Optimized Chitosan/Anion Polyelectrolyte Complex Based Inserts for Vaginal Delivery of Fluconazole: In Vitro/In Vivo Evaluation

Darwesh, Bayan; Aldawsari, Hibah M; Badr-Eldin, Shaimaa M.

doi:10.3390/pharmaceutics10040227

Cited by 25 publications

(18 citation statements)

References 37 publications

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“…Based on the literature reviewed previously, chitosan and HPMC are the mucoadhesive polymers that have been studied most extensively by researchers in the management of vaginal infections. It has been employed in drug-delivery systems attributed to its mucoadhesive, controlled release, and permeation-enhancing properties [ 174 ]. It is a biocompatible, safe, and biodegradable polymer that can be used together with other synthetic polymers such as HPMC, sodium alginate, and carbopol to improve the drug delivery system [ 80 , 96 , 174 ].…”

Section: Expert Opinionmentioning

confidence: 99%

“…It has been employed in drug-delivery systems attributed to its mucoadhesive, controlled release, and permeation-enhancing properties [ 174 ]. It is a biocompatible, safe, and biodegradable polymer that can be used together with other synthetic polymers such as HPMC, sodium alginate, and carbopol to improve the drug delivery system [ 80 , 96 , 174 ]. Among all the dosage forms mentioned in this review, vaginal gels contain high amount of water allowing it to apply and distribute well in the vagina, thus having better patient compliance compared to other vaginal preparations.…”

Section: Expert Opinionmentioning

confidence: 99%

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Promising Drug Delivery Approaches to Treat Microbial Infections in the Vagina: A Recent Update

et al. 2020

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An optimal host–microbiota interaction in the human vagina governs the reproductive health status of a woman. The marked depletion in the beneficial Lactobacillus sp. increases the risk of infection with sexually transmitted pathogens, resulting in gynaecological issues. Vaginal infections that are becoming increasingly prevalent, especially among women of reproductive age, require an effective concentration of antimicrobial drugs at the infectious sites for complete disease eradication. Thus, topical treatment is recommended as it allows direct therapeutic action, reduced drug doses and side effects, and self-insertion. However, the alterations in the physiological conditions of the vagina affect the effectiveness of vaginal drug delivery considerably. Conventional vaginal dosage forms are often linked to low retention time in the vagina and discomfort which significantly reduces patient compliance. The lack of optimal prevention and treatment approaches have contributed to the unacceptably high rate of recurrence for vaginal diseases. To combat these limitations, several novel approaches including nano-systems, mucoadhesive polymeric systems, and stimuli-responsive systems have been developed in recent years. This review discusses and summarises the recent research progress of these novel approaches for vaginal drug delivery against various vaginal diseases. An overview of the concept and challenges of vaginal infections, anatomy and physiology of the vagina, and barriers to vaginal drug delivery are also addressed.

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Section: Expert Opinionmentioning

confidence: 99%

Section: Expert Opinionmentioning

confidence: 99%

Promising Drug Delivery Approaches to Treat Microbial Infections in the Vagina: A Recent Update

et al. 2020

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“…The ability of CHT to interact with mucus indicates that the residence time of the CHT gel + IC at the vaginal site would be enough to provide localized sustained release of PGT. In addition, vaginal insert based on CHT showed better mucoadhesion than inserts based on carbopol which is one of the main components of Crinone® (Darwesh et al, 2018). Vaginal irritation and other undesirable effects at the site of application were reported for Crinone®.…”

Section: Resultsmentioning

confidence: 99%

“…Vaginal irritation and other undesirable effects at the site of application were reported for Crinone®. These effects would be less significant with the CHT gel + IC due to the formulation has fewer inactive ingredients and the biocompatibility of the polymer was showed in vaginal formulations based on the lack of toxicity and absence of inflammatory reactions (Tuğcu-Demiröz et al, 2013, Darwesh et al, 2018, Cook and Brown, 2018). Crinone® is applied as a gel, while the low viscosity of the thermosensitive CHT formulation ensures the capacity of covering the required surface of the tissue resulting in the in situ formation of a gel mucoadhesive layer at the physiological temperature.…”

Section: Resultsmentioning

confidence: 99%

Progesterone loaded thermosensitive hydrogel for vaginal application: Formulation and in vitro comparison with commercial product

Velazquez

Turino

Luna

et al. 2019

Saudi Pharmaceutical Journal

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Progesterone (PGT) is a natural hormone that stimulates and regulates various important functions, such as the preparation of the female body for conception and pregnancy. Due to its low water solubility, it is administered in a micronized form and/or in vehicles with specific solvents requirements. In order to improve the drug solubility, inclusion complexes of PGT and β-cyclodextrins were obtained by the freeze-drying method. Two β-cyclodextrins (native and methylated) in two solvents (water and water:ethanol) and different molar ratio of the reagents were the variables tested for the selection of the best condition for the preparation of the complexes. The PGT/randomly methylated-β-cyclodextrin complexes were incorporated into chitosan thermosensitive hydrogels, as an alternative formulation for the vaginal administration of PGT. Neither the micro and macroscopic characteristics of the gels nor the transition time from solution to gel were modified after the complexes incorporation. In addition, chitosan gels with complexes resisted better the degradation in simulated vaginal fluid in comparison to commercial gel (Crinone®). The chitosan gel with inclusion complexes and Crinone® were tested in vitro in a diffusion assay to evaluate the delivery of the hormone and its diffusion through porcine epithelial mucosa obtained from vaginal tissue. Chitosan gel presented sustained diffusion similar to the exhibited by commercial gel. The use of chitosan gels with inclusion complexes based on cyclodextrins would be a viable alternative for vaginal administration of PGT.

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“…Among different materials used for the formation of PECs with CS dedicated for mucosal administration, polyanionic natural gums with anionic carboxylic acid groups, such as gellan [ 22 ], Arabic [ 23 ] and xanthan gum (XG) [ 24 ], arouse great interest of researchers, while the combination of CS with tragacanth gum (TG) is a relatively new technological approach.…”

Section: Introductionmentioning

confidence: 99%

Tragacanth Gum/Chitosan Polyelectrolyte Complexes-Based Hydrogels Enriched with Xanthan Gum as Promising Materials for Buccal Application

et al. 2020

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Polyelectrolyte complexes based on the electrostatic interactions between the polymers mixed are of increasing importance, therefore, the aim of this study was to develop hydrogels composed of anionic tragacanth gum and cationic chitosan with or without the addition of anionic xanthan gum as carriers for buccal drug delivery. Besides the routine quality tests evaluating the hydrogel’s applicability on the buccal mucosa, different methods directed toward the assessment of the interpolymer complexation process (e.g., turbidity or zeta potential analysis, scanning electron microscopy and Fourier-transform infrared spectroscopy) were employed. The addition of xanthan gum resulted in stronger complexation of chitosan that affected the hydrogel’s characteristics. The formation of a more viscous PEC hydrogel with improved mucoadhesiveness and mechanical strength points out the potential of such polymer combination in the development of buccal drug dosage forms.

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Optimized Chitosan/Anion Polyelectrolyte Complex Based Inserts for Vaginal Delivery of Fluconazole: In Vitro/In Vivo Evaluation

Cited by 25 publications

References 37 publications

Promising Drug Delivery Approaches to Treat Microbial Infections in the Vagina: A Recent Update

Promising Drug Delivery Approaches to Treat Microbial Infections in the Vagina: A Recent Update

Progesterone loaded thermosensitive hydrogel for vaginal application: Formulation and in vitro comparison with commercial product

Tragacanth Gum/Chitosan Polyelectrolyte Complexes-Based Hydrogels Enriched with Xanthan Gum as Promising Materials for Buccal Application

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