Engineering tenofovir loaded chitosan nanoparticles to maximize microbicide mucoadhesion

Meng, Jianing; Sturgis, Timothy F.; Youan, Bi‐Botti C.

doi:10.1016/j.ejps.2011.06.007

Cited by 152 publications

(91 citation statements)

References 68 publications

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“…The chitosan formulation presented a high potential for the release of antimicrobial agents due to controlled release, bioadhesion, and safety. 23 The incorporation of nanostructured systems, such as nanocapsules, into chitosan gels represents the unification of different systems with interesting properties, as previously mentioned. The incorporation of Eudragit ® RS 100 nanocapsules (Evonik Industries AG, Essen, Germany) in chitosan hydrogels and the controlled-release property of the formulation has already been described.…”

Section: Introductionmentioning

confidence: 99%

“…2 The use of chitosan vehicles and nanoparticles for vaginal delivery have been reported by some scholars. 3,4,23 For instance, hydrogels formed by chitosan derivatives have shown higher adhesion to pig vaginal mucosa than a commercial gel. 3 The citrate salt of chitosan has been proven to be suitable for the preparation of gels incorporating substances with low permeation potential for vaginal administration.…”

Section: Introductionmentioning

confidence: 99%

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Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery

Frank¹,

Sandri²,

D’Autilia³

et al. 2014

IJN

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The vaginal route of administration is an alternative for several treatments for either local or systemic pharmacological effects. However, the permanence of a drug in this route represents a challenge for formulation development that can be overcome by using nanoencapsulation and chitosan gel. Thus, this work aimed to evaluate the performance of chitosan hydrogels containing cationic and anionic acrylic-based nanocapsules (Eudragit ® RS 100 and Eudragit ® S 100, respectively) with Nile red as a model of lipophilic substance in the vaginal route of administration, as measured by increases in the residence time and the penetration of these formulations. Several formulations were prepared with increasing chitosan concentrations, and were analyzed in terms of pH and rheological behavior so that the most suitable formulation could be selected. The enhancement of the adhesion (tensile stress test and washability profile) and penetration (confocal laser scanning microscopy and extraction followed by quantification) properties of the formulations, when applied to porcine vaginal mucosa, were evaluated. The nanocapsule suspensions produced presented adequate properties: size of approximately 200 nm (polydispersity index of ≤v0.2); zeta potential around +10 mV for the cationic formulation and -10 mV for the anionic formulation; and pH values of 6.1±0.1 (Eudragit RS 100), 5.3±0.2 (Eudragit S 100), 6.2±0.1 (Nile red loaded Eudragit RS 100), and 5.1±0.1 (Nile red loaded Eudragit S 100). The chitosan formulation presented suitable viscosity for vaginal application and acidic pH (approximately 4.5). The tensile stress test showed that both formulations containing polymeric nanocapsules presented higher mucoadhesion when compared with the formulation without nanocapsules. In the washability experiment, no significant differences were found between formulations. Confocal microscopy and fluorescence quantification after extraction from the mucosa showed higher penetration of Nile red when it was nanoencapsulated, particularly in cationic nanocapsules. The formulations developed based on chitosan gel vehicle at 2.5% weight/weight containing polymeric nanocapsules, especially the cationic nanocapsules, demonstrated applicability for the vaginal delivery of hydrophobic substances.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery

Frank¹,

Sandri²,

D’Autilia³

et al. 2014

IJN

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“…[8][9][10] Among polycations, it has received considerable attention for its safety-recent studies have shown that chitosan and its derivatives had no cytotoxic effect on vaginal epithelial cells. 11,12) Chitosan is also reported to show penetration enhancement properties by improving the active agent transport through epithelium layer containing tight junctions. 12) In addition, it possesses antibacterial and antifungal activity 13) and due to its good mucoadhesive properties resulted from the cationic behaviour and the presence of free hydroxyl and amine groups enabling polymer to interact with mucin by hydrogen and electrostatic bonding-chitosan is regarded as a suitable excipient to prepare buccal and vaginal dosage forms.…”

Section: -7)mentioning

confidence: 99%

Vaginal Chitosan Tablets with Clotrimazole—Design and Evaluation of Mucoadhesive Properties Using Porcine Vaginal Mucosa, Mucin and Gelatine

et al. 2014

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Topical administration of clotrimazole represents the common use therapy in the antimycotic genitourinary tract treatment. Due to the fast self-cleaning action of the vagina, commercially available vaginal dosage forms with clotrimazole cannot assure prolonged contact time with mucosa, therefore the main objective of this study was to develop a dosage form for vaginal administration of clotrimazole using chitosan-a biodegradable and biocompatible derivative of chitin. Tablets mucoadhesive properties were examined using texture analyser under the presence of porcine vaginal mucosa and two different models of adhesive layersmucin gel and gelatine discs. In addition, friability, hardness, swelling behaviour, residence time, surface morphology of the performed tablets, the in vitro release profile of clotrimazole and clotrimazole release kinetics were determined. The release of clotrimazole from formulations with 25 or 40% of chitosan (F2 and F3) followed non Fickian diffusion through chitosan-gel layer and was retarded up to 6 h. Additionally, tablets F2 showed the best results in terms of mucoadhesive properties and appeared to be a good alternative to commercially available antimycotic vaginal dosage forms.

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“…One demonstrate chitosan nanoparticle as a potential microbicide delivery system with a safe bioadhesive and control release properties [223]. In another approach, Belletti and coworkers investigated tenofovir loaded nanoparticle of chitosan and/or poly-(d,l-lactide-coglycolide) (PLGA).…”

Section: Prevention Of Human Immune Deficiency (Hiv) Virus Infectionmentioning

confidence: 99%

Polysaccharide Based Formulations for Mucosal Drug Delivery: A Review

Boateng

Okeke²,

Khan³

2015

CPD

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There has been increased interest in novel drug delivery systems to be administered via mucosal routes as an alternative to the currently used traditional routes such as parenteral (injections) and oral routes of administration. This is due to the several advantages they offer including avoiding first pass metabolism in the liver for oral administration and local activity which avoids the need for high systemic doses. To achieve the foregoing objectives, bioadhesive vehicles are required that ensure prolonged residence time to achieve systemic bioavailability via substantial drug absorption or significant drug concentration for local action.The drug delivery system is also required to be non-deleterious to the site of application and be well tolerated by vulnerable groups such as paediatric and geriatric patients. These essential characteristics are mainly satisfied by naturally occurring polymers, including polysaccharide based polymers which have the advantage of biocompatibility, biodegradability and therefore safety. This review discusses various bioadhesive polymers of polysaccharide origin formulated into a variety of dosage forms for drug delivery via the body's mucosal (moist) surfaces including ocular, oral (buccal and sublingual), nasal, gastrointestinal and vaginal mucosa, as well as moist wound sites. The anatomy and / or physiology of each site, coupled with the unique challenges each poses, the strategies employed for ensuring therapeutic efficacy, as well as the current state of the art will also be covered.

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Engineering tenofovir loaded chitosan nanoparticles to maximize microbicide mucoadhesion

Cited by 152 publications

References 68 publications

Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery

Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery

Vaginal Chitosan Tablets with Clotrimazole—Design and Evaluation of Mucoadhesive Properties Using Porcine Vaginal Mucosa, Mucin and Gelatine

Polysaccharide Based Formulations for Mucosal Drug Delivery: A Review

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