Departamento de Farmacia Galénica y Tecnología Alimentaria, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain.
Departamento de Farmacia Galénica y Tecnología Alimentaria, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain; Instituto Universitario de Farmacia Industrial, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain.
Eur J Pharm Sci. 2024 Dec 1;203:106919. doi: 10.1016/j.ejps.2024.106919. Epub 2024 Sep 30.
Genital herpes, caused by herpes simplex virus type 2 (HSV-2), affects nearly 500 million people, mostly women. Since the main route of transmission is sexual contact, the development of an acyclovir extended-release vaginal microbicide would be a suitable tool for the prevention of virus transmission. In this work, we evaluated the potential of three polymers with different characteristics (chitosan, xanthan gum and ethyl cellulose) for obtaining acyclovir extended-release vaginal tablets. By combining the polymers, certain useful synergies were observed to modify their mucoadhesive capacity and control drug release. In the swelling studies, it observed that a polyelectrolyte complex with more moderate swelling and sustained gelation was formed between chitosan and xanthan gum exclusively in acidic medium (simulated vaginal fluid). This complex allowed prolonging the mucoadhesion of the tablets in ex vivo studies performed with vaginal mucosa, which would translate into better retention in the vagina after administration. In addition, the combination of chitosan and xanthan gum allowed obtaining a controlled release of acyclovir for 5 days, regardless of the pH of the medium, which would guarantee that drug release continues even in the presence of seminal fluid.
生殖器疱疹是由单纯疱疹病毒 2 型（HSV-2）引起的，影响近 5 亿人，其中大多数是女性。由于主要传播途径是性接触，因此开发一种阿昔洛韦延长释放阴道杀微生物剂将是预防病毒传播的合适工具。在这项工作中，我们评估了三种具有不同特性的聚合物（壳聚糖、黄原胶和乙基纤维素）在获得阿昔洛韦延长释放阴道片方面的潜力。通过将聚合物结合在一起，观察到某些有用的协同作用，以改变它们的粘膜粘附能力并控制药物释放。在溶胀研究中，观察到壳聚糖和黄原胶之间仅在酸性介质（模拟阴道液）中形成具有中等溶胀和持续凝胶化的聚电解质复合物。该复合物允许延长在阴道粘膜上进行的离体研究中片剂的粘膜粘附，这将转化为给药后在阴道中的更好保留。此外，壳聚糖和黄原胶的组合允许获得阿昔洛韦的 5 天控释，而与介质的 pH 值无关，这将保证即使在存在精液的情况下药物释放也能持续。
