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Berberine hydrochloride (BH) is an effective isoquinolin alkaloid drug for treating cancer.While the poor aqueous solubility, gastro-intestinal absorption, and rapid metabolism of BH are the main limited factors for human absorption.A solid lipid nanoparticle (SLN) formulation, incorporating BH, was prepared from a lipid mixture of Precirol ATO5 and Gelucire 50/13 and emulsifiers of Tween 80 and Poloxamer 188, in order to establish a stable drug cartier for persistent and effective absorption.The physicochemical properties of BH-loaded SLNs with lipid mixtures and surfactant compositions were investigated, and the mean particle size was 32 ± 3nm, and zeta potential was at the range of-14 to-18 mV.Meanwhile, drug entrapment efficiency, relative long-term physical stability, and release profiles of BH from SLNs were evaluated.In order to confirm whether it could help BH function well on its anti-tumor activities on MCF-7 breast cancer cells, cell viability assay, cell cycle analysis, and cell apoptosis were investigated.The results in vitro indicated that the inhibition of cell proliferation, cell cycle arrest and cell apoptosis effects were increased in BH-loaded SLNs comparing with free BH.Our study presented that the described SLNs formulation may be a potential delivery system for BH to improve its antitumor activity effect on MCF-7 breast cancer cells.