Development of vaginal rings for sustained release of nonhormonal contraceptives and anti-HIV agents
Development of vaginal rings for sustained release of nonhormonal contraceptives and anti-HIV agents
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DOI：
10.1016/j.contraception.2007.04.006
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发表时间：
2007-08-01
期刊：
影响因子：
2.9
通讯作者：
Saxena, Brij B.
中科院分区：
文献类型：
--
作者：
Han, Young A.;Singh, Mukul;Saxena, Brij B.
目的：构建非激素性避孕药阴道环和抗HIV药物3-叠氮-3‘-脱氧胸腺嘧啶核苷(AZT)，并测定其每日释放量和体外药效。材料与方法：将直径5~5.5 cm、外缘0.5~0.7 cm的阴道环浇铸于模具内。环由可生物溶解的相思胶或不可生物降解的甲基丙烯酸羟乙酯(HEMA)和甲基丙烯酸钠(SMA)水凝胶[P(HEMAco-SMA)]组成。环内注入葡萄糖酸亚铁等非激素性避孕药，增加宫颈粘液黏度的L抗坏血酸，以及pH值为4~5或AZT的药效液。结果：非激素性避孕药和AZT在体外的日释放量均较高。非激素避孕药的累积效应在30 S内表现出完全的精子稳定作用，最长可达10天和28天。两种环每日释放的AZT也可能分别有效地抑制HIV的体外增殖10天和28天。结论：这两种环可用于非激素性避孕药和/或抗HIV药物的阴道给药。(C)2007 Elsevier Inc.保留所有权利。
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(HEMAco-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. (C) 2007 Elsevier Inc. All rights reserved.