| Objective:To study the effective inhibitory effect of enantiomeric copolymers-based doxorubicin(DOX) loaded stereocomplexmicelleon the growth of renal carcinoma cellsand its cellular mechanism. Methods:Fabricate three kinds of DOX loaded copolymermicelles(PDM/DOX, PLM/DOX and SCM/DOX). Characterizations in vitro(mensurate the sizes, stability and the DOX release in vitro). Characterizations in vivo(the intracellular DOX release, cytotoxicity, stability in the blood circulation and blood compatibility). Result:The hydrodynamic diameters(Dhs) of PDM/DOX, PLM/DOX and SCM/DOX were 115, 105 and 90 nm, respectively, which were proper for them to aggregate effectively in the tumor site through the enhanced permeabilityand retention(EPR) effect. All these three drug loaded micelles could keep stable sizes in the normal environment. The drug release resultsin vitro demonstrated that the SCM/DOX could release the DOX much slower than PDM/DOX and PLM/DOX. With the extension of time, the SCM/DOX exhibited more effective DOX accumulation in the renal carcinoma cells. The cytotoxicity assay(MTT) also demonstrated that SCM/DOX could kill renal carcinoma cells more effectively than PDM/DOX, PLM/DOX and free DOX. Furthermore, SCM/DOX exhibited satisfactoryblood compatibility, whichindicating the great potential for the intravenous medication. All the results indicated the great potential of SCM/DOX for chemotherapy in advanced renal cell carcinoma in the future. Conclusion:1. Compared to PDM/DOX and PLM/DOX, SCM/DOX exhibited smaller diameter and much more satisfactory DOX release results.2. SCM/DOX could better realize the DOX release and accumulation in renal carcinoma cells, which caused much more effective antitumor efficiency.3. SCM/DOX exhibited satisfactory blood compatibility, which provided the basis for its future application. |
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