Pharmaceutical Technology Division, Department of Chemical Technology, Dr. Babasaheb Ambedkar, Marathwada University, Aurangabad, India.
Drug Dev Ind Pharm. 2020 May;46(5):732-743. doi: 10.1080/03639045.2020.1752709. Epub 2020 May 6.
The aim of this study is to develop Darunavir (DRV) proliposome powder for oral delivery. Darunavir-loaded oral proliposome powder (OPP) was prepared by a solvent evaporation technique with varying independent variables at three different levels. Based on different levels, proliposome powder formulation was optimized by using Box-Behnken design. The formulations were analyzed for its size distribution, entrapment efficiency, and surface morphology. Optimized proliposome batch A was evaluated for physical parameter, morphological parameters, entrapment efficiency, followed by , , and studies. Oral proliposome powder showed good micromeritic properties with angle of repose was less than 30°, Carr's index and Hausner's ratio were also less than 21 and 1.25, respectively. The mean size of the vesicles was in the range of 180-290 nm. The assay and entrapment efficiency of pro-liposome powder formulations were 79.00 ± 0.2 and 93.46 ± 0.2%, respectively. release of DRV proliposome powder was 78.17 ± 0.1% after 24 h which shows good release from the vesicle of proliposome permeation study shows 58.11% enhancement which shows good permeation. The optimize batch A of proliposome powder indicated 50% enhancement in the relative bioavailability as compared to the DRV suspension. The results showed that proliposome powder containing DRV can efficiently deliver in to the blood stream. This drug delivery system has been designed as a novel platform for potential oral delivery of drugs having poor water solubility and high first-pass metabolism.
本研究旨在开发达芦那韦（DRV）前体脂质体粉末用于口服给药。采用溶剂蒸发技术，以三个不同水平的三个独立变量制备载达芦那韦的口服前体脂质体粉末（OPP）。根据不同的水平，采用 Box-Behnken 设计优化前体脂质体粉末配方。对制剂进行粒径分布、包封效率和表面形态分析。对优化的前体脂质体批 A 进行物理参数、形态参数、包封效率评估，随后进行、、和研究。口服前体脂质体粉末具有良好的微粉学性质，休止角小于 30°，Carr 指数和 Hausner 比也小于 21 和 1.25。囊泡的平均粒径在 180-290nm 范围内。前体脂质体粉末制剂的含量和包封效率分别为 79.00±0.2%和 93.46±0.2%。DRV 前体脂质体粉末的释放 24 小时后达到 78.17±0.1%，表明从前体脂质体的囊泡中释放良好。渗透研究显示 58.11%的渗透增强，表明具有良好的渗透性能。与 DRV 混悬剂相比，前体脂质体粉末的优化批 A 表明相对生物利用度提高了 50%。结果表明，载有 DRV 的前体脂质体粉末可以有效地递送到血液中。该给药系统已设计为具有较差水溶性和高首过代谢的药物的潜在口服递药的新型平台。
