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Effect of A-317491 delivered by glycolipid-like polymer micelles on endometriosis pain

Authors Yuan M, Ding S, Meng TT, Lu B, Shao S, Zhang X, Yuan H, Hu F

Received 16 July 2017

Accepted for publication 17 September 2017

Published 9 November 2017 Volume 2017:12 Pages 8171—8183

DOI https://doi.org/10.2147/IJN.S146569

Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Dr Linlin Sun


Ming Yuan,1 Shaojie Ding,2 Tingting Meng,3 Binbin Lu,3 Shihong Shao,1 Xinmei Zhang,2 Hong Yuan,3 Fuqiang Hu1,3

1Institute of Marine Biology, Ocean College, Zhejiang University, Zhoushan, 2Department of Gynecology, Women’s Hospital, School of Medicine, Zhejiang University, Hangzhou, 3Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, China

Abstract: Endometriosis is a common gynecological disease with a lack of effective clinical treatment. Current therapy often results in endometriosis pain recurrence and serious side effects. P2X3 receptor, an adenosine triphosphate (ATP)-gated ion channel, might be implicated in endometriosis pain. In this study, chitosan oligosaccharide-g-stearic acid (CSOSA) polymer micelles-coated nanostructured lipid carriers (NLCs) were developed as a novel delivery system for A-317491, a selective P2X3 receptor antagonist for endometriosis pain therapy. A-317491-loaded NLC (NLC/A-317491) could be coated by CSOSA micelles to form CSOSA/NLC/A-317491 nanoparticles. Pheochromocytoma PC12 cells, which highly expressed P2X3 receptors, were used as a cell model, and the CSOSA/NLC/A-317491 partly blocked the Ca2+ influx induced by ATP stimulation. In nude mouse and rat endometriotic models, CSOSA/NLC could accumulate into endometriotic lesions after vein injection. In endometriotic rats, CSOSA/NLC/A-317491 reversed mechanical and heat hyperalgesia with long-term efficacy, which might be attributed to the massive CSOSA/NLC/A-317491 distribution in the endometriotic lesions. In conclusion, A-317491 delivered by CSOSA/NLC nanoparticles attenuated endometriosis pain in rats, and CSOSA/NLC/A-317491 could be used as an effective treatment strategy for P2X3-targeted therapy in endometriosis pain.

Keywords: glycolipid-like polymer, A-317491, nanostructured lipid carriers, endometriosis pain, P2X3 receptor

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