蟾毒灵纳米结构脂质载体的制备及性质研究

本文采用高压均质法成功将脂溶性药物蟾毒灵(BUF)负载于纳米结构脂质载体(NLC)中,并对其物理化学性质、体外释放性质及体外肿瘤细胞毒性等进行了研究。结果表明,制备获得的蟾毒灵纳米结构脂质载体(BUF-NLC)粒径小、分散度和稳定性好,具有明显的药物缓释作用。MTT实验表明,将BUF负载于NLC后,作用初期对肿瘤细胞的毒性作用低于原药,作用时间延长,毒性与原药达到一致,说明NLC的包裹并未降低蟾毒灵的药效,而是逐步释放出来,这对克服临床应用中蟾毒灵的高毒副作用有非常重要的意义。

Preparation and characterization of bufalin nanostructure lipid carriers

In this paper, Bufalin loaded nanostructure lipid carriers (BUF-NLC) was successfully prepared by high pressure homogenization. The physicochemical properties, in vitro release and cytotoxicity (MTT) were thoroughly characterized. The results indicated that BUF-NLC exhibited stable system with small particle size and good dispersion. The MTT assay suggested that the cytotoxicity of BUF-NLC on tumor cells was lower than free BUF in the initial stage, but when prolonged the action time, the cytotoxicity of BUF-NLC was consistent with BUF. That showed NLC package did not reduce the cytotoxicity of BUF, but gradually released, which was very important to overcome the side-effects caused by the high toxicity of BUF.