Preparation of Celastrol-Coicis Semen Oil Microemulsions and Evaluation of Its  Antitumor Activity

LI Ping; HUANG Meng-meng; LIU Yu-ping; JU Jian-ming; CHEN Yan

doi:10.13422/j.cnki.syfjx.2017060001

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Preparation of Celastrol-Coicis Semen Oil Microemulsions and Evaluation of Its Antitumor Activity

更新时间：2024-01-04

- Preparation of Celastrol-Coicis Semen Oil Microemulsions and Evaluation of Its Antitumor Activity
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 23, Issue 6, Pages: 1-6(2017)
- 作者机构：
- 作者简介：
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- DOI：10.13422/j.cnki.syfjx.2017060001
  CLC： R283.6
- Published：2017
- 稿件说明：
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LI Ping, HUANG Meng-meng, LIU Yu-ping, et al. Preparation of Celastrol-Coicis Semen Oil Microemulsions and Evaluation of Its Antitumor Activity[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(6): 1-6.
DOI：

LI Ping, HUANG Meng-meng, LIU Yu-ping, et al. Preparation of Celastrol-Coicis Semen Oil Microemulsions and Evaluation of Its Antitumor Activity[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(6): 1-6. DOI： 10.13422/j.cnki.syfjx.2017060001.

摘要

目的：制备雷公藤红素-薏苡仁油微乳（CC-MEs）并对其理化性质及体外抗肿瘤活性进行评价。方法：通过考察雷公藤红素在不同介质中的溶解度，筛选CC-MEs的最佳油相、乳化剂及助乳化剂。采用水滴定法制备微乳，根据其粒径，多分散指数（PDI），Zeta电位，包封率和载药量筛选CC-MEs的最佳处方，并对制备微乳的形态、稳定性和体外释放进行考察。通过四甲基偶氮唑盐法考察CC-MEs对宫颈癌HeLa细胞的毒性，评价其体外抗肿瘤活性。结果：CC-MEs最佳处方为雷公藤红素10 mg，薏苡仁油既为药物又兼作油相（用量400 mg），聚氧乙烯氢化蓖麻油450 mg，聚乙二醇400 150 mg；制备的微乳外观形态圆整，平均粒径（31.63±0.63）nm，PDI 0.06±0.01，Zeta电位（-10.14±1.35）mV，48 h时雷公藤红素体外累积释放度（19.89±0.59）%，具有一定的缓释特性。CC-MEs对HeLa细胞具有较好的增殖抑制作用，其半数抑制浓度以薏苡仁油计为20.7 mg·L-1，以雷公藤红素计为0.82 μmol·L-1，联合用药指数0.93，表明两药联用具有协同作用。结论：CC-MEs粒径小且分布均匀、稳定性好、辅料用量少。雷公藤红素与薏苡仁油组分配伍制剂能够增强对HeLa细胞的增殖抑制作用，二者具有协同抗肿瘤功效。

Abstract

Objective: To prepare celastrol-Coicis Semen oil microemulsions (CC-MEs) and evaluate its physicochemical properties and in vitro anticancer activity. Method: The optimal oil phase

emulsifier and co-emulsifier of CC-MEs were selected by examining solubility of celastrol in different media.According to determination of particle size

Zeta potential

morphology

encapsulation efficiency and drug loading

the prescription was optimized.The stability and in vitro release of the microemulsions was investigated.The cytotoxicity of CC-MEs on cervical cancer HeLa cell was studied by MTT assay and its in vitro anti-tumor activity was evaluated. Result: Optimum prescription was as following:celastrol of 10 mg

Coicis Semen oil of 400 mg as material and oil phase

cremophor RH40 of 450 mg and polyethylene glycol 400 (PEG-400) of 150 mg.CC-MEs displayed the spherical surface with mean particle size of (31.63±0.63) nm

polydispersity index (PDI) of 0.06±0.01 and Zeta potential of (-10.14±1.35) mV.The cumulative in vitro release rate of celastrol was (19.89±0.59)% in 48 h with a sustained-release characteristics.MTT experiment showed that 50%inhibitory concentrations (IC50) of CC-MEs were 0.82 μmol·L-1 counted as celastrol and 20.7 mg·L-1 counted as Coicis Semen oil;the combination index (CI) was 0.93

indicating that celastrol and Coicis Semen oil had a synergistic effect. Conclusion: CC-MEs presents small particle size

well-distributed

good stability and less excipients.In addition

preparations with the compatibility of celastrol and Coicis Semen oil can enhance the inhibitory effect on proliferation of HeLa cell.

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