New nanomicelle curcumin formulation for ocular delivery: improved stability, solubility, and ocular anti-inflammatory treatment

Context: A stable topical ophthalmic curcumin formulation with high solubility, stability, and efficacy is needed for pharmaceutical use in clinics. Objectives: The objective of this article was to describe a novel curcumin containing a nanomicelle formulation using a polyvinyl caprolactam-polyvinyl...

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Veröffentlicht in:Drug development and industrial pharmacy 2017-11, Vol.43 (11), p.1846-1857
Hauptverfasser: Li, Mengshuang, Xin, Meng, Guo, Chuanlong, Lin, Guiming, Wu, Xianggen
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container_end_page 1857
container_issue 11
container_start_page 1846
container_title Drug development and industrial pharmacy
container_volume 43
creator Li, Mengshuang
Xin, Meng
Guo, Chuanlong
Lin, Guiming
Wu, Xianggen
description Context: A stable topical ophthalmic curcumin formulation with high solubility, stability, and efficacy is needed for pharmaceutical use in clinics. Objectives: The objective of this article was to describe a novel curcumin containing a nanomicelle formulation using a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (PVCL-PVA-PEG) graft copolymer. Methods: Nanomicelle curcumin was formulated and optimized and then further evaluated for in vitro cytotoxicity/in vivo ocular irritation, in vitro cellular uptake/in vivo corneal permeation, and in vitro antioxidant activity/in vivo anti-inflammatory efficacy. Results: The solubility, chemical stability, and antioxidant activity were greatly improved after the encapsulation of the PVCL-PVA-PEG nanomicelles. The nanomicelle curcumin ophthalmic solution was simple to prepare and the nanomicelles are stable to the storage conditions, and it had good cellular tolerance. Nanomicelle curcumin also had excellent ocular tolerance in rabbits. The use of nanomicelles significantly improved in vitro cellular uptake and in vivo corneal permeation as well as improved anti-inflammatory efficacy when compared with a free curcumin solution. Conclusions: These findings indicate that nanomicelles could be promising topical delivery systems for the ocular administration of curcumin.
doi_str_mv 10.1080/03639045.2017.1349787
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Objectives: The objective of this article was to describe a novel curcumin containing a nanomicelle formulation using a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (PVCL-PVA-PEG) graft copolymer. Methods: Nanomicelle curcumin was formulated and optimized and then further evaluated for in vitro cytotoxicity/in vivo ocular irritation, in vitro cellular uptake/in vivo corneal permeation, and in vitro antioxidant activity/in vivo anti-inflammatory efficacy. Results: The solubility, chemical stability, and antioxidant activity were greatly improved after the encapsulation of the PVCL-PVA-PEG nanomicelles. The nanomicelle curcumin ophthalmic solution was simple to prepare and the nanomicelles are stable to the storage conditions, and it had good cellular tolerance. Nanomicelle curcumin also had excellent ocular tolerance in rabbits. The use of nanomicelles significantly improved in vitro cellular uptake and in vivo corneal permeation as well as improved anti-inflammatory efficacy when compared with a free curcumin solution. Conclusions: These findings indicate that nanomicelles could be promising topical delivery systems for the ocular administration of curcumin.</description><identifier>ISSN: 0363-9045</identifier><identifier>EISSN: 1520-5762</identifier><identifier>DOI: 10.1080/03639045.2017.1349787</identifier><identifier>PMID: 28665151</identifier><language>eng</language><publisher>England: Taylor &amp; Francis</publisher><subject>Administration, Ophthalmic ; Animals ; Anti-Inflammatory Agents - chemistry ; Anti-Inflammatory Agents - pharmacology ; Chemistry, Pharmaceutical ; Cornea - chemistry ; Cornea - physiopathology ; Curcumin ; Curcumin - chemistry ; Curcumin - pharmacology ; Drug Delivery Systems - methods ; Micelles ; nanomicelle ; Nanoparticles ; ocular drug delivery ; Ophthalmic Solutions - administration &amp; dosage ; Ophthalmic Solutions - chemistry ; Polyethylene Glycols - chemistry ; polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PVCL-PVA-PEG) ; Polyvinyls - chemistry ; Rabbits ; Solubility ; stability</subject><ispartof>Drug development and industrial pharmacy, 2017-11, Vol.43 (11), p.1846-1857</ispartof><rights>2017 Informa UK Limited, trading as Taylor &amp; Francis Group 2017</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c413t-274945c18899db1fb441a7a55f8f114b6a22262a7ef21587b4cb1bb9d0c02f2d3</citedby><cites>FETCH-LOGICAL-c413t-274945c18899db1fb441a7a55f8f114b6a22262a7ef21587b4cb1bb9d0c02f2d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/28665151$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Li, Mengshuang</creatorcontrib><creatorcontrib>Xin, Meng</creatorcontrib><creatorcontrib>Guo, Chuanlong</creatorcontrib><creatorcontrib>Lin, Guiming</creatorcontrib><creatorcontrib>Wu, Xianggen</creatorcontrib><title>New nanomicelle curcumin formulation for ocular delivery: improved stability, solubility, and ocular anti-inflammatory treatment</title><title>Drug development and industrial pharmacy</title><addtitle>Drug Dev Ind Pharm</addtitle><description>Context: A stable topical ophthalmic curcumin formulation with high solubility, stability, and efficacy is needed for pharmaceutical use in clinics. 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subjects Administration, Ophthalmic
Animals
Anti-Inflammatory Agents - chemistry
Anti-Inflammatory Agents - pharmacology
Chemistry, Pharmaceutical
Cornea - chemistry
Cornea - physiopathology
Curcumin
Curcumin - chemistry
Curcumin - pharmacology
Drug Delivery Systems - methods
Micelles
nanomicelle
Nanoparticles
ocular drug delivery
Ophthalmic Solutions - administration & dosage
Ophthalmic Solutions - chemistry
Polyethylene Glycols - chemistry
polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PVCL-PVA-PEG)
Polyvinyls - chemistry
Rabbits
Solubility
stability
title New nanomicelle curcumin formulation for ocular delivery: improved stability, solubility, and ocular anti-inflammatory treatment
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