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A Novel Gel-Forming Solution Based on PEG-DSPE/Solutol HS 15 Mixed Micelles and Gellan Gum for Ophthalmic Delivery of Curcumin

Curcumin (Cur) is a naturally hydrophobic polyphenol with potential pharmacological properties. However, the poor aqueous solubility and low bioavailability of curcumin limits its ocular administration. Thus, the aim of this study was to prepare a mixed micelle in situ gelling system of curcumin (Cu...

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Autores principales: Sai, Na, Dong, Xiaoxv, Huang, Pingqing, You, Longtai, Yang, Chunjing, Liu, Yi, Wang, Wenping, Wu, Huimin, Yu, Yingchao, Du, Yuanyuan, Leng, Xin, Yin, Xingbin, Qu, Changhai, Ni, Jian
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6983186/
https://www.ncbi.nlm.nih.gov/pubmed/31878332
http://dx.doi.org/10.3390/molecules25010081
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author Sai, Na
Dong, Xiaoxv
Huang, Pingqing
You, Longtai
Yang, Chunjing
Liu, Yi
Wang, Wenping
Wu, Huimin
Yu, Yingchao
Du, Yuanyuan
Leng, Xin
Yin, Xingbin
Qu, Changhai
Ni, Jian
author_facet Sai, Na
Dong, Xiaoxv
Huang, Pingqing
You, Longtai
Yang, Chunjing
Liu, Yi
Wang, Wenping
Wu, Huimin
Yu, Yingchao
Du, Yuanyuan
Leng, Xin
Yin, Xingbin
Qu, Changhai
Ni, Jian
author_sort Sai, Na
collection PubMed
description Curcumin (Cur) is a naturally hydrophobic polyphenol with potential pharmacological properties. However, the poor aqueous solubility and low bioavailability of curcumin limits its ocular administration. Thus, the aim of this study was to prepare a mixed micelle in situ gelling system of curcumin (Cur-MM-ISG) for ophthalmic drug delivery. The curcumin mixed micelles (Cur-MMs) were prepared via the solvent evaporation method, after which they were incorporated into gellan gum gels. Characterization tests showed that Cur-MMs were small in size and spherical in shape, with a low critical micelle concentration. Compared with free curcumin, Cur-MMs improved the solubility and stability of curcumin significantly. The ex vivo penetration study revealed that Cur-MMs could penetrate the rabbit cornea more efficiently than the free curcumin. After dispersing the micelles in the gellan gum solution at a ratio of 1:1 (v/v), a transparent Cur-MM-ISG with the characteristics of a pseudoplastic fluid was formed. No obvious irritations were observed in the rabbit eyes after ocular instillation of Cur-MM-ISG. Moreover, Cur-MM-ISG showed a longer retention time on the corneal surface when compared to Cur-MMs using the fluorescein sodium labeling method. These findings indicate that biocompatible Cur-MM-ISG has great potential in ophthalmic drug therapy.
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spelling pubmed-69831862020-02-06 A Novel Gel-Forming Solution Based on PEG-DSPE/Solutol HS 15 Mixed Micelles and Gellan Gum for Ophthalmic Delivery of Curcumin Sai, Na Dong, Xiaoxv Huang, Pingqing You, Longtai Yang, Chunjing Liu, Yi Wang, Wenping Wu, Huimin Yu, Yingchao Du, Yuanyuan Leng, Xin Yin, Xingbin Qu, Changhai Ni, Jian Molecules Article Curcumin (Cur) is a naturally hydrophobic polyphenol with potential pharmacological properties. However, the poor aqueous solubility and low bioavailability of curcumin limits its ocular administration. Thus, the aim of this study was to prepare a mixed micelle in situ gelling system of curcumin (Cur-MM-ISG) for ophthalmic drug delivery. The curcumin mixed micelles (Cur-MMs) were prepared via the solvent evaporation method, after which they were incorporated into gellan gum gels. Characterization tests showed that Cur-MMs were small in size and spherical in shape, with a low critical micelle concentration. Compared with free curcumin, Cur-MMs improved the solubility and stability of curcumin significantly. The ex vivo penetration study revealed that Cur-MMs could penetrate the rabbit cornea more efficiently than the free curcumin. After dispersing the micelles in the gellan gum solution at a ratio of 1:1 (v/v), a transparent Cur-MM-ISG with the characteristics of a pseudoplastic fluid was formed. No obvious irritations were observed in the rabbit eyes after ocular instillation of Cur-MM-ISG. Moreover, Cur-MM-ISG showed a longer retention time on the corneal surface when compared to Cur-MMs using the fluorescein sodium labeling method. These findings indicate that biocompatible Cur-MM-ISG has great potential in ophthalmic drug therapy. MDPI 2019-12-24 /pmc/articles/PMC6983186/ /pubmed/31878332 http://dx.doi.org/10.3390/molecules25010081 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Sai, Na
Dong, Xiaoxv
Huang, Pingqing
You, Longtai
Yang, Chunjing
Liu, Yi
Wang, Wenping
Wu, Huimin
Yu, Yingchao
Du, Yuanyuan
Leng, Xin
Yin, Xingbin
Qu, Changhai
Ni, Jian
A Novel Gel-Forming Solution Based on PEG-DSPE/Solutol HS 15 Mixed Micelles and Gellan Gum for Ophthalmic Delivery of Curcumin
title A Novel Gel-Forming Solution Based on PEG-DSPE/Solutol HS 15 Mixed Micelles and Gellan Gum for Ophthalmic Delivery of Curcumin
title_full A Novel Gel-Forming Solution Based on PEG-DSPE/Solutol HS 15 Mixed Micelles and Gellan Gum for Ophthalmic Delivery of Curcumin
title_fullStr A Novel Gel-Forming Solution Based on PEG-DSPE/Solutol HS 15 Mixed Micelles and Gellan Gum for Ophthalmic Delivery of Curcumin
title_full_unstemmed A Novel Gel-Forming Solution Based on PEG-DSPE/Solutol HS 15 Mixed Micelles and Gellan Gum for Ophthalmic Delivery of Curcumin
title_short A Novel Gel-Forming Solution Based on PEG-DSPE/Solutol HS 15 Mixed Micelles and Gellan Gum for Ophthalmic Delivery of Curcumin
title_sort novel gel-forming solution based on peg-dspe/solutol hs 15 mixed micelles and gellan gum for ophthalmic delivery of curcumin
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6983186/
https://www.ncbi.nlm.nih.gov/pubmed/31878332
http://dx.doi.org/10.3390/molecules25010081
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