The study was aimed at formulating self-assembled capsaicin prodrug nanoparticles (Cap-SSVE NPs) with improved bioavailability, increased antihyperlipidemic activity and less gastrointestinal mucosa irritations. The in vitro release profile of the developed Cap-SSVE NPs was stable in HCl solution (pH 1.2) and distilled water, but very susceptible in PBS (pH 6.8 and 7.4). The relative oral bioavailability of Cap-SSVE NPs was 3.2 folds higher than free capsaicin, with an extended T_max (0.25–1 h). The Cap-SSVE NPs decreased certain lipid profile indices of both the liver tissue (Total lipids and TG) and the blood sample (TC, TG, LDL and TBA) with elevated levels of HDL in high fat diet induced hyperlipidemic rats. The nanoparticles also predominantly accumulated in the liver with reduced irritations in the gastrointestinal mucosa. Collectively, the formulated Cap-SSVE NPs showed an enhanced bioavailability, increased hypolipidemic effects and reduced mucosa irritations.

这项研究旨在配制生物利用度提高，降血脂活性增加和胃肠道粘膜刺激性降低的自组装辣椒素前药纳米颗粒（Cap-SSVE NPs）。在体外发达的Cap-SSVE NP的释放曲线是在HCl溶液中稳定（pH为1.2）和蒸馏水，但在PBS（pH为6.8和7.4）非常敏感。Cap-SSVE NPs的相对口服生物利用度比游离辣椒素高3.2倍，T _max延长（0.25–1小时）。在高脂饮食诱发的高脂血症大鼠中，Cap-SSVE NPs降低了肝脏组织（总脂质和TG）和血液样品（TC，TG，LDL和TBA）的某些脂质谱指数，HDL水平升高。纳米颗粒也主要在肝脏中积累，对胃肠道粘膜的刺激​​性降低。总的来说，配制的Cap-SSVE NPs具有更高的生物利用度，更高的降血脂作用和减少的粘膜刺激性。