Department of Pharmaceutics, School of Pharmaceutical Science, Shenyang Pharmaceutical University, Shenyang, PR China.
Drug Dev Ind Pharm. 2009 Aug;35(8):959-68. doi: 10.1080/03639040902718039.
The water-soluble peptide, melittin, was modified with an anionic agent, sodium dodecyl sulfate by hydrophobic ion-pairing. Investigations showed that the formed complex was very soluble in organic solvent, especially, in dimethylsulfoxide and dehydrated alcohol. Furthermore, the physiochemical properties of the complex in the solid state or in an aqueous medium were characterized using octanol/water partition measurement, Fourier transform infrared spectroscopy, and differential scanning calorimetry. The complex was formulated into poly(D,L-lactide-co-glycolide acid) nanoparticles by an emulsion solvent diffusion method. It was found that the nanoparticles of about 130 nm in size can be produced with a high encapsulation efficiency, and the entrapment of nanoparticles prepared with the formed complex increased from about 50% to nearly 100% compared with that for pure melittin. Moreover, the growth inhibitory effects of modified melittin and melittin-loaded nanoparticles in breast cancer MCF-7 cells were not changed comparing with free melittin as determined by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay.
水溶性肽蜂毒素通过疏水离子对与阴离子试剂十二烷基硫酸钠进行了修饰。研究表明，形成的复合物在有机溶剂中非常易溶，特别是在二甲基亚砜和脱水乙醇中。此外，通过辛醇/水分配测量、傅里叶变换红外光谱和差示扫描量热法对复合物在固态或水介质中的物理化学性质进行了表征。该复合物通过乳液溶剂扩散法被制成聚（D，L-乳酸-共-乙醇酸）纳米粒。结果发现，可制备出粒径约为 130nm 的纳米粒，且具有较高的包封效率，与纯蜂毒素相比，用形成的复合物制备的纳米粒的包封率从约 50%增加到近 100%。此外，通过（3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐）测定，与游离蜂毒素相比，乳腺癌 MCF-7 细胞中修饰的蜂毒素和载药纳米粒的生长抑制作用没有改变。
