The Preparation and Evaluation of Cepharanthine-Nanostructured Lipid Carriers In Vitro and In Vivo

This study was designed to prepare Cepharanthine-nanostructured lipid carriers (CEP-NLC) and investigate their structure, physical and chemical properties, in vitro release and in vivo pharmacokinetics. CEP-NLCs were prepared by the emulsification evaporation-low temperature solidification method. Particle size and encapsulation efficiency as CEP-NLCs evaluation indexes to optimize formulation through Box-Behnken. Optimal formulation: total lipid content 313.0 mg, Cepharanthine 4.4 mg and tween-80 3%. The CEP-NLC prepared according this formulation possessed a round appearance, were of uniform size, exhibited no adhesion, had an encapsulation efficiency of (98.19±0.48)%, and cold storage stability. Using 5% mannitol as a freeze-drying protective agent, the quality freeze-dried powder of CEP-NLC was excellent. CEP-NLC had a sustained-release effect, a good biocompatibility when the concentration of CEP was lower than 80 μg/ml. In vivo experiments showed that CEP-NLC increases the blood concentration and bioavailability of CEP and in mice altered the drug tissue distribution of CEP, showing preferential targeting to the lung. In summary, the optimization of formulation and preparation, successfully prepared excellent physicochemical properties and high bioavailability of CEP-NLC.