Young A Han1, Mukul Singh, Brij B Saxena. 1. Division of Reproductive Endocrinology, Department of Obstetrics and Gynecology, Weill Medical College of Cornell University, 515 East 71st Street, S-412, New York, NY 10021, USA.
Abstract
OBJECTIVES: Construction of vaginal rings to deliver nonhormonal contraceptives and 3'-azido-3'-deoxythymidine (AZT) as an anti-HIV agent and determination of their daily release and efficacy in vitro. MATERIALS AND METHODS: Intravaginal rings of 0.5-0.7 cm rim and 5-5.5 cm in diameter were cast in the molds. The rings were composed of biosoluble acacia gum or nonbiodegradable hydrogel of 2-hydroxyethyl methacrylate (HEMA) and sodium methacrylate (SMA) [P(HEMA-co-SMA)]. The rings were impregnated with nonhormonal contraceptives such as ferrous gluconate to cause spermiostasis, l-ascorbic acid to increase the viscosity of the cervical mucus, and pharmalytes of pH 4-5 or AZT. RESULTS: The daily release rate of nonhormonal contraceptives as well as AZT from the rings was efficacious in vitro. Cumulative effect of nonhormonal contraceptives showed complete spermiostasis within 30 s up to 10 and 28 days, respectively. Daily release of AZT from both rings was also likely to be efficacious to inhibit HIV proliferation in vitro for 10 and 28 days, respectively. CONCLUSION: The data indicate that the rings described here can be developed for intravaginal delivery of nonhormonal contraceptives and/or anti-HIV agents.
OBJECTIVES: Construction of vaginal rings to deliver nonhormonal contraceptives and 3'-azido-3'-deoxythymidine (AZT) as an anti-HIV agent and determination of their daily release and efficacy in vitro. MATERIALS AND METHODS: Intravaginal rings of 0.5-0.7 cm rim and 5-5.5 cm in diameter were cast in the molds. The rings were composed of biosoluble acacia gum or nonbiodegradable hydrogel of 2-hydroxyethyl methacrylate (HEMA) and sodium methacrylate (SMA) [P(HEMA-co-SMA)]. The rings were impregnated with nonhormonal contraceptives such as ferrous gluconate to cause spermiostasis, l-ascorbic acid to increase the viscosity of the cervical mucus, and pharmalytes of pH 4-5 or AZT. RESULTS: The daily release rate of nonhormonal contraceptives as well as AZT from the rings was efficacious in vitro. Cumulative effect of nonhormonal contraceptives showed complete spermiostasis within 30 s up to 10 and 28 days, respectively. Daily release of AZT from both rings was also likely to be efficacious to inhibit HIV proliferation in vitro for 10 and 28 days, respectively. CONCLUSION: The data indicate that the rings described here can be developed for intravaginal delivery of nonhormonal contraceptives and/or anti-HIV agents.
Authors: Marc M Baum; Irina Butkyavichene; Joshua Gilman; Sean Kennedy; Etana Kopin; Amanda M Malone; Cali Nguyen; Thomas J Smith; David R Friend; Meredith R Clark; John A Moss Journal: J Pharm Sci Date: 2012-05-22 Impact factor: 3.534