 domains—socio-demographic, medical, quality of health/life and cost/cost-effectiveness. Results and discussion: The markers for quality of health/life were correlated with the direct and indirect costs of care, comparing subgroup 1 of patients with prophylactic vs. subgroup 2 with on-demand replacement. Based on the incremental quality adjusted life years and the incremental costs, we calculated the incremental cost-effectiveness ratio (ICER) proving that prophylaxis is more cost-effective than on-demand replacement on a long time basis. Conclusions: The ICER is a threshold recommending the reimbursement of costs for a life-long prophylactic replacement in our country. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

14 pages, 3093 KiB

Open AccessArticle

Hot Melt Extrusion Processing Parameters Optimization

by Abdullah Alshetaili, Saad M. Alshahrani, Bjad K. Almutairy and Michael A. Repka

Processes 2020, 8(11), 1516; https://doi.org/10.3390/pr8111516 - 22 Nov 2020

Cited by 16 | Viewed by 4519

Abstract

The aim of this study was to demonstrate the impact of processing parameters of the hot-melt extrusion (HME) on the pharmaceutical formulation properties. Carbamazepine (CBZ) was selected as a model water-insoluble drug. It was incorporated into Soluplus^®, which was used as [...] Read more.

The aim of this study was to demonstrate the impact of processing parameters of the hot-melt extrusion (HME) on the pharmaceutical formulation properties. Carbamazepine (CBZ) was selected as a model water-insoluble drug. It was incorporated into Soluplus^®, which was used as the polymeric carrier, to produce a solid dispersion model system. The following HME-independent parameters were investigated at different levels: extrusion temperature, screw speed and screw configuration. Design of experiment (DOE) concept was applied to find the most significant factor with minimum numbers of experimental runs. A full two-level factorial design was applied to assess the main effects, parameter interactions and total error. The extrudates’ CBZ content and the in vitro dissolution rate were selected as response variables. Material properties, including melting point, glass transition, and thermal stability, and polymorphs changes were used to set the processing range. In addition, the extruder torque and pressure were used to find the simplest DOE model. Each change of the parameter showed a unique pattern of dissolution profile, indicating that processing parameters have an influence on formulation properties. A simple, novel and two-level factorial design was able to evaluate each parameter effect and find the optimized formulation. Screw configuration and extrusion temperature were the most affecting parameters in this study. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

19 pages, 22747 KiB

Open AccessArticle

Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

by Maria Drăgan, Cătălina Daniela Stan, Andreea Teodora Iacob, Oana Maria Dragostin, Mihaela Boancă, Cătălina Elena Lupuşoru, Carmen Lăcrămioara Zamfir and Lenuţa Profire

Processes 2020, 8(11), 1401; https://doi.org/10.3390/pr8111401 - 02 Nov 2020

Cited by 6 | Viewed by 2202

Abstract

The purpose of this study was to evaluate the in vivo biological potential of new azetidine-2-one derivatives of ferulic acid (6a–f). First, the in vivo acute toxicity of azetidine-2-one derivatives of ferulic acid on Swiss white mice was investigated and, based [...] Read more.

The purpose of this study was to evaluate the in vivo biological potential of new azetidine-2-one derivatives of ferulic acid (6a–f). First, the in vivo acute toxicity of azetidine-2-one derivatives of ferulic acid on Swiss white mice was investigated and, based on the obtained results, it can be stated that the studied derivatives belong to compounds with moderate toxicity. The in vivo anti-inflammatory potential of these derivatives was determined in a model of acute inflammation induced by carrageenan in rats and in a chronic inflammation model induced in rats using the granuloma test. In the acute inflammation model, all the studied compounds had a maximum anti-inflammatory effect 24 h after administration, which suggests that these compounds may be classified, from a pharmacokinetic point of view, in the category of long-acting compounds. The most active compound in the series was found to be compound 6b. In the case of the chronic inflammation model, it was observed that the studied compounds (6a–f) reduced the formation of granulation tissue compared to the control group, having an intense effect of inhibiting the proliferative component. The most important inhibitory effect of inhibiting the proliferative component was recorded for compound 6b. Additionally, the investigation of liver function was performed by determining the serum levels of liver enzymes aspartate transaminase (AST), alanine aminotransferase (ALT), lactate dehydrogenase (LDH) and bilirubin (total and direct). The results showed that, in the series of azetidin-2-one derivatives, the liver enzymes concentration values were close to those recorded for the reference anti-inflammatories (diclofenac sodium and indomethacin) and slightly higher compared to the values for the healthy control group. At the end of the experiment, the animals were euthanized and fragments of liver, lung, and kidney tissue were taken from all groups in the study. These were processed for histopathological examination, and we noticed no major changes in the groups treated with the azetidine 2-one derivatives of ferulic acid compared to the healthy groups. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

9 pages, 588 KiB

Open AccessArticle

The Importance of Dose Intensity When Administering Cytotoxic Chemotherapy in NSCLC—A Matter as Actual Now as in the Past

by Cornelia Nitipir, Cristina Orlov-Slavu, Mihaela Olaru, Andreea Parosanu, Ana-Maria Popa, Cristian Iaciu, Bogdan Catalin Popescu, Maria Alexandra Barbu, Cristina Pirlog, Valentin Calu, Andreea Catarina Popescu, Dragos Bumbacea, Cristian Paleru, Iulian Slavu and Lucian Alecu

Processes 2020, 8(8), 936; https://doi.org/10.3390/pr8080936 - 04 Aug 2020

Cited by 1 | Viewed by 2348

Abstract

Lung cancer, as the leading cause of death in oncology is one of the most challenging diseases nowadays. Even after the implementation of checkpoint inhibitors and targeted therapy as a standard of therapy for metastatic disease, the chemotherapy backbone remains essential in the [...] Read more.

Lung cancer, as the leading cause of death in oncology is one of the most challenging diseases nowadays. Even after the implementation of checkpoint inhibitors and targeted therapy as a standard of therapy for metastatic disease, the chemotherapy backbone remains essential in the treatment of these patients. This study aimed to evaluate how administration particularities in chemotherapy and toxicity management can influence the outcome. We conducted a retrospective single-institution study, at Elias University Emergency Hospital, Bucharest, Romania, between 2014 and 2018, in a heterogeneous patient population with metastatic non-small cell lung cancer that received combination chemotherapy. The inclusion criteria for this trial were—histological proof of non-small cell lung cancer (NSCLC), stage IV disease, ECOG (Eastern Cooperative Oncology Group) performance status of a maximum of two, treatment with cytotoxic chemotherapy for at least four courses (patients with fewer courses were excluded). All patients received combination chemotherapy. The main focus was on the effect of dose reduction and treatment delay on overall survival and progression-free survival. A total of 129 patients were enrolled. The response rate in the studied population was 69% and 62.8% had no toxicity greater than grade 2. Chemotherapy regimens used had the following distribution—paclitaxel + carboplatin 41.9%, paclitaxel + carboplatin + bevacizumab 12.4%, pemetrexed + carboplatin 12.4%, gemcitabine + carboplatin 26.4% and other regimens 7%. Mean PFS (Progression Free Survival) was 9.1 months and the mean OS (Overall Survival) was 14 months. OS was not significantly different in the treatment delay group versus the no delay one, p < 0.25 but dose- reduction significantly impacted OS, p < 0.03. Administration particularities, like febrile neutropenia prophylaxis, treatment of chemotherapy-related anemia, respecting the details of chemostability and preparation rules and emesis prophylaxis, were considered reasons for the good outcome. Details regarding cytotoxic chemotherapy administration remain of paramount importance for a good outcome and the benefit for survival they convey is crucial. Sometimes the benefit the patient derives from these details is comparable to the one newer therapies convey. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

23 pages, 4189 KiB

Open AccessFeature PaperArticle

Synthesis and Characterization of New Fluoro/Trifluoromethyl-Substituted Acylthiourea Derivatives with Promising Activity against Planktonic and Biofilm-Embedded Microbial Cells

by Carmen Limban, Diana Camelia Nuta, Alexandru Vasile Missir, Roxana Roman, Miron Teodor Caproiu, Florea Dumitrascu, Lucia Pintilie, Amalia Stefaniu, Mariana Carmen Chifiriuc, Marcela Popa, Irina Zarafu, Andreea Letiția Arsene, Cristina Elena Dinu Pirvu, Denisa Ioana Udeanu and Ioana Raluca Papacocea

Processes 2020, 8(5), 503; https://doi.org/10.3390/pr8050503 - 26 Apr 2020

Cited by 10 | Viewed by 3042

Abstract

The aim of this study was preparation of new derivatives based on 2-((4-chlorophenoxy)methyl)-N-(arylcarbamothioyl)benzamide structure; the new compounds were characterized by IR, NMR (¹H, ¹³C) spectroscopy, and elemental analysis. The obtained compounds were evaluated for their in vitro antimicrobial [...] Read more.

The aim of this study was preparation of new derivatives based on 2-((4-chlorophenoxy)methyl)-N-(arylcarbamothioyl)benzamide structure; the new compounds were characterized by IR, NMR (¹H, ¹³C) spectroscopy, and elemental analysis. The obtained compounds were evaluated for their in vitro antimicrobial activity against planktonic and biofilm-embedded microbial cells (Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Candida albicans), by qualitative and quantitative assays. Some of the compounds revealed promising antibacterial and antifungal activities, with low minimum inhibitory concentration values between 0.15 and 2.5 mg/mL and minimal biofilm eradication concentrations of 0.019–2.5 mg/mL. To investigate the potential target of their antibacterial activity, in silico drug-likeness and molecular docking screenings on Staphylococcus aureus DNA gyrase were performed. The compound with the best antibacterial activity (1g) was docked into topoisomerase II DNA gyrase enzymes (PDB ID: 2XCS) and showed valuable interactions with the target protein along with good docking scores, suggesting that it can act by the inhibition of DNA replication. The tested compounds exhibited only a poor antioxidant activity, as revealed by the in vitro assay using 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

Review

Jump to: Research

16 pages, 549 KiB

Open AccessFeature PaperEditor’s ChoiceReview

COVID-19-Current Therapeutical Approaches and Future Perspectives

by Raluca Elisabeta Lupașcu (Moisi), Marina Ionela Ilie, Bruno Ștefan Velescu, Denisa Ioana Udeanu, Camelia Sultana, Simona Ruță and Andreea Letiția Arsene

Processes 2022, 10(6), 1053; https://doi.org/10.3390/pr10061053 - 25 May 2022

Cited by 1 | Viewed by 2018

Abstract

The ongoing pandemic of coronavirus disease (COVID-19) stimulated an unprecedented international collaborative effort for rapid diagnosis, epidemiologic surveillance, clinical management, prevention, and treatment. This review focuses on the current and new therapeutical approaches, summarizing the viral structure and life cycle, with an emphasis [...] Read more.

The ongoing pandemic of coronavirus disease (COVID-19) stimulated an unprecedented international collaborative effort for rapid diagnosis, epidemiologic surveillance, clinical management, prevention, and treatment. This review focuses on the current and new therapeutical approaches, summarizing the viral structure and life cycle, with an emphasis on the specific steps that can be interfered by antivirals: (a) inhibition of viral entry with anti-spike monoclonal antibodies; (b) inhibition of the RNA genome replication with nucleosidic analogs blocking the viral RNA polymerase; (c) inhibition of the main viral protease (Mpro), which directs the formation of the nonstructural proteins. An overview of the immunomodulatory drugs currently used for severe COVID-19 treatment and future therapeutical options are also discussed. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

16 pages, 513 KiB

Open AccessReview

Paracetamol-Induced Hypothermia in Rodents: A Review on Pharmacodynamics

by Laurențiu Coman, Horia Păunescu, Cristina Isabel Viorica Ghiță, Radu Ciprian Țincu, Sorina Vasile, Delia Cinteza, Ion Fulga and Oana Andreia Coman

Processes 2022, 10(4), 687; https://doi.org/10.3390/pr10040687 - 31 Mar 2022

Cited by 2 | Viewed by 3849

Abstract

Paracetamol can induce hypothermia in humans and rodents. The study’s aim is to review the mechanisms of paracetamol-induced hypothermia in rodents or the results issued from in vitro studies on the same species’ tissues (in doses that do not produce hepatic impairment) using [...] Read more.

Paracetamol can induce hypothermia in humans and rodents. The study’s aim is to review the mechanisms of paracetamol-induced hypothermia in rodents or the results issued from in vitro studies on the same species’ tissues (in doses that do not produce hepatic impairment) using the latest developments published in scientific journals over the last 15 years. Available human studies are also analysed. An extensive search in PubMed databases exploring the hypothermic response to paracetamol was conducted. 4669 articles about paracetamol’s effects on body temperature in mice or rats were found. After applying additional filters, 20 articles were selected for review, with 9 of them presented in tabular forms. The analysis of these articles found that the hypothermic effect of paracetamol is due to the inhibition of a cyclooxygenase-1 variant, is potentiated by endothelin receptor antagonists, and can be mediated through GABA_A receptors and possibly through transient receptor potential cation channel subfamily A member 1 via N-acetyl-p-benzoquinone imine in the central nervous system. Human studies confirm the in vivo and in vitro experiments in rodents regarding the presence of a hypothermic effect after high, non-toxic doses of paracetamol. Further research is required to understand the mechanisms behind paracetamol’s hypothermic effect in humans. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

10 pages, 722 KiB

Open AccessReview

Docetaxel for Breast Cancer Treatment-Side Effects on Ocular Surface, a Systematic Review

by Elena Andreea Stoicescu, Marian Burcea, Raluca Claudia Iancu, Mirela Zivari, Alina Popa Cherecheanu, Inna Adriana Bujor, Cristina Rastoaca and George Iancu

Processes 2021, 9(7), 1086; https://doi.org/10.3390/pr9071086 - 23 Jun 2021

Cited by 7 | Viewed by 4228

Abstract

Docetaxel is a very effective chemotherapeutic agent for the treatment of metastatic or locally advanced breast cancer. Epiphora (hyperlacrimation) has been shown to be the most common eye condition in patients receiving docetaxel-based chemotherapy. This symptom does not decrease visual acuity, but decreases [...] Read more.

Docetaxel is a very effective chemotherapeutic agent for the treatment of metastatic or locally advanced breast cancer. Epiphora (hyperlacrimation) has been shown to be the most common eye condition in patients receiving docetaxel-based chemotherapy. This symptom does not decrease visual acuity, but decreases the quality of life. Daily activities (reading, working on the computer, watching TV, and so on) are affected, with patients complaining about an alteration of daily life with the appearance of this symptom. The mechanism by which epiphora occurs is considered to be the canalicular stenosis, but the trials on the subject failed to reach statistical significance. The objective of this scoping review is to determine whether there is a treatment regimen-dependent relationship between docetaxel administration and the presence of epiphora in women with breast cancer. The inclusion criteria were met by 10 trials, from which one was excluded owing to data selection biases. Accordingly, nine studies were evaluated quantitatively and qualitatively in the present review. We included subjects with docetaxel as single treatment or docetaxel in combination with other chemotherapy compounds. The occurrence of epiphora among subjects treated with docetaxel, regardless of the therapeutic regimen used, was statistically significant (p = 0.005). The proportion of patients with epiphora after weekly administration of docetaxel (54 out of 131 subjects, 41.22%) was different compared with that of those who received docetaxel at three week intervals (112 out of 325 subjects, 34.15%), but the difference between the two was not statistically significant (p = 0.732). The present study demonstrates that epiphora occurs more frequently in patients receiving weekly docetaxel-based chemotherapy than those taking the three-weekly regimen, but the difference is not statistically significant. Ophthalmologic assessment of all patients starting this treatment is recommended. The causal relationship between canalicular stenosis and epiphora is not fully elucidated as long as this ocular symptom occurs in women who do not have stenosis of the lacrimal system. Further well-designed trials are required to bring new insights into the mechanisms of epiphora pathogenesis in subjects treated with docetaxel. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Figure 1

18 pages, 1201 KiB

Open AccessReview

Drug Carriers: Classification, Administration, Release Profiles, and Industrial Approach

by Paolo Trucillo

Processes 2021, 9(3), 470; https://doi.org/10.3390/pr9030470 - 06 Mar 2021

Cited by 69 | Viewed by 18679

Abstract

This work is aimed at providing a description of the complex world of drug carriers, starting from the description of this particular market in terms of revenue. Then, a brief overview of several types of conventional and innovative drug carrier systems has been [...] Read more.

This work is aimed at providing a description of the complex world of drug carriers, starting from the description of this particular market in terms of revenue. Then, a brief overview of several types of conventional and innovative drug carrier systems has been included. The types of administration routes were also analyzed, with a critical and qualitative comment on drug release kinetics and drug profile shapes. Carriers were classified according to their ability to provide a prolonged and targeted release. The concept of the therapeutic window has been presented, providing advantages of having pulsed drug release to avoid side effects to target tissues. A critical comment on the use of conventional and innovative techniques for the production of drug carriers by large industrial companies has been proposed. As a final attempt for this work, an overall unique schematization of a drug carrier production process has been added, highlighting the necessity to create a strong double link among world-requested versatility of drug carriers for human applications and the newly developed industrial processes. Full article

(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis)

► Show Figures

Graphical abstract

Journal Menu

Journal Browser

Pharmaceutical Development and Bioavailability Analysis

Share This Special Issue

Special Issue Editors

Special Issue Information

Keywords

Published Papers (23 papers)

Research

Review

Further Information

Guidelines

MDPI Initiatives

Follow MDPI