用于治疗 HIV-1 的富马酸替诺福韦二吡呋酯负载纳米粒子的合成与表征

Nano Select Pub Date : 2024-02-13 DOI:10.1002/nano.202300157
O. Obisesan, L. Tshweu, Sipho Chauke, K. Malatji, B. Ramalapa, K. Alexandre, H. Mufhandu
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引用次数: 0

摘要

人类免疫缺陷病毒(HIV)具有逃避宿主免疫系统和传统抗逆转录病毒疗法的超强能力,这给实现彻底根除 HIV 感染者(PLWHIV)体内的病毒带来了巨大挑战。然而,纳米技术已经成为解决与使用抗逆转录病毒药物相关的一些障碍的大有可为的途径,其方法是在纳米尺度上对药物分子进行修饰。因此,本研究探讨了利用聚(epsilon-caprolactone)(PCL)作为载体封装富马酸替诺福韦二吡呋酯(TDF),为艾滋病毒感染提供一种替代治疗方法。利用双乳液溶剂蒸发技术成功制备了负载 TDF 的聚合物纳米粒子,并对其进行了表征。对不同药物与聚合物比例的 TDF 负载聚合物纳米粒子的表征表明,TDF 在 PCL 中的包封效率和药物负载能力分别为 23%-46% 和 4.8%-19.9%。值得注意的是,与游离的 TDF 相比,负载 TDF 的聚合物纳米粒子的中和效果更好。用 PCL 包封 TDF 并没有阻碍 TDF 对 HIV-1 感染的抗病毒活性,反而增强了其效力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis and characterization of tenofovir disoproxil fumarate loaded nanoparticles for HIV‐1 treatment
The remarkable ability of the human immunodeficiency virus (HIV) to evade the host's immune system and conventional antiretroviral therapy, has posed significant challenges in achieving complete eradication of the virus in people living with HIV (PLWHIV). However, nanotechnology has emerged as promising avenue for addressing some of the obstacles associated with the use of antiretroviral drugs by modifying drug molecules in nanoscale dimensions. Hence, the present study explores the utilization of poly(epsilon‐caprolactone) (PCL) as a carrier for encapsulating tenofovir disoproxil fumarate (TDF), offering an alternative treatment approach for HIV infection. TDF‐loaded polymeric nanoparticles were successfully prepared using double emulsion solvent evaporation technique and characterized. The characterization of TDF‐loaded polymeric nanoparticles at varied drug to polymer ratios showed that TDF was loaded in PCL with an encapsulation efficiency and drug loading capacity in the range of 23–46% and 4.8–19.9%, respectively. Of note, the neutralization efficacy of TDF‐loaded polymeric nanoparticles was more improved compared to free TDF. Encapsulation of TDF with PCL did not hinder the antiviral activity of TDF against HIV‐1 infection but rather enhanced its potency.
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