Development and characterization of bioadhesive vaginal films of sodium polystyrene sulfonate (PSS), a novel contraceptive antimicrobial agent
Development and characterization of bioadhesive vaginal films of sodium polystyrene sulfonate (PSS), a novel contraceptive antimicrobial agent
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DOI：
10.1007/s11095-005-2490-1
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发表时间：
2005-04-01
影响因子：
3.7
通讯作者：
Zaneveld, LJD
中科院分区：
文献类型：
--
作者：
Garg, S;Vermani, K;Zaneveld, LJD
目的。聚苯乙烯磺酸盐(PSS)是一种新型的无细胞毒性的抗菌避孕药。在I期临床试验中，PSS凝胶制剂被发现可以安全地经阴道给药。本研究的目的是开发和评价PSS的新型生物粘附性阴道膜剂。采用溶剂挥发法制备了PSS薄膜，并对其各种物理、机械和美学性能进行了优化。此外，对薄膜的各种生物活性和安全性进行了评价。已经开发出每单位含有300毫克PSS的阴道膜，使用通常被认为是安全的(GRAS)列出的辅料。这些薄膜无色、透明、薄、软、韧，在生理液体中迅速溶解，形成光滑、粘稠的生物粘附液，可在阴道内保留较长时间。PSS膜对精子功能的抑制(透明质酸酶和宫颈粘液渗透)以及对人类免疫缺陷病毒(HIV)和单纯疱疹病毒(HSV)的抗菌活性与PSS相似。此外，薄膜不抑制正常的阴道微生物群(乳杆菌)，并且没有细胞毒性，这表明精子固定和对宿主细胞的细胞毒性可以忽略不计。速溶生物黏附阴道膜剂PSS具有理想的物理、机械、美学和生物学性能，是一种适合于防止性传播疾病(STDS)的候选阴道杀菌剂，并已准备好进行毒理学和临床评价。
Purpose. Polystyrene sulfonate (PSS) is a novel noncytotoxic antimicrobial contraceptive agent. A gel formulation of PSS was found safe for vaginal administration in phase I clinical trials. The purpose of the current study was to develop and evaluate novel bioadhesive vaginal film formulations of PSS.Methods. PSS films were prepared by solvent evaporation and optimized for various physical, mechanical, and aesthetic properties. Further, films were evaluated for various biological activities and safety.Results. Vaginal films containing 300 mg PSS per unit have been developed, using generally regarded as safe (GRAS) listed excipients. The films are colorless, transparent, thin, soft, and tough, dissolve rapidly in physiologic fluid to form a smooth, viscous and bioadhesive solution that could be retained in the vagina for prolonged intervals. Sperm function inhibition ( hyaluronidase and cervical mucus penetration) and antimicrobial activities against human immunodeficiency virus (HIV) and herpes simplex virus (HSV) by PSS films were found comparable to PSS. Also, films did not inhibit normal vaginal microflora ( Lactobacillus) and were noncytotoxic as indicated by negligible sperm immobilization and cytotoxicity to host cell assays.Conclusions. Rapidly dissolving bioadhesive vaginal film formulation of PSS with desired physical, mechanical, aesthetic, and biological properties is a suitable candidate vaginal microbicide for prevention of sexually transmitted disease (STDs) and is ready for toxicological and clinical evaluation.