Preparation and characterization of norcantharidin liposomes modified with stearyl glycyrrhetinate.
Preparation and characterization of norcantharidin liposomes modified with stearyl glycyrrhetinate.
复制标题
甘草次酸硬脂酯修饰去甲斑蝥素脂质体的制备及表征
DOI：
10.3892/etm.2018.6416
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发表时间：
2018-09
影响因子：
2.7
通讯作者：
Wu W
中科院分区：
文献类型：
--
作者：
Zhu J;Zhang W;Wang D;Li S;Wu W
本研究采用乙醇注射法制备了甘草酸硬脂酯（SG; SG-NCTD- lip）载去甲斑蝥素（NCTD）脂质体（LIPs）。为提高药物包封率，采用单因素试验和正交设计对其处方进行优化。平衡透析法评价SG-NCTD-LIP体外释放NCTD的情况。MTT法研究SG-NCTD-LIP对HepG2的细胞毒性。结果表明，脂质体的EE为~27.80%，SG-NCTD-LIP的平均粒径为87.5 nm，与溶液中的NCTD相比，SG-NCTD-LIP的体外释放延迟，释放动力学符合一阶模型。MTT实验显示，与游离NCTD相比，SG-NCTD-LIP对HepG2细胞的细胞毒活性增加。综上所述，本研究制备的SG-NCTD-LIP可能是一种很有前途的肝靶向抗癌药物脂质体给药系统。
In the current study, norcantharidin (NCTD)-loaded liposomes (LIPs) modified with stearyl glycyrrhetinate (SG; SG-NCTD-LIP) were prepared by the ethanol injection method. To increase the drug encapsulation efficiency (EE), the formulation of NCTD-LIP was optimized by single factor test and orthogonal design. The release of NCTD in vitro from SG-NCTD-LIP was evaluated by equilibrium dialysis. The cytotoxicity of SG-NCTD-LIP in HepG2 was investigated by MTT assay. The results revealed that the EE of liposomes was ~27.80%, the average SG-NCTD-LIP was 87.5 nm, the in vitro NCTD release from SG-NCTD-LIP was delayed compared with NCTD in solution and the drug-release kinetic followed a first-order model. MTT assays revealed increased cytotoxicity activity against HepG2 cells for SG-NCTD-LIP compared with free NCTD. In conclusion, SG-NCTD-LIP prepared in the present study may be a promising liposomal drug delivery system for anticancer drugs in liver-targeting therapy.
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