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20 pages, 4286 KiB

Open AccessArticle

Chitosan and Anionic Solubility Enhancer Sulfobutylether-β-Cyclodextrin-Based Nanoparticles as Dexamethasone Ophthalmic Delivery System for Anti-Inflammatory Therapy

by Giuseppe Francesco Racaniello, Gennaro Balenzano, Ilaria Arduino, Rosa Maria Iacobazzi, Antonio Lopalco, Angela Assunta Lopedota, Hakon Hrafn Sigurdsson and Nunzio Denora

Pharmaceutics 2024, 16(2), 277; https://doi.org/10.3390/pharmaceutics16020277 - 16 Feb 2024

Viewed by 988

Abstract

Cataract surgery interventions are constantly increasing, particularly among adult and elderly patients. This type of surgery can lead to inflammatory states of the ocular anterior segment (AS), usually healed via postoperative treatment with dexamethasone (DEX)-containing eye drops. The application of eye drops is [...] Read more.

Cataract surgery interventions are constantly increasing, particularly among adult and elderly patients. This type of surgery can lead to inflammatory states of the ocular anterior segment (AS), usually healed via postoperative treatment with dexamethasone (DEX)-containing eye drops. The application of eye drops is challenging due to the high number of daily administrations. In this study, mucoadhesive nanoparticles (NPs) were formulated to improve the residence time of DEX on the corneal mucosa, enhancing the drug’s solubility and bioavailability. The NPs were generated using an ionotropic gelation technique, exploiting the interaction between the cationic group of chitosan (CS) and the anionic group of sulfobutylether-β-cyclodextrin (SBE-β-CD). The formation of the inclusion complex and its stoichiometry were studied through phase solubility studies, Job’s plot method, and Bi-directional transport studies on MDCKII-MDR1. The obtained NPs showed good chemical and physical characteristics suitable for drug loading and subsequent testing on animal mucosa. The DEX-loaded CS/SBE-β-CD NPs exhibited a prolonged residence time on animal mucosa and demonstrated enhanced drug permeability through the corneal membrane, showing a sustained release profile. The developed NPs posed no irritation or toxicity concerns upon local administration, making them an optimal and innovative drug delivery system for inflammatory AS diseases treatment. Full article

(This article belongs to the Special Issue Development of Chitosan/Cyclodextrins in Drug Delivery Field)

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19 pages, 6132 KiB

Open AccessArticle

Study of the Early Effects of Chitosan Nanoparticles with Glutathione in Rats with Osteoarthrosis

by Patricia Ramírez-Noguera, Iliane Zetina Marín, Blanca Margarita Gómez Chavarin, Moisés Eduardo Valderrama, Laura Denise López-Barrera and Roberto Díaz-Torres

Pharmaceutics 2023, 15(8), 2172; https://doi.org/10.3390/pharmaceutics15082172 - 21 Aug 2023

Viewed by 1121

Abstract

Due to cartilage’s limited capacity for regeneration, numerous studies have been conducted to find new drugs that modify osteoarthrosis’s progression. Some evidence showed the capability of chitosan nanoparticles with glutathione (Np-GSH) to regulate the oxide-redox status in vitro in human chondrocytes. This work [...] Read more.

Due to cartilage’s limited capacity for regeneration, numerous studies have been conducted to find new drugs that modify osteoarthrosis’s progression. Some evidence showed the capability of chitosan nanoparticles with glutathione (Np-GSH) to regulate the oxide-redox status in vitro in human chondrocytes. This work aimed to evaluate the capacity of Np-GSH in vivo, using Wistar rats with induced surgical osteoarthritis. Radiographic, biochemical (GSH and TBARS quantification), histopathological, and immunohistochemical (Col-2 and MMP-13) analyses were performed to evaluate the progress of the osteoarthritic lesions after the administration of a single dose of Np-GSH. According to the results obtained, the GSH contained in the NPs could be vectored to chondrocytes and used by the cell to modulate the oxidative state reduction, decreasing the production of ROS and free radicals induced by agents oxidizing xenobiotics, increasing GSH levels, as well as the activity of GPx, and decreasing lipid peroxidation. These results are significant since the synthesis of GSH develops exclusively in the cell cytoplasm, and its quantity under an oxidation–reduction imbalance may be defective. Therefore, the results allow us to consider these nanostructures as a helpful study tool to reduce the damage associated with oxidative stress in various diseases such as osteoarthritis. Full article

(This article belongs to the Special Issue Development of Chitosan/Cyclodextrins in Drug Delivery Field)

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23 pages, 2279 KiB

Open AccessArticle

Comparative Serum and Brain Pharmacokinetics of Quercetin after Oral and Nasal Administration to Rats as Lyophilized Complexes with β-Cyclodextrin Derivatives and Their Blends with Mannitol/Lecithin Microparticles

by Konstantina Manta, Paraskevi Papakyriakopoulou, Anna Nikolidaki, Evangelos Balafas, Nikolaos Kostomitsopoulos, Sabrina Banella, Gaia Colombo and Georgia Valsami

Pharmaceutics 2023, 15(8), 2036; https://doi.org/10.3390/pharmaceutics15082036 - 28 Jul 2023

Cited by 2 | Viewed by 1407

Abstract

Quercetin (Que) is one of the most studied flavonoids with strong antioxidant properties ascribed to its ability to bind free radicals and inactivate them. However, the low solubility of the compound along with its inadequate absorption after oral administration limit its beneficial effects. [...] Read more.

Quercetin (Que) is one of the most studied flavonoids with strong antioxidant properties ascribed to its ability to bind free radicals and inactivate them. However, the low solubility of the compound along with its inadequate absorption after oral administration limit its beneficial effects. Que’s complexation with two different cyclodextrin (CD) derivatives (hydroxypropyl-β-CD and methyl-β-CD) via the neutralization/lyophilization method has been found to improve its physicochemical properties. Moreover, blends of the lyophilized powders with mannitol/lecithin microparticles (MLMPs) have been proposed as candidates for intranasal (IN) administration after in vitro and ex vivo evaluations. In this context, a comparative pharmacokinetic (PK) study of the IN vs oral administration of Que lyophilized powders and their blends with MLMPs (75:25 w/w) was performed on Wistar rats. The PK parameters estimated by a non-compartmental analysis using the sparse data methodology in Phoenix^® 8.3 (Certara, Princeton, NJ, USA) illustrated the effectiveness of IN administration either in brain targeting or in reaching the bloodstream. Significant levels of the compound were achieved at both sites, compared to those after oral delivery which were negligible. These results favor the potential application of the prepared Que nasal powders for systemic and nose-to-brain delivery for the prevention and/or treatment of neuroinflammatory degenerative conditions, such as Parkinson’s and Alzheimer’s disease. Full article

(This article belongs to the Special Issue Development of Chitosan/Cyclodextrins in Drug Delivery Field)

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18 pages, 8462 KiB

Open AccessEditor’s ChoiceArticle

Effects of Adding Chitosan on Drug Entrapment Efficiency and Release Duration for Paclitaxel-Loaded Hydroxyapatite—Gelatin Composite Microspheres

by Meng-Ying Wu, I-Fang Kao, Chien-Yao Fu and Shiow-Kang Yen

Pharmaceutics 2023, 15(8), 2025; https://doi.org/10.3390/pharmaceutics15082025 - 26 Jul 2023

Cited by 2 | Viewed by 1296

Abstract

Hydroxyapatite—gelatin microspheres with cone-like pores were synthesized via the wet-chemical method using ammonium dihydrogen phosphate ((NH₄)H₂PO₄) and calcium nitrate (Ca(NO₃)₂·4H₂O) as a source of calcium and phosphate ions with the addition [...] Read more.

Hydroxyapatite—gelatin microspheres with cone-like pores were synthesized via the wet-chemical method using ammonium dihydrogen phosphate ((NH₄)H₂PO₄) and calcium nitrate (Ca(NO₃)₂·4H₂O) as a source of calcium and phosphate ions with the addition of gelatin, which proved to be more osteoconductive than commercial products, such as fibrin glue and Osteoset^® Bone Graft Substitute. Following the method of the previous study for loading paclitaxel (PTX), a drug entrapment efficiency of around 58% was achieved, which is much lower than that of the doxorubicin (DOX)-loaded one. Since PTX is hydrophobic while DOX is hydrophilic, the order of chitosan processing and addition of the solvent were tuned in this study, finally leading to an increase in drug entrapment efficiency of 94%. Additionally, the release duration of PTX exceeded six months. The MTT assay indicated that the effect of drug release on the suppression of cancer cells reached more than 40% after one week, thereby showcasing PTX’s capacity to carry out its medicinal functions without being affected by the loading procedures. Full article

(This article belongs to the Special Issue Development of Chitosan/Cyclodextrins in Drug Delivery Field)

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18 pages, 2028 KiB

Open AccessArticle

Design, Evaluation and Comparison of Nanostructured Lipid Carriers and Chitosan Nanoparticles as Carriers of Poorly Soluble Drugs to Develop Oral Liquid Formulations Suitable for Pediatric Use

by Giulia Nerli, Lídia M. D. Gonçalves, Marzia Cirri, António J. Almeida, Francesca Maestrelli, Natascia Mennini and Paola A. Mura

Pharmaceutics 2023, 15(4), 1305; https://doi.org/10.3390/pharmaceutics15041305 - 21 Apr 2023

Cited by 4 | Viewed by 1542

Abstract

There is a serious need of pediatric drug formulations, whose lack causes the frequent use of extemporaneous preparations obtained from adult dosage forms, with consequent safety and quality risks. Oral solutions are the best choice for pediatric patients, due to administration ease and [...] Read more.

There is a serious need of pediatric drug formulations, whose lack causes the frequent use of extemporaneous preparations obtained from adult dosage forms, with consequent safety and quality risks. Oral solutions are the best choice for pediatric patients, due to administration ease and dosage-adaptability, but their development is challenging, particularly for poorly soluble drugs. In this work, chitosan nanoparticles (CSNPs) and nanostructured lipid carriers (NLCs) were developed and evaluated as potential nanocarriers for preparing oral pediatric solutions of cefixime (poorly soluble model drug). The selected CSNPs and NLCs showed a size around 390 nm, Zeta-potential > 30 mV, and comparable entrapment efficiency (31–36%), but CSNPs had higher loading efficiency (5.2 vs. 1.4%). CSNPs maintained an almost unchanged size, homogeneity, and Zeta-potential during storage, while NLCs exhibited a marked progressive Zeta-potential decrease. Drug release from CSNPs formulations (differently from NLCs) was poorly affected by gastric pH variations, and gave rise to a more reproducible and controlled profile. This was related to their behavior in simulated gastric conditions, where CSNPs were stable, while NLCs suffered a rapid size increase, up to micrometric dimensions. Cytotoxicity studies confirmed CSNPs as the best nanocarrier, proving their complete biocompatibility, while NLCs formulations needed 1:1 dilution to obtain acceptable cell viability values. Full article

(This article belongs to the Special Issue Development of Chitosan/Cyclodextrins in Drug Delivery Field)

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20 pages, 10178 KiB

Open AccessArticle

Voriconazole Cyclodextrin Based Polymeric Nanobeads for Enhanced Solubility and Activity: In Vitro/In Vivo and Molecular Simulation Approach

by Mudassir Farooq, Faisal Usman, Mahrukh Naseem, Hanan Y. Aati, Hassan Ahmad, Sirikhwan Manee, Ruqaiya Khalil, Kashif ur Rehman Khan, Muhammad Imran Qureshi and Muhammad Umair

Pharmaceutics 2023, 15(2), 389; https://doi.org/10.3390/pharmaceutics15020389 - 24 Jan 2023

Cited by 6 | Viewed by 2003

Abstract

Hydroxypropyl β-cyclodextrin (HPβCD) based polymeric nanobeads containing voriconazole (VRC) were fabricated by free radical polymerization using N, N′-methylene bisacrylamide (MBA) as a cross-linker, 2-acrylamide-2-methylpropane sulfonic acid (AMPS) as monomer and ammonium persulfate (APS) as reaction promoter. Optimized formulation (CDN5) had a particle [...] Read more.

Hydroxypropyl β-cyclodextrin (HPβCD) based polymeric nanobeads containing voriconazole (VRC) were fabricated by free radical polymerization using N, N′-methylene bisacrylamide (MBA) as a cross-linker, 2-acrylamide-2-methylpropane sulfonic acid (AMPS) as monomer and ammonium persulfate (APS) as reaction promoter. Optimized formulation (CDN5) had a particle size of 320 nm with a zeta potential of −35.5 mV and 87% EE. Scanning electron microscopy (SEM) depicted porous and non-spherical shaped beads. No evidence of chemical interaction was evident in FT-IR studies, whereas distinctive high-intensity VRC peaks were found superimposed in XRD. A stable polymeric network formation was evident in DSC studies owing to a lower breakdown in VRC loaded HPβCD in comparison to blank HPβCD. In vitro release studies showed 91 and 92% drug release for optimized formulation at pH 1.2 and 6.8, respectively, with first-order kinetics as the best-fit model and non-Fickian diffusion as the release mechanism. No evidence of toxicity was observed upon oral administration of HPβCD loaded VRC polymeric nanobeads owing to with cellular morphology of vital organs as observed in histopathology. Molecular docking indicates the amalgamation of the compounds highlighting the hydrophobic patching mediated by nanogel formulation. It can be concluded that the development of polymeric nanobeads can be a promising tool to enhance the solubility and efficacy of hydrophobic drugs such as VRC besides decreased toxicity and for effective management of fungal infections. Full article

(This article belongs to the Special Issue Development of Chitosan/Cyclodextrins in Drug Delivery Field)

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11 pages, 2020 KiB

Open AccessArticle

Concentration-Dependent Antibacterial Activity of Chitosan on Lactobacillus plantarum

by Renátó Kovács, Lóránd Erdélyi, Ferenc Fenyvesi, Noémi Balla, Fruzsina Kovács, György Vámosi, Ágnes Klusóczki, Alexandra Gyöngyösi, Ildikó Bácskay, Miklós Vecsernyés and Judit Váradi

Pharmaceutics 2023, 15(1), 18; https://doi.org/10.3390/pharmaceutics15010018 - 21 Dec 2022

Cited by 6 | Viewed by 1725

Abstract

The antimicrobial effect of chitosan and synthetic chitosan derivatives has been confirmed on many Gram-positive and Gram-negative bacteria and fungi. The tests were carried out on pathogenic microorganisms, so the mechanism and concentration dependence of the inhibitory effect of chitosan were revealed. We [...] Read more.

The antimicrobial effect of chitosan and synthetic chitosan derivatives has been confirmed on many Gram-positive and Gram-negative bacteria and fungi. The tests were carried out on pathogenic microorganisms, so the mechanism and concentration dependence of the inhibitory effect of chitosan were revealed. We conducted our tests on a probiotic strain, Lactobacillus plantarum. Commercially available chitosan derivatives of different molecular weights were added to L. plantarum suspension in increasing concentrations. The minimum inhibitory concentration (MIC) value of chitosan was determined and confirmed the viability decreasing effect at concentrations above the MIC with a time-kill assay. The release of bacterium cell content was measured at 260 nm after treatment with 0.001–0.1% concentration chitosan solution. An increase in the permeability of the cell membrane was observed only with the 0.1% treatment. The interaction was also investigated by zeta potential measurement, and the irreversible interaction and concentration dependence were established in all concentrations. The interaction of fluorescein isothiocyanate (FITC) labeled low molecular weight chitosan and bacterial cells labeled with membrane dye (FM^® 4–64) was confirmed by confocal microscopy. In conclusion, the inhibitory effect of chitosan was verified on a probiotic strain, which is an undesirable effect in probiotic preparations containing chitosan additives, while the inhibitory effect experienced with pathogenic strains is beneficial. Full article

(This article belongs to the Special Issue Development of Chitosan/Cyclodextrins in Drug Delivery Field)

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19 pages, 1613 KiB

Open AccessArticle

Assisted Extraction with Cyclodextrins as a Way of Improving the Antidiabetic Activity of Actinidia Leaves

by Szymon Sip, Anna Gościniak, Piotr Szulc, Jarosław Walkowiak and Judyta Cielecka-Piontek

Pharmaceutics 2022, 14(11), 2473; https://doi.org/10.3390/pharmaceutics14112473 - 16 Nov 2022

Cited by 4 | Viewed by 1294

Abstract

Five varieties of Actinidia leaves (Geneva, Jumbo, Ken’s Red, Kijivska Hibridna, and Sentyabraskaya) were analyzed. The profiles of active compounds were determined, namely quercetin, rutin, epicatechin, chlorogenic acid, and kaempferol, in the raw material. Suspecting that the raw material might prove important in [...] Read more.

Five varieties of Actinidia leaves (Geneva, Jumbo, Ken’s Red, Kijivska Hibridna, and Sentyabraskaya) were analyzed. The profiles of active compounds were determined, namely quercetin, rutin, epicatechin, chlorogenic acid, and kaempferol, in the raw material. Suspecting that the raw material might prove important in the treatment of diabetes, the authors assessed the antioxidant activity and the ability to inhibit enzymes responsible for the development of diabetes (α-glucosidase and α-amylase). As a result of the conducted analysis, the Ken’s Red variety was indicated as having the highest biological activity (DPPH IC₅₀ = 0.332 ± 0.048; FRAP IC_0.5 = 0.064 ± 0.005; α-glucosidase inhibition IC₅₀ = 0.098 ± 0.007; α-amylase inhibition IC₅₀ = 0.083 ± 0.004). In order to increase the efficiency of the extraction of active compounds from Ken’s Red variety leaves, cyclodextrins (α-CD, β-CD, and γ-CD) were used as extraction process enhancers. The obtained results showed a significant increase in the contents of extracted active compounds. In addition, the type of CD used enhanced the extraction of selected compounds (quercetin, kaempferol, rutin, chlorogenic acid, and epicatechin. This study shows that the application of cyclodextrin-based extraction significantly improved the leaf activity of the Ken’s Red variety (DPPH IC₅₀ = 0.160 ± 0.019; FRAP IC_0.5 = 0.008 ± 0.001; α-glucosidase inhibition IC₅₀ = 0.040 ± 0.002; α-amylase inhibition IC₅₀ = 0.012 ± 0.003). Full article

(This article belongs to the Special Issue Development of Chitosan/Cyclodextrins in Drug Delivery Field)

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16 pages, 2599 KiB

Open AccessArticle

Chitosan as a Functional Carrier for the Local Delivery Anti-Inflammatory Systems Containing Scutellariae baicalensis radix Extract

by Magdalena Paczkowska-Walendowska and Judyta Cielecka-Piontek

Pharmaceutics 2022, 14(10), 2148; https://doi.org/10.3390/pharmaceutics14102148 - 10 Oct 2022

Cited by 9 | Viewed by 1371

Abstract

The aim of the study was to establish the influence of chitosan on the preparation of systems containing Scutellariae baicalensis radix extract and to demonstrate the potential of anti-inflammatory action for the treatment of periodontitis. In the first stage, the impact of the [...] Read more.

The aim of the study was to establish the influence of chitosan on the preparation of systems containing Scutellariae baicalensis radix extract and to demonstrate the potential of anti-inflammatory action for the treatment of periodontitis. In the first stage, the impact of the variables (extraction mixture composition, temperature, and the number of extraction cycles) on the extracted samples’ biological characteristics was analyzed using the Design of Experiments (DoE) approach. The best conditions for baicalin, baicalein, and wogonin extraction from Scutellariae baicalensis radix were 80% methanol in the extraction mixture, 70 °C, and 4 cycles per 60 min. The DoE approach can be used to choose the best chitosan system parameters with equal success. An increase in the deacetylation degree of chitosan used in the system improved the potential for reducing free radicals and inhibiting the hyaluronidase enzyme. Also, increasing the degree of chitosan deacetylation results in increased resistance of the carrier to biodegradation and an extended baicalin release profile, which is also associated with an increase in the viscosity of the chitosan-based system. In total, the system of a freeze-dried extract with chitosan 90/500 in the ratio of 2:1 (system S9) turns out to be the one with the best physicochemical (high percentage of baicalin release and the highest viscosity conditioning the prolonged stay at the site of administration) and biological properties (the highest antioxidant and anti-inflammatory activities), resulting in the highest potential for use in the treatment of oral inflammatory diseases. Full article

(This article belongs to the Special Issue Development of Chitosan/Cyclodextrins in Drug Delivery Field)

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17 pages, 3885 KiB

Open AccessArticle

Novel 3D-Printed Dressings of Chitosan–Vanillin-Modified Chitosan Blends Loaded with Fluticasone Propionate for Treatment of Atopic Dermatitis

by Georgia Michailidou and Dimitrios N. Bikiaris

Pharmaceutics 2022, 14(9), 1966; https://doi.org/10.3390/pharmaceutics14091966 - 18 Sep 2022

Cited by 4 | Viewed by 1695

Abstract

In the present study, the blends of CS and Vanillin–CS derivative (VACS) were utilized for the preparation of printable inks for their application in three-dimensional (3D) printing procedures. Despite the synergic interaction between the blends, the addition of ι-carrageenan (iCR) as a thickening [...] Read more.

In the present study, the blends of CS and Vanillin–CS derivative (VACS) were utilized for the preparation of printable inks for their application in three-dimensional (3D) printing procedures. Despite the synergic interaction between the blends, the addition of ι-carrageenan (iCR) as a thickening agent was mandatory. Their viscosity analysis was conducted for the evaluation of the optimum CS/VACS ratio. The shear thinning behavior along with the effect of the temperature on viscosity values were evident. Further characterization of the 3D-printed structures was conducted. The effect of the CS/VACS ratio was established through swelling and contact angle measurements. An increasing amount of VACS resulted in lower swelling ability along with higher hydrophobicity. Fluticasone propionate (FLU), a crystalline synthetic corticosteroid, was loaded into the CS/VACS samples. The drug was loaded in its amorphous state, and consequently, its in vitro release was significantly enhanced. An initial burst release, followed by a sustained release profile, was observed. Full article

(This article belongs to the Special Issue Development of Chitosan/Cyclodextrins in Drug Delivery Field)

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Review

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33 pages, 3251 KiB

Open AccessReview

Chitosan and Cyclodextrins—Versatile Materials Used to Create Drug Delivery Systems for Gastrointestinal Cancers

by Alfred Najm, Adelina-Gabriela Niculescu, Alexandra Bolocan, Marius Rădulescu, Alexandru Mihai Grumezescu, Mircea Beuran and Bogdan Severus Gaspar

Pharmaceutics 2024, 16(1), 43; https://doi.org/10.3390/pharmaceutics16010043 - 27 Dec 2023

Viewed by 1470

Abstract

Gastrointestinal cancers are characterized by a frequent incidence, a high number of associated deaths, and a tremendous burden on the medical system and patients worldwide. As conventional chemotherapeutic drugs face numerous limitations, researchers started to investigate better alternatives for extending drug efficacy and [...] Read more.

Gastrointestinal cancers are characterized by a frequent incidence, a high number of associated deaths, and a tremendous burden on the medical system and patients worldwide. As conventional chemotherapeutic drugs face numerous limitations, researchers started to investigate better alternatives for extending drug efficacy and limiting adverse effects. A remarkably increasing interest has been addressed to chitosan and cyclodextrins, two highly versatile natural carbohydrate materials endowed with unique physicochemical properties. In this respect, numerous studies reported on fabricating various chitosan and cyclodextrin-based formulations that enabled prolonged circulation times, improved cellular internalization of carried drugs, preferential uptake by the targeted cells, reduced side effects, enhanced apoptosis rates, and increased tumor suppression rates. Therefore, this paper aims to briefly present the advantageous properties of these oligo- and polysaccharides for designing drug delivery systems, further focusing the discussion on nanocarrier systems based on chitosan/cyclodextrins for treating different gastrointestinal cancers. Specifically, there are reviewed studies describing promising solutions for colorectal, liver, gastric, pancreatic, and other types of cancers of the digestive system towards creating an updated framework of what concerns anticancer chitosan/cyclodextrin-based drug delivery systems. Full article

(This article belongs to the Special Issue Development of Chitosan/Cyclodextrins in Drug Delivery Field)

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53 pages, 8211 KiB

Open AccessEditor’s ChoiceReview

Cyclodextrin Inclusion Complexes for Improved Drug Bioavailability and Activity: Synthetic and Analytical Aspects

by Álvaro Sarabia-Vallejo, María del Mar Caja, Ana I. Olives, M. Antonia Martín and J. Carlos Menéndez

Pharmaceutics 2023, 15(9), 2345; https://doi.org/10.3390/pharmaceutics15092345 - 19 Sep 2023

Cited by 5 | Viewed by 2770

Abstract

Many active pharmaceutical ingredients show low oral bioavailability due to factors such as poor solubility and physical and chemical instability. The formation of inclusion complexes with cyclodextrins, as well as cyclodextrin-based polymers, nanosponges, and nanofibers, is a valuable tool to improve the oral [...] Read more.

Many active pharmaceutical ingredients show low oral bioavailability due to factors such as poor solubility and physical and chemical instability. The formation of inclusion complexes with cyclodextrins, as well as cyclodextrin-based polymers, nanosponges, and nanofibers, is a valuable tool to improve the oral bioavailability of many drugs. The microencapsulation process modifies key properties of the included drugs including volatility, dissolution rate, bioavailability, and bioactivity. In this context, we present relevant examples of the stabilization of labile drugs through the encapsulation in cyclodextrins. The formation of inclusion complexes with drugs belonging to class IV in the biopharmaceutical classification system as an effective solution to increase their bioavailability is also discussed. The stabilization and improvement in nutraceuticals used as food supplements, which often have low intestinal absorption due to their poor solubility, is also considered. Cyclodextrin-based nanofibers, which are polymer-free and can be generated using environmentally friendly technologies, lead to dramatic bioavailability enhancements. The synthesis of chemically modified cyclodextrins, polymers, and nanosponges based on cyclodextrins is discussed. Analytical techniques that allow the characterization and verification of the formation of true inclusion complexes are also considered, taking into account the differences in the procedures for the formation of inclusion complexes in solution and in the solid state. Full article

(This article belongs to the Special Issue Development of Chitosan/Cyclodextrins in Drug Delivery Field)

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