Preparation and in vitro evaluation of pH-sensitive charge-reversal nanoparticles loaded with curcumin / 中草药

ABSTRACT

Objective: To prepare charge-reversal pH-sensitive nanoparticles loaded with curcumin (PCE/Cur NPs), and investigate the optimizing technology, physicochemical characterizations, and inhibitory effect on B16 cell. Methods: The β-carboxyl amidized cationic MPEG-PCL-PEI polymers (PCE) were negatively charged, which were prepared into the negative PCE/Cur NPs with pH dependence. When pH > 7, there was no charge-reversal. When pH < 6, the β-carboxyl amides were hydrolyzed rapidly into corresponding amines. As a result, PCE/Cur NPs became positively charged again. The obtained PCE/Cur NPs were characterized by detection of particle size, morphology study, drug loading, encapsulation efficiency, and release study. The effect of anti-migratory and anti-invasive actions of PCE/Cur NPs on B16 cell was investigated using MTT assays and wound healing test. Results: PCE/Cur NPs dependent on pH charge inversion were successfully prepared. The obtained PCE/Cur NPs were round, and the size was uniform, the adhesion was not found. The Results: showed that the prepared PCE/Cur NPs had the highest DL (8.0 ± 1.0)%, EE (90.0 ± 2.0)%, mean particle size of (80 ± 5) nm, and zeta potential of (-35 ± 5) mV. Within 48 h, the accumulative release rate was (69.2 ± 5.2)% (pH 7.4) and (71.2 ± 4.3)% (pH 5), respectively, and then PCE/Cur NPs released slowly. These Results: by MTT assay and wound healing assay indicated that PCE/Cur NPs not only inhibited the proliferation of B16 cells in a concentration- and time-dependent manner, but also can induce apoptosis. Conclusion: PCE/Cur NPs were prepared successfully, which might have great potential application in drug delivery system.