School of Life Science, Jiangxi Science and Technology Normal University, Nanchang, Jiangxi, People's Republic of China.
Curr Drug Deliv. 2024;21(4):592-602. doi: 10.2174/1567201820666230619112502.
Using targeted liposomes to encapsulate and deliver drugs has become a hotspot in biomedical research. Folated Pluronic F87/D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) co-modified liposomes (FA-F87/TPGS-Lps) were fabricated for curcumin delivery, and intracellular targeting of liposomal curcumin was investigated.
FA-F87 was synthesized and its structural characterization was conducted through dehydration condensation. Then, cur-FA-F87/TPGS-Lps were prepared via thin film dispersion method combined with DHPM technique, and their physicochemical properties and cytotoxicity were determined. Finally, the intracellular distribution of cur-FA-F87/TPGS-Lps was investigated using MCF-7 cells.
Incorporation of TPGS in liposomes reduced their particle size, but increased the negative charge of the liposomes as well as their storage stability, and the encapsulation efficiency of curcumin was improved. While, modification of liposomes with FA increased their particle size, and had no impact on the encapsulation efficiency of curcumin in liposomes. Among all the liposomes (cur-F87-Lps, cur-FA-F87-Lps, cur-FA-F87/TPGS-Lps and cur-F87/TPGS-Lps), cur-FA-F87/TPGS-Lps showed highest cytotoxicity to MCF-7 cells. Moreover, cur-FA-F87/TPGS-Lps was found to deliver curcumin into the cytoplasm of MCF-7 cells.
Folate-Pluronic F87/TPGS co-modified liposomes provide a novel strategy for drug loading and targeted delivery.
利用靶向脂质体包封和递送药物已成为生物医学研究的热点。叶酸聚氧乙烯醚 F87/维生素 E 聚乙二醇 1000 琥珀酸酯（TPGS）共修饰脂质体（FA-F87/TPGS-Lps）被用于递送姜黄素，并研究了脂质体姜黄素的细胞内靶向作用。
合成 FA-F87 并通过脱水缩合进行结构表征。然后，通过薄膜分散法结合 DHPM 技术制备 cur-FA-F87/TPGS-Lps，并测定其理化性质和细胞毒性。最后，使用 MCF-7 细胞研究 cur-FA-F87/TPGS-Lps 的细胞内分布。
TPGS 的掺入降低了脂质体的粒径，但增加了脂质体的负电荷和储存稳定性，并提高了姜黄素的包封效率。而 FA 修饰脂质体增加了其粒径，但对脂质体中姜黄素的包封效率没有影响。在所有脂质体（cur-F87-Lps、cur-FA-F87-Lps、cur-FA-F87/TPGS-Lps 和 cur-F87/TPGS-Lps）中，cur-FA-F87/TPGS-Lps 对 MCF-7 细胞的细胞毒性最高。此外，cur-FA-F87/TPGS-Lps 被发现将姜黄素递送到 MCF-7 细胞的细胞质中。
叶酸-聚氧乙烯醚 F87/TPGS 共修饰脂质体为载药和靶向递药提供了一种新策略。
