Ghosal Kajal, Hazra Bipad Taran, Bhowmik Benoy Brata, Thomas Sabu
Flat No: 26, 10 Vychodilova, Zaboversky 2551, Brno 61600, Czech Republic.
Curr HIV Res. 2016;14(4):295-306. doi: 10.2174/1570162x14666151113123040.
The purpose of this study was formulation and optimization of vaginal film formulation containing abacavir (ABC), a potent nucleoside reverse transcriptase inhibitor.
Vaginal films were prepared by solvent evaporation method using hydroxypropyl methylcellulose (HPMC) blended with polyvinyl pyrrolidone (PVP). Various physicochemical parameters of the prepared films such as drug content, thickness, tensile strength, percentage elongation at break, drug polymer interaction, swelling capacity, folding endurance, bio-adhesion, pH, and moisture content were evaluated with morphological studies. In vitro release study and in vivo release study were also performed.
Films exhibited favorable physicochemical properties. The in vitro study showed that HPMC-PVP combination can control the release of abacavir through vaginal films with higher amount of PVP in the formulation resulting in an enhanced drug release rate. During the in vivo study in rabbits, systemic absorption of the drug was noted and the films remained intact for long in vagina without causing any sort of irritations.
Thus, in a nutshell, the findings of our experimental work indicate that such films can be considered as a novel drug carrier system for the treatment of AIDS and other sexually transmitted diseases (STDs), and are suitable for local as well as systemic effects.
本研究旨在制备并优化含阿巴卡韦（ABC）的阴道膜制剂，阿巴卡韦是一种有效的核苷类逆转录酶抑制剂。
采用溶剂蒸发法，以羟丙基甲基纤维素（HPMC）与聚乙烯吡咯烷酮（PVP）混合制备阴道膜。通过形态学研究评估所制备膜的各种物理化学参数，如药物含量、厚度、拉伸强度、断裂伸长率、药物与聚合物相互作用、溶胀能力、耐折度、生物黏附性、pH值和水分含量。还进行了体外释放研究和体内释放研究。
膜表现出良好的物理化学性质。体外研究表明，HPMC - PVP组合可控制阿巴卡韦通过阴道膜的释放，制剂中PVP含量较高时药物释放速率增强。在兔体内研究期间，观察到药物的全身吸收，且膜在阴道内长时间保持完整，未引起任何刺激。
简而言之，我们实验工作的结果表明，此类膜可被视为治疗艾滋病和其他性传播疾病（STD）的新型药物载体系统，适用于局部和全身作用。
