ABSTRACT
Objective: The study aims at preparing the didodecyldimethylammonium bromide (DMAB)-modified PLGA nanoparticles (NPs) loading tetrandrine (Tet) (DMAB-Tet-PLGA-NPs) and investigating the preparation process, physicochemical characterization, in vitro cytotoxicity, and particle cellular uptake. Methods: DMAB-Tet-PLGA-NPs were prepared by the emulsion solvent diffusion method and the preparation process was optimized with the uniform design experiment. The drug loading, entrapment efficiency (EE), and in vitro drug release were studied to evaluate the drug-loading property. The in vitro cytotoxicity against human lung cancer cell A549 was measured by the standard MTT assay. The particles cellular uptake in A549 was evaluated by qualitative and quantitative methods. Results: DMAB-Tet-PLGA-NPs in the mean size of (205.40±2.66) nm with spherical shape and showed positive surface charge. Drug loading and EE were (2.130±0.035)% and (50.780±3.253)%, respectively. DMAB-Tet-PLGA-NPs could retard drug release in pH 7.4 release media and the cumulative release was up to 64.56% over 48 h. And DMAB-Tet-PLGA-NPs showed the significant dose-and time-dependent cytotoxicity of Tet in vitro and well cellular uptake by A549. Conclusion: DMAB-Tet-PLGA-NPs shows the good EE, uniform particle size, and could retard drug release in vitro. And DMAB-Tet-PLGA-NPs shows the significant cytotoxicity in vitro and well cellular uptake by A549.