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Int J Pharm. 2016 Oct 15;512(1):22-31. doi: 10.1016/j.ijpharm.2016.08.038. Epub 2016 Aug 18.

(-)-Epigallocatechin gallate (EGCG)-nanoethosomes as a transdermal delivery system for docetaxel to treat implanted human melanoma cell tumors in mice.

Author information

1
The Key Laboratory for Quality Improvement of Agricultural Products of Zhejiang Province, The College of Agricultural and Food Sciences, Zhejiang A & F University, Linan 311300, China.
2
Experimental Animal Center of the Zhejiang Academy of Medical Sciences, Hangzhou 310013, China.
3
Guelph Food Research Center, Agriculture and Agri-Food Canada, Guelph, Ontario N1G 5C9, Canada.
4
Tea Research Institute, Chinese Academy of Agricultural Sciences, Key Laboratory of Tea Biology and Resources Utilization, Ministry of Agriculture, Hangzhou 310008, China.
5
The Key Laboratory for Quality Improvement of Agricultural Products of Zhejiang Province, The College of Agricultural and Food Sciences, Zhejiang A & F University, Linan 311300, China. Electronic address: qizhendu@163.com.

Abstract

(-)-Epigallocatechin-3-O-gallate (EGCG), a versatile natural product in fresh tea leaves and green tea, has been investigated as a preventative treatment for cancers and cardiovascular disease. The objective of this study was to develop EGCG-nanoethosomes for transdermal delivery and to evaluate them for treating subcutaneously implanted human melanoma cell tumors. EGCG-nanoethosomes, composed of 0.2% EGCG, 2% soybean phosphatidylcholine, 30% ethanol, 1% Tween-80 and 0.1% sugar esters, were prepared and characterized using laser transmission electron microscopy. These nanoethosomes were smoother and more compact than basic-nanoethosomes with the same components except for EGCG. The effectiveness of transdermal delivery by EGCG-nanoethosomes was demonstrated in an in vitro permeability assay system using mouse skin. The inhibitory effect of docetaxel (DT) loaded in EGCG-nanoethosomes (DT-EGCG-nanoethosomes) was analyzed by monitoring growth of a subcutaneously implanted tumor from A-375 human melanoma cells in mice. Mice treated with DT-EGCG-nanoethosomes exhibited a significant therapeutic effect, with tumors shrinking, on average, by 31.5% of initial volumes after 14 d treatment. This indicated a potential for treating skin cancer. In a pharmacokinetic study, transdermal delivery by DT-EGCG-nanoethosomes enabled sufficient DT exposure to the tumor. Together, these findings indicated that EGCG-nanoethosomes have great potential as drug carriers for transdermal delivery.

KEYWORDS:

(−)-Epigallocatechin-3-O-gallate; (−)-Epigallocatechin-3-O-gallate (PubChem CID: 65064); Docetaxel; Docetaxel (PubChem CID: 148124); Nanoethosomes; Pharmacokinetics; Skin cancer; Transdermal delivery

PMID:
27544847
DOI:
10.1016/j.ijpharm.2016.08.038
[Indexed for MEDLINE]

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