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甘草次酸硬脂酯修饰去甲斑蝥素脂质体的制备与表征

Preparation and characterization of norcantharidin liposomes modified with stearyl glycyrrhetinate.

作者信息

Zhu Jing, Zhang Wei, Wang Dandan, Li Suzhen, Wu Wei

机构信息

Department of Pharmaceutics, College of Pharmacy, Guilin Medical University, Guilin, Guangxi 541004, P.R. China.

Clinical Experimental Teaching Center, Affiliated Hospital of Guilin Medical University, Guilin, Guangxi 541004, P.R. China.

出版信息

Exp Ther Med. 2018 Sep;16(3):1639-1646. doi: 10.3892/etm.2018.6416. Epub 2018 Jul 6.

DOI:10.3892/etm.2018.6416
PMID:30186382
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6122258/
Abstract

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 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 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.

摘要

在本研究中，采用乙醇注入法制备了硬脂酰甘草次酸（SG）修饰的载去甲斑蝥素（NCTD）脂质体（LIPs，即SG-NCTD-LIP）。为提高药物包封率（EE），通过单因素试验和正交设计对NCTD-LIP的处方进行优化。采用平衡透析法评价SG-NCTD-LIP中NCTD的释放情况。采用MTT法研究SG-NCTD-LIP对HepG2细胞的细胞毒性。结果显示，脂质体的包封率约为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中NCTD的释放延迟，且药物释放动力学符合一级模型。MTT试验显示，与游离NCTD相比，SG-NCTD-LIP对HepG2细胞的细胞毒性活性增强。总之，本研究制备的SG-NCTD-LIP可能是一种用于肝癌靶向治疗的有前景的脂质体药物递送系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/979e65d7d987/etm-16-03-1639-g06.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/9ec6e25f5471/etm-16-03-1639-g00.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/ba31599c9d06/etm-16-03-1639-g01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/31786d476b7d/etm-16-03-1639-g02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/9c1ba6e5aa17/etm-16-03-1639-g03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/2ee5d8e16bf8/etm-16-03-1639-g04.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/554fbd654371/etm-16-03-1639-g05.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/979e65d7d987/etm-16-03-1639-g06.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/9ec6e25f5471/etm-16-03-1639-g00.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/ba31599c9d06/etm-16-03-1639-g01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/31786d476b7d/etm-16-03-1639-g02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/9c1ba6e5aa17/etm-16-03-1639-g03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/2ee5d8e16bf8/etm-16-03-1639-g04.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/554fbd654371/etm-16-03-1639-g05.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6339/6122258/979e65d7d987/etm-16-03-1639-g06.jpg

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