Pharmacology Efficacy in vitro of PTX-PLGA Microspheres and Surface Modified PTX-PLGA Microspheres by Quaternized Chitosan
壳聚糖季铵盐表面修饰对载紫杉醇PLGA微球体外药效学的影响

Poly(dl-lactic-co-glycolic acid)(PLGA) microspheres containing PTX and surface modified PTX-PLGA microspheres with HTCC were prepared by premix membrane emulsification combined with solvent evaporation.Then the corresponding effects on surface morphology,loading and encapsulation efficiencies,release profile and antitumor activity in vitro were systematically investigated.The results showed that the mean diameter of PTX-loaded HTCC-PLGA microspheres was 882 nm,the loading and encapsulation efficiencies were 5.15% and 70.46%,and the cumulative release rate in vitro for 22 d was 70.17%,which had little difference from PTX-loaded PLGA microspheres.However,PTX-loaded HTCC-PLGA microspheres showed positive surface charge as +36.7 mV and PLGA was -14.8 mV.The intracellular PTX incubated with PTX-loaded PLGA and PLGA-HTCC microspheres was 5.6 and 9.7 times as much as that of Taxol,and HTCC-PLGA microspheres showed lower cell viability than PLGA microspheres.Therefore,PTX-loaded HTCC-PLGA microspheres were the potential delivery system for insoluble drug PTX.