a Faculty of Pharmacy, Department of Pharmaceutical Technology , Hacettepe University , Ankara , Turkey.
Pharm Dev Technol. 2018 Mar;23(3):301-310. doi: 10.1080/10837450.2017.1329835. Epub 2017 May 29.
Infection with the human immunodeficiency virus (HIV) is affecting women disproportionally with increasing incidence rates over the last decades. Tenofovir is one of the most commonly used antiretroviral agents, which belongs to the nucleoside/nucleotide reverse transcriptase inhibitor family, for the prevention of HIV acquisition. In scope of this study, a thermogelling system containing tenofovir-loaded chitosan nanoparticles for the controlled release of tenofovir was developed and characterized. The in vitro release studies have shown that the burst release effect was decreased to 27% with f-TFV CS NPs-Gel. Gelation temperature of developed formulation was found as 26.6 ± 0.2 °C, which provides ease of administration while gelation occurs after the administration to the vagina. The work of adhesion values was used as parameters for comparison of mucoadhesive performance and the mucoadhesion of f-TFV CS NPs-Gel was found as 0.516 ± 0.136 N.s at 37 °C. The biocompatibility of blank formulations was evaluated by cell viability studies using L929 cells, in which Gel + CS NPs formulation was found to be safe with 82.4% and 90.2% cell viability for 1:16 and 1:32 dilutions, respectively. In conclusion, an improved tenofovir containing vaginal gel formulation was successfully developed and evaluated for preventing HIV transmission.
人类免疫缺陷病毒 (HIV) 的感染对女性的影响不成比例，在过去几十年中发病率不断上升。替诺福韦是最常用的抗逆转录病毒药物之一，属于核苷/核苷酸逆转录酶抑制剂家族，用于预防 HIV 感染。在本研究范围内，开发并表征了一种含有替诺福韦负载壳聚糖纳米颗粒的温敏凝胶系统，用于替诺福韦的控制释放。体外释放研究表明，f-TFV CS NPs-Gel 的突释效应降低至 27%。开发制剂的胶凝温度为 26.6±0.2°C，在给药后凝胶化，便于给药。工作粘附值被用作比较粘膜粘附性能的参数，并且 f-TFV CS NPs-Gel 的粘膜粘附性在 37°C 时为 0.516±0.136 N.s。通过使用 L929 细胞进行细胞活力研究评估空白配方的生物相容性，其中 Gel+CS NPs 配方在 1:16 和 1:32 稀释度下的细胞活力分别为 82.4%和 90.2%，被认为是安全的。总之，成功开发并评估了一种改良的含有替诺福韦的阴道凝胶制剂，用于预防 HIV 传播。
