Aim: This work aimed to encapsulate lamivudine in liposomes for targeted delivery to HIV reservoirs and thereby reduce its side effects.

Methods: The lamivudine liposomes were prepared by thin film hydration method using 3² factorial design and characterised for vesicle size, % drug entrapment efficiency, polydispersity index etc. Optimisation by graphical and numerical methods was carried out by fixing minimum and maximum limits for each response. In vivo plasma and tissue distribution of plain lamivudine and lamivudine encapsulated optimised liposomes were compared in rats.

Results: The optimised liposomes displayed vesicle size 276.20 ± 13.36 nm, percent entrapment 60.20 ± 2.86% and PDI 0.291 ± 0.053. Compared to plain lamivudine, the liposomes were rapidly cleared from the plasma and displayed 10.97 ± 0.72 and 1.38 ± 0.52 fold accumulation in liver and spleen tissues respectively.

Conclusions: Lamivudine encapsulated in liposomes remains in the body for a longer period of time with well distribution in tissues.

目的：这项工作旨在将拉米夫定包裹在脂质体中，以便有针对性地传递到艾滋病毒库中，从而减少其副作用。

方法：拉米夫定脂质体通过薄膜水化法，采用3 ²因子设计制备，并表征囊泡大小，药物包封率％，多分散指数等。通过确定每种反应的最小和最大极限值，通过图形和数值方法进行优化。 。在大鼠中比较了普通拉米夫定和拉米夫定封装的优化脂质体的体内血浆和组织分布。

结果：优化的脂质体的囊泡大小为276.20±13.36 nm，包封率为60.20±2.86％，PDI为0.291±0.053。与普通拉米夫定相比，脂质体可从血浆中快速清除，并在肝脏和脾脏组织中分别显示出10.97±0.72和1.38±0.52倍的积累。

结论：包裹在脂质体内的拉米夫定在人体中保留的时间较长，并且在组织中分布良好。