Formulation development and evaluation of innovative two-polymer (SR-2P) bioadhesive vaginal gel
Autor: | Gita N. Shankar, Carsten Alt, Satheesh Podaralla |
---|---|
Rok vydání: | 2013 |
Předmět: |
Serial dilution
Anti-HIV Agents Polymers Swine Bioadhesive Chemistry Pharmaceutical Pharmaceutical Science Aquatic Science medicine.disease_cause Viscosity Mice Microbicide Drug Discovery Polymer chemistry medicine Animals Ecology Evolution Behavior and Systematics Chromatography Ecology Chemistry Vaginal microbicide Osmolar Concentration Temperature Adhesiveness General Medicine Poloxamer Hydrogen-Ion Concentration Dilution Vagina Vaginal Creams Foams and Jellies Swine Miniature Female Irritation Agronomy and Crop Science Gels Research Article |
Zdroj: | AAPS PharmSciTech. 15(4) |
ISSN: | 1530-9932 |
Popis: | The main objective of this investigation was to study the feasibility of developing a vaginal bioadhesive microbicide using a SRI’s proprietary two-polymer gel platform (SR-2P). Several formulations were prepared with different combinations of temperature-sensitive polymer (Pluronic® F-127) and mucoadhesive polymer (Noveon® AA-1), producing gels of different characteristics. Prototype polymeric gels were evaluated for pH, osmolality, buffering capacity, and viscosity under simulated vaginal semen dilutions, and bioadhesivity using ex vivo mini pig vaginal tissues and texture analyzer. The pH of the polymeric gel formulations ranged from 5.1 to 6.4; the osmolality varied from 13 to 173 mOsm. Absolute viscosity ranged from 513 to 3,780 cPs, and was significantly reduced (1.5- to 3-fold) upon incubation with simulated vaginal and semen fluid mixture. Among the tested gels (indicated in the middle row as a molar ratio of a mixture of Noveon vs. Pluronic), only SR-2P retained gel structure upon dilution with simulated fluids and mild simulated coital stress. The pH of the SR-2P gel was maintained at about 4.6 in simulated vaginal fluid and also showed high peak force of adhesion in mini pig vaginal tissue. Furthermore, SR-2P gel caused no or only minimal irritation in a mouse vaginal irritation model. The results of this preliminary study demonstrated the potential application of SR-2P gel as a vaginal microbicide vehicle for delivery of anti-HIV agents. |
Databáze: | OpenAIRE |
Externí odkaz: |