载多西紫杉醇的F3多肽靶向单分子胶束的制备和体外评价

目的:制备载多西紫杉醇的F3多肽靶向单分子胶束(DTX/PAMAM-PLA-PEG-F3),并对其进行体外评价.方法:所制备的单分子胶束采用动态光散射仪和透射电镜测定其粒径分布和形态;采用高效液相色谱法测定单分子胶束的载药量和评估其体外释药特性;采用MTT法考察单分子胶束的抗肿瘤活性;采用流式细胞仪和共聚焦显微镜探究细...

Preparation of docetaxel-loaded and F3 peptide-targeted unimolecular micelles and in vitro evaluation

OBJECTIVE To prepare DTX-loaded F3 peptide-targeted unimolecular micelles (DTX/PAMAM-PLA-PEG-F3) and evaluate its in vitro profiles.METHODS The particle size distribution and morphology of the prepared unimolecular micelles were measured by dynamic light scattering and transmission electron microscopy; The drug loading contents and in vitro drug release profiles were determined by high performance liquid chromatography (HPLC); The anti-tumor activity was examined by methyl thiazolyl tetrazolium (MTT); Flow cytometry and confocal microscope were utilized for exploring the mechanism of cellular uptake.RESULTS The prepared unimolecular micelles were spherical with an average particle size of (32.0±5.8) nm, the drug loading contents of it was (12.4±1.3) wt.%. In vitro drug release studies showed that the unimolecular micelles were pH-responsive. Compared with non-targeted micelles group, targeted micelles group demonstrated had higher cytotoxicity and cell uptake efficiency to breast cancer MDA-MB-231 cells. The targeting ligand F3 peptide could mediate a specific uptake of targeted unimolecular micelles by tumor cells.CONCLUSION DTX/PAMAM-PLA-PEG-F3, as a drug delivery system, has broad application prospects in improving anti-tumor efficacy.