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Pharmaceutical Development and Bioavailability Analysis (Volume II)
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Pharmaceutical Development and Bioavailability Analysis (Volume II)

A special issue of Processes (ISSN 2227-9717). This special issue belongs to the section "Pharmaceutical Processes".

Deadline for manuscript submissions: 15 September 2024 | Viewed by 6972

Special Issue Editors

Prof. Dr. Andreea Letitia Arsene

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Guest Editor
Department of Pharmaceutical Microbiology, Faculty of Pharmacy, University of Medicine and Pharmacy “Carol Davila”, 020956 Bucharest, Romania
Interests: prebiotics; probiotics; microbiota; microbiology control; infectious contaminants; food safety
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Denisa Udeanu

E-Mail Website
Guest Editor
Department of Clinical Laboratory and Food Safety, Faculty of Pharmacy, University of Medicine and Pharmacy “Carol Davila”, 020956 Bucharest, Romania
Interests: nutritional evaluation; nutritional biomarkers; practical nutrition; metabolic disease; diabetes
Special Issues, Collections and Topics in MDPI journals
Dr. Bruno Velescu

E-Mail Website
Guest Editor
Department of Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, University of Medicine and Pharmacy “Carol Davila”, 37 Dionisie Lupu Str., 030167 Bucharest, Romania
Interests: drug development and analysis; pharmacokinetics; drug–drug interactions; experimental pharmacology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The frontiers of pharmaceutical development have been broadly extended over the past few years, with a significant impact on the research, design, and manufacture of both novel synthetized substances and classic molecules (whose formulations, bioavailability, and uses need updating). In the century of nanoscale, the scientific and clinical approaches of pharmaceuticals are challenging; in many cases, the necessity of emphasizing practical solutions and applications to theoretical and research-based problems occurs.

Nowadays, pharmaceutical development faces a large host of issues deriving from the particularities of each pharmacological active principle, from botanicals to biologics and biosimilars. In many cases, these molecules or already-formulated drugs create controversies regarding the bioavailability, interactions, and novel potential mechanisms of action with consequences on their efficacy and risks.

Therefore, in this Special Issue titled “Pharmaceutical Development and Bioavailability Analysis”, we encourage researchers to present the most recent studies regarding various developments in the pharmaceutical field, with a strong focus on the drugs’ bioavailability and potential effects on formulations, delivery systems, pharmacokinetics, interactions, and preclinical and clinical significance. The manuscripts may include research articles and reviews in order to advance pharmaceutical development.

Prof. Dr. Andreea Letitia Arsene
Dr. Denisa Udeanu
Dr. Bruno Velescu
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Processes is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2400 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • preformulation and pharmaceutical formulation studies
  • bioavailability studies
  • drug–drug interactions
  • design of dosage forms
  • drug delivery system research and quality improvement
  • medicinal chemistry
  • structure–property correlations
  • binding affinity
  • radiopharmaceuticals
  • animal experimentation and clinical trials

Published Papers (5 papers)

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Research

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38 pages, 12696 KiB  
Article
Exploring Partial Structural Disorder in Anhydrous Paraxanthine through Combined Experiment, Solid-State Computational Modelling, and Molecular Docking
by Jolanta Natalia Latosińska, Magdalena Latosińska, Janez Seliger and Veselko Žagar
Processes 2023, 11(9), 2740; https://doi.org/10.3390/pr11092740 - 14 Sep 2023
Cited by 1 | Viewed by 814
Abstract
Paraxanthine (PX), a major metabolite of caffeine, a protective agent against Alzheimer’s and Parkinson’s disease, and a promising drug for the treatment of post-COVID 2019 anosmia and ageusia, has been studied in the solid state and protein–ligand complex. Partial disorder in PX, caused [...] Read more.
Paraxanthine (PX), a major metabolite of caffeine, a protective agent against Alzheimer’s and Parkinson’s disease, and a promising drug for the treatment of post-COVID 2019 anosmia and ageusia, has been studied in the solid state and protein–ligand complex. Partial disorder in PX, caused by the methyl group at the N(7) position, has been modelled and discussed. The relationship between the unusual structural disorder and the propensity to form a specific system of non-covalent bonds was analyzed. Three 1H-14N NMR-NQR (nuclear magnetic resonance–nuclear quadrupole resonance) experimental techniques were used, namely multiple frequency sweeps, Larmor frequency scanning, and the two-frequency irradiation, followed by solid-state computational modelling (density functional theory, supplemented by quantum theory of atoms in molecules, 3D Hirshfeld surfaces, and reduced density gradient), and molecular docking approaches. New quantitative methods for estimating changes in the global pattern of interactions under the influence of rotation of the methyl group in N(7) based on the Pompeiu–Hausdorff and Bhattacharayya metrics and the Wasserstein distance have been proposed and applied. A spectrum consisting of 12 lines, indicating the presence of 4 chemically inequivalent nitrogen sites in the PX molecule, was recorded, and the lines’ assignment to particular sites was made. The influence of the methyl rotation on the eigenvalues and eigenvectors of the electric field gradient tensor, NQR parameters, and resonance line positions was modelled in the solid (GGA/RPBE, m-GGA/RSCAN) and cluster (Minnesota M062X hybrid). Three factors have been found to determine structural disorder in PX: larger crystal voids near the methyl at N(7) than at N(1) (opening the path for the disorder), hyperconjugation strongly affecting the density distribution in the five-membered ring, and the involvement of the methyl group at N(7) in many non-covalent bonds that intercept (capture) subsequent jumping protons. The Pompeiu–Hausdorff and Bhattacharayya metrics and the Wasserstein distance confirmed the changes in the distribution and strength of non-covalent interactions throughout the molecule as a result of methyl rotation. This effect is clearly visible regardless of the type of metric, and its order of magnitude is consistent with the modulation effect of the NQR spectra (experimental and calculated). Through molecular docking, it was discovered that the PX moiety in protein–ligand complexes adopt the same methyl group conformation at N(7) as in the solid state. It was found that the cooperation–competition between the C-H⋯O hydrogen bonds and C-H⋯H-C dispersion interactions is the crucial factor that impedes methyl rotation and induces structural disorder, as well as being an important factor in the formation of the protein–ligand complexes. Full article
(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis (Volume II))
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16 pages, 6873 KiB  
Article
Study of the Effect of Eudragit RSPO on the Photostability of Venlafaxine in a Physical Mixture and in a Melt Form
by Anna Maślanka, Marek Szlósarczyk, Przemysław Talik, Joanna Szafraniec-Szczęsny, Krzysztof Woyna-Orlewicz, Paweł Żmudzki and Urszula Hubicka
Processes 2023, 11(8), 2479; https://doi.org/10.3390/pr11082479 - 18 Aug 2023
Viewed by 733
Abstract
The effect of Eudragit RSPO on the photostability of venlafaxine in a physical mixture and as a melt was studied. A validated ultra-high-performance liquid chromatography mass spectrometry method was used to determine the content of venlafaxine alongside degradation products. The most likely structures [...] Read more.
The effect of Eudragit RSPO on the photostability of venlafaxine in a physical mixture and as a melt was studied. A validated ultra-high-performance liquid chromatography mass spectrometry method was used to determine the content of venlafaxine alongside degradation products. The most likely structures of the degradation products were determined by mass spectrometry. The samples were evaluated before and after exposure to ultraviolet A by differential scanning calorimetry and scanning electron microscopy. The kinetic parameters of the decomposition of venlafaxine in the physical mixture and melt form were calculated and comparable to those of venlafaxine as an active pharmaceutical ingredient. The results indicate that the process of venlafaxine decomposition is more than three times slower in the venlafaxine–eudragit melt than in its physical mixture with eudragit and its pure form. The strong photoprotective nature of the tested polymer against venlafaxine in the melt form was also confirmed by differential scanning calorimetry and scanning electron microscopy. Full article
(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis (Volume II))
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27 pages, 19384 KiB  
Article
Development and Experimental Evaluation of Some Silver Nanoparticles with Antimicrobial Potential
by Bruno Ștefan Velescu, Marina Ionela Ilie, Anca Ioana Amzăr, Raluca Elisabeta Lupașcu, Ilinca Mihaela Marandiuc, Miruna-Maria Apetroaei, Andreea Letiția Arsene, Emilian Ionuț Blejan, Octvian Alexandru Nedea, Toma Fistos, Radu Claudiu Fierăscu, Florica Bărbuceanu, Cristina Țoca, Irina Fierăscu, Denisa Ioana Udeanu, Manuela Ghica, Doina Drăgănescu and Pavel Călin Cobelschi
Processes 2023, 11(4), 1212; https://doi.org/10.3390/pr11041212 - 14 Apr 2023
Viewed by 1461
Abstract
By adjusting the synthesis process, silver nanoparticles (AgNp) of various shapes, sizes, and structures can be obtained, all of which have a substantial impact on the biological effect, notably, the regulation of antibacterial activity in the present circumstances of growing bacterial resistance. Due [...] Read more.
By adjusting the synthesis process, silver nanoparticles (AgNp) of various shapes, sizes, and structures can be obtained, all of which have a substantial impact on the biological effect, notably, the regulation of antibacterial activity in the present circumstances of growing bacterial resistance. Due to their relatively small size, nanoparticles may be disseminated evenly throughout the body of the experimental animal, even at low doses, and exert more potent antibacterial activities. Our research was centered on the synthesis, production, and biological evaluation of antibacterial silver nanoparticles. Using the Turkevich method, we were able to effectively synthesize and characterize nanoscale silver particles, with an average crystallite size of 9.49 nm. We examined their acute toxicity and pharmacokinetic characteristics in rats after administering a single dosage. In addition, we evaluated the biological effect of topical AgNp suspension on the progression of burn-type lesions in the experimental animals. The pharmacokinetic profile demonstrated that the plasma concentration of silver nanoparticles, as well as their clearance rate, and dispersion throughout the body, are significantly enhanced in large rodent species. The restorative effect of synthesized silver nanoparticles in the form of a suspension in distilled water was corroborated by the values of the hematological parameters. These results demonstrated an intense stimulation of the cellular and molecular processes of the local immune defense, which has resulted in significantly faster regeneration in the AgNp-treated group. Full article
(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis (Volume II))
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Review

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19 pages, 3461 KiB  
Review
Three-Dimensional Printing Technologies in Oral Films Manufacturing—A Minireview
by Emma Adriana Ozon, Iulian Sarbu, Violeta Popovici, Mirela Adriana Mitu, Adina Magdalena Musuc, Oana Karampelas and Bruno Stefan Velescu
Processes 2023, 11(9), 2628; https://doi.org/10.3390/pr11092628 - 03 Sep 2023
Viewed by 1339
Abstract
The interest in buccal drug delivery is under consideration due to some distinct properties compared to the traditional pharmaceutical formulations for oral administration: significantly higher bioavailability, a faster absorption rate of the drug, and substantial compliance for special needs patients. Oral films are [...] Read more.
The interest in buccal drug delivery is under consideration due to some distinct properties compared to the traditional pharmaceutical formulations for oral administration: significantly higher bioavailability, a faster absorption rate of the drug, and substantial compliance for special needs patients. Oral films are obtained through various technologies, from conventional tools to 3D and 4D printing approaches. This minireview aims to describe the current additive manufacturing technologies in oral film fabrication, display their advantages and limitations, and discuss various formulation strategies. It also provides advanced data regarding synthetic and natural polymers used in 3D printing technologies for oral films. Moreover, it shows the most recent studies with 3D-printed orodispersible films and mucoadhesive buccal films manufactured through previously analyzed methods. Finally, conclusions and future perspectives are also briefly summarized. Full article
(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis (Volume II))
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18 pages, 1469 KiB  
Review
Folic Acid and Its Role in Oral Health: A Narrative Review
by Cristina-Crenguța Albu, Maria-Angelica Bencze, Anca-Oana Dragomirescu, Ioana Suciu, Mihaela Tănase, Ştefan-Dimitrie Albu, Emily-Alice Russu and Ecaterina Ionescu
Processes 2023, 11(7), 1994; https://doi.org/10.3390/pr11071994 - 02 Jul 2023
Cited by 3 | Viewed by 1910
Abstract
Vitamins, exogenous organic compounds that play a vital role in metabolic reactions, and fundamental powerful antioxidants with a crucial role in the genetic transcription process, are considered essential nutritional factors. Folic acid (FA), also known as folate, or Vitamin B9, plays an indispensable [...] Read more.
Vitamins, exogenous organic compounds that play a vital role in metabolic reactions, and fundamental powerful antioxidants with a crucial role in the genetic transcription process, are considered essential nutritional factors. Folic acid (FA), also known as folate, or Vitamin B9, plays an indispensable role in various intracellular reactions, being the main pawn, with a strong impact on medical and dental science. The aim of this paper mainly focuses on presenting the latest and most advanced aspects related to the following topics: (1) the resonance that FA, and more specifically FA deficiency, has at the level of the oral cavity; (2) the elements involved in the molecular landscape, which reflect the interaction and the possible mechanisms of action, through which FA influences oral health; and (3) the particular processes by which FA deficiency causes certain clinical conditions. Moreover, we aim to draw the attention and trigger the curiosity of health professionals on the need to know the specific host–environment interactions, particularly the linkage between individual genotype and phenotypic variability, which in the future could represent the basis of novel and effective treatment methods. From this perspective, we begin by providing an overview of the general radar echo of the human body induced by FA deficiency, before focusing on the genetic strategic substrate and biochemical processes involved in the molecular mechanisms through which FA acts at the cellular level. Finally, we reflect on the resulting conclusions: (1) the complex interrelationships between different types of cytokines (CKs) and abnormal folate metabolism are involved in the occurrence of neural tube defects (NTDs) and orofacial clefts (OFCs); (2) increased oxidative stress, endothelial dysfunction, and genomic instability, induced by folate deficiency, have a major impact on periodontal health; and (3) glutamate carboxypeptidase II, GCP2 1561C>T allelic variant, constitutes the main pawn, which specifically influences the bioavailability of natural folates and FA, as the main actors, with essential roles in oral health. Full article
(This article belongs to the Special Issue Pharmaceutical Development and Bioavailability Analysis (Volume II))
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