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Targeted delivery of ginsenoside compound K using TPGS/PEG-PCL mixed micelles for effective treatment of lung cancer

Authors Yang L, Zhang Z, Hou J, Jin X, Ke Z, Liu D, Du M, Jia X, Lv H

Received 19 June 2017

Accepted for publication 9 August 2017

Published 17 October 2017 Volume 2017:12 Pages 7653—7667

DOI https://doi.org/10.2147/IJN.S144305

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Govarthanan Muthusamy

Peer reviewer comments 2

Editor who approved publication: Dr Linlin Sun


Lei Yang,1,2 Zhenghai Zhang,1 Jian Hou,1,2 Xin Jin,1 Zhongcheng Ke,1 Dan Liu,1 Mei Du,1 Xiaobing Jia,1,2 Huixia Lv3

1Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Jiangsu, Nanjing, China; 2College of Pharmacy, Jiangsu University, Jiangsu, Zhenjiang, China; 3Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Jiangsu Sheng, China

Abstract: Ginsenoside compound K (CK) is one of the effective ingredients in antitumor composition of ginsenoside. However, the poor water solubility and significant efflux have limited the widespread clinical use of CK. In this study, preparation of novel CK-loaded D-alpha-tocopheryl polyethylene glycol 1,000 succinate/poly(ethylene glycol)-poly(ε-caprolactone) mixed micelles (CK-M) is discussed to solve the above problems. Particle size, zeta potential, and morphology were characterized using dynamic light scattering and transmission electron microscopy. CK-M are spherical shaped with an average particle size of 53.07±1.31 nm with high drug loading of 11.19%±0.87% and entrapment efficiency of 94.60%±1.45%. Water solubility of CK was improved to 3.78±0.09 mg/mL, which was ~107.35 times higher than free CK. A549 and PC-9 cells were used to evaluate in vitro cytotoxicity and cellular uptake. IC50 values of CK-M in A549 and PC-9 cells (24 h) were 25.43±2.18 and 18.35±1.90 µg/mL, respectively. Enhanced cellular uptake of CK-M was observed in both cells. Moreover, CK-M promoted tumor cell apoptosis, inhibited tumor cell invasion, metastasis, and efflux through regulation of Bax, Bcl-2, matrix metalloproteinase-2, Caspase-3, and P-glycoprotein. In vivo imaging indicated that CK-M has excellent tumor targeting effect within 24 h, and the relative tumor inhibition rate of CK-M was 52.04%±4.62% compared with control group (P<0.01). Thus, CK-M could be an appropriate delivery agent for enhanced solubility and antitumor effect of CK.

Keywords: ginsenoside compound K, TPGS, PEG-PCL, mixed micelles, antitumor, non-small cell lung cancer

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