Nanomedicine and Biosensor Laboratory, School of Life Science and Engineering, Harbin Institute of Technology, Harbin 150080, People's Republic of China.
Colloids Surf B Biointerfaces. 2012 Oct 1;98:97-104. doi: 10.1016/j.colsurfb.2012.05.001. Epub 2012 May 8.
Efforts to improve the stability of liposomes have recently led to the development of organic-inorganic liposomal cerasomes. In this study, we explore the potential to modulate the sustained release of paclitaxel from cerasomes by alteration in vesicle composition. Specifically, composite cerasomes have been prepared from mixtures of cerasome-forming lipid (lipid 1) and 1,2-distearoyl-sn-glycero-3-phosphocholine (lipid 2) via one-step construction. The influences of vesicle composition on the physical properties (e.g., particle diameter and surface charge density), physiochemical and long-term storage stability, drug-loading capacity, and release rates of paclitaxel have been investigated. Notably, a wide range of the release profiles of paclitaxel have been achieved by varying the contents of lipid 2, and the composite vesicles display excellent stability when the percentage content of lipid 2 is lower than 50%. Composite vesicles composed of lipids 1 and 2 at a 1:1 molar ratio also exhibited good cytocompatibility and the released paclitaxel effectively inhibit the proliferation of HeLa cancer cells. Together, the development of composite vesicles offers a promising strategy to obtain excellent stability, good drug-loading capacity and cytocompatibility, and enhanced paclitaxel release in single vesicles.
最近，人们努力提高脂质体的稳定性，从而开发出了有机-无机脂质体复合囊泡。在本研究中，我们通过改变囊泡组成来探索调节紫杉醇从复合囊泡中持续释放的潜力。具体而言，通过一步构建法，由复合囊泡形成脂质（脂质 1）和 1,2-二硬脂酰-sn-甘油-3-磷酸胆碱（脂质 2）的混合物制备了复合囊泡。考察了囊泡组成对物理性质（例如粒径和表面电荷密度）、物理化学和长期储存稳定性、载药能力以及紫杉醇释放率的影响。值得注意的是，通过改变脂质 2 的含量可以实现广泛的紫杉醇释放曲线，并且当脂质 2 的百分比含量低于 50%时，复合囊泡显示出优异的稳定性。由摩尔比为 1:1 的脂质 1 和 2 组成的复合囊泡也表现出良好的细胞相容性，并且释放的紫杉醇有效抑制了 HeLa 癌细胞的增殖。总之，复合囊泡的开发为获得单囊泡中优异的稳定性、良好的载药能力和细胞相容性以及增强紫杉醇释放提供了一种有前途的策略。
