Department of Material Science and Engineering, Engineering Research Center of Artificial Organs and Materials, Jinan University, Guangzhou, 510632, China.
Department of Material Science and Engineering, Engineering Research Center of Artificial Organs and Materials, Jinan University, Guangzhou, 510632, China.
Mater Sci Eng C Mater Biol Appl. 2017 Nov 1;80:156-164. doi: 10.1016/j.msec.2017.05.136. Epub 2017 May 24.
Liposome is one of a promising delivery system to improve water solubility, stability, and bioavailability of curcumin. But its instability is not favorable for long-circulating treatment, controlled release or conservation. To overcome the disadvantages, thiol derivatised chitosan (CSSH) were synthesized and utilized to coat liposomes. The CSSH coated curcumin liposomes (Cur-Lip-CSSH) had an encapsulation efficiency (EE) of 93.95%, a drug loading (DL) of 7.95%, an average particle size of 406.0nm, and a positive zeta-potential of 36.6mV, which were all higher than that of Cur-Lip. Cur-Lip-CSSH showed slower in vitro release than Cur-Lip at pH5.5 and pH7.4, and the higher retention of curcumin would be remained for the following uptake of cells. The stability of the both liposomes at 4°C was almost the same, but Cur-Lip-CSSH displayed a higher stability at room temperature and higher temperature by DSC characterization. Curcumin can inhibit the growth of cancer cells under certain conditions. MCF-7 cell line was used to study its inhibition and proliferation after treating with curcumin and Cur-Lip-CSSH. Treatment of MCF-7 with curcumin and Cur-Lip-CSSH showed dose and time dependent cytotoxicity, with growth suppression at 200μM, 72h, obviously. These results indicate that the proper coating of liposomes is able to improve the stability of liposomes and the Lip-CSSH can function as potential drug delivery system.
脂质体是一种很有前途的给药系统,可以提高姜黄素的水溶性、稳定性和生物利用度。但其不稳定性不利于长期循环治疗、控制释放或保存。为了克服这些缺点,合成了巯基化壳聚糖(CSSH)并用于包裹脂质体。CSSH 包裹的姜黄素脂质体(Cur-Lip-CSSH)的包封效率(EE)为 93.95%,载药量(DL)为 7.95%,平均粒径为 406.0nm,正zeta 电位为 36.6mV,均高于 Cur-Lip。Cur-Lip-CSSH 在 pH5.5 和 pH7.4 时的体外释放速度比 Cur-Lip 慢,并且在随后的细胞摄取中,会保持更高的姜黄素保留率。两种脂质体在 4°C 时的稳定性几乎相同,但 Cur-Lip-CSSH 在室温下和较高温度下通过 DSC 特性显示出更高的稳定性。在一定条件下,姜黄素可以抑制癌细胞的生长。MCF-7 细胞系被用于研究姜黄素和 Cur-Lip-CSSH 处理后对其抑制和增殖的影响。用姜黄素和 Cur-Lip-CSSH 处理 MCF-7 细胞表现出剂量和时间依赖性细胞毒性,在 200μM,72h 时明显抑制生长。这些结果表明,适当的脂质体包裹可以提高脂质体的稳定性,Lip-CSSH 可以作为潜在的药物传递系统。