Preparation and Evaluation of Plumbagin Nanoparticles Based on Nanostructured Lipid Carriers

OBJECTIVE To prepare nanostructured lipid carriers(NLCs) of plumbagin(PLB) modified with mannose(Man), investigate the in vitro drug release pattern, and conduct in vitro cytotoxicity experiments and preliminary pharmacological studies.

METHODS PLB-NLCs were prepared using the ethanol injection method, and then PLB-Man-NLCs were obtained by combining single-factor screening with Box-Behnken design-response surface methodology. The in vitro release pattern of PLB-Man-NLCs was evaluated using dialysis method and fitted with the optimal equation. NIH3T3 cells were used forotoxicity and cell proliferation inhibition experiments.

RESULTS The optimal formulation of PLB-Man-NLCs was as follows: drug-to-lip ratio of 1∶10, liquid-to-solid lipid ratio of 1∶3.85, and PLB concentration of 0.49 mg·mL⁻¹. PLB-Man-NLCs spherical or quasi-spherical shape with a particle size of (175.66±3.29)nm a Zeta potential of (−42.81±2.44)mV. The encapsulation efficiency and drug loading were (85.89±0.75)% and (5.69±0.07)%, respectively. The release curve of PLB-Man-NLCs was best fitted the Weibull equation. PLB-Man-NLCs reduced the toxicity of PLB to NIH3T3 cells and inhibited TGF-β1 induced fibroblast proliferation.

CONCLUSION PLB-Man-NLCs are successfully prepared, which the solubility and in vitro release of PLB. The experimental results provide a solid theoretical basis for further formulation development.