Han Young A, Singh Mukul, Saxena Brij B
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.
Contraception. 2007 Aug;76(2):132-8. doi: 10.1016/j.contraception.2007.04.006. Epub 2007 Jun 27.
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.
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.
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.
The data indicate that the rings described here can be developed for intravaginal delivery of nonhormonal contraceptives and/or anti-HIV agents.
构建用于递送非激素避孕药和作为抗HIV药物的3'-叠氮基-3'-脱氧胸苷（AZT）的阴道环，并测定其每日释放量及体外有效性。
在模具中浇铸边缘为0.5 - 0.7厘米、直径为5 - 5.5厘米的阴道环。这些环由生物可溶的阿拉伯胶或由甲基丙烯酸2-羟乙酯（HEMA）和甲基丙烯酸钠（SMA）[P（HEMA-co-SMA）]组成的不可生物降解水凝胶制成。环中浸渍有非激素避孕药，如葡萄糖酸亚铁以导致精子制动、L-抗坏血酸以增加宫颈黏液的黏度，以及pH值为4 - 5的两性电解质或AZT。
非激素避孕药以及AZT从环中的每日释放率在体外是有效的。非激素避孕药的累积效应分别在30秒内直至10天和28天显示出完全的精子制动。两种环中AZT的每日释放在体外分别抑制HIV增殖10天和28天也可能是有效的。
数据表明，此处所述的环可用于开发用于阴道递送非激素避孕药和/或抗HIV药物。
