title: Microparticulated anti-HIV vaginal gel: in vitro-in vivo drug release and vaginal irritation study.
abstract: The aim of this study was to develop and evaluate a Zidovudine (AZT)-loaded microparticulated bioadhesive vaginal gel (MBVG) in order to obtain a controlled releasing, safe gel delivery system. AZT microparticles (ZMPs) were evaluated for encapsulation efficiency, drug loading, surface morphology and in vitro drug release profiles and drug release mechanism and optimized. The optimized ZMPs were then encompassed in bioadhesive gel using different bioadhesive polymers and evaluated for the drug encapsulation efficiency, drug loading, in vitro and in vivo drug release profiles, drug release mechanism and vaginal irritancy study. From the dissolution data of ZMP4 and MBVG4 showed a zero-order diffusion pattern and Fickian diffusion case I transport mechanism in 24 and 36 h, respectively. On the basis of a pharmacokinetic study of MBVG4 (containing ZMP: Carbopol 1:4), it was found to have better bioavailability, larger AUC and T(max) in comparison to an oral pure suspension of AZT.
authors.affiliation: Department of Pharmaceutics, Himalayan Pharmacy Institute, Majhitar, Rangpo, Sikkim, India. arkendu2001@yahoo.co.in
authors.forename: Arkendu
authors.initials: A
authors.lastname: Chatterjee
authors.forename: Lalit
authors.initials: L
authors.lastname: Kumar
authors.forename: Benoy Brata
authors.initials: BB
authors.lastname: Bhowmik
authors.forename: Amlan
authors.initials: A
authors.lastname: Gupta
mesh_terms: D000282:Administration, Intravaginal; D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D002482:Cellulose / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry*; D004058:Diffusion; D005260:Female; D015658:HIV Infections / Q000517:prevention & control*; D006801:Humans; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D013997:Time Factors; D014622:Vaginal Creams, Foams, and Jellies / Q000008:administration & dosage / Q000737:chemistry*; D015215:Zidovudine / Q000097:blood / Q000493:pharmacokinetics
chemical_list: D003692:Delayed-Action Preparations; D014622:Vaginal Creams, Foams, and Jellies; D015215:Zidovudine; C013517:ethyl cellulose; D002482:Cellulose