Novel ultra-small micelles based on ginsenoside Rb1: a potential nanoplatform for ocular drug delivery
Objectives: Ginsenosides Rb1 (Rb1) could form micelles in aqueous solutions. Self-assembled Rb1 micelles could potentially be utilized as ocular drug delivery system, and it was postulated that the encapsulation of a medicine within Rb1 micelles might strengthen the drug’s therapeutic action and red...
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Format: | Article |
Language: | English |
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Taylor & Francis Group
2019-01-01
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Series: | Drug Delivery |
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Online Access: | http://dx.doi.org/10.1080/10717544.2019.1600077 |
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author | Mengshuang Li Jie Lan Xuefei Li Meng Xin Hui Wang Fan Zhang Xiaohong Lu Zengfang Zhuang Xianggen Wu |
author_facet | Mengshuang Li Jie Lan Xuefei Li Meng Xin Hui Wang Fan Zhang Xiaohong Lu Zengfang Zhuang Xianggen Wu |
author_sort | Mengshuang Li |
collection | DOAJ |
description | Objectives: Ginsenosides Rb1 (Rb1) could form micelles in aqueous solutions. Self-assembled Rb1 micelles could potentially be utilized as ocular drug delivery system, and it was postulated that the encapsulation of a medicine within Rb1 micelles might strengthen the drug’s therapeutic action and reduce side effects. Methods: Diclofenac-loaded Rb1 micelles (Rb1-Dic micelles) were formulated, optimized, and then further evaluated for in vitro cytotoxicity/in vivo ocular irritation, in vivo corneal permeation, and in vivo anti-inflammatory efficacy. Results: Rb1 self-assembled into micelles with ultra-small particle size (<8 nm) in a homogeneous distribution state (polydispersity index [PDI] < 0.3). Diclofenac was highly encapsulated into the micelles according to the weight ratios of Rb1 to diclofenac. The ophthalmic solution of Rb1-Dic micelle was simple to prepare. Rb1 had good cellular tolerance, and it also improved the cellular tolerance of the encapsulated diclofenac. Rb1-Dic micelles also showed non-irritants to the rabbit eyes. The use of Rb1 micelles significantly improved the in vivo corneal permeation as well as the anti-inflammatory efficacy of diclofenac when compared to commercial diclofenac eye drops. Conclusion: Rb1 micelle formulations have great potential as a novel ocular drug delivery system to improve the bioavailability of drugs such as diclofenac. |
first_indexed | 2024-12-21T02:35:10Z |
format | Article |
id | doaj.art-3b2812d03b654edca3e8034564404b16 |
institution | Directory Open Access Journal |
issn | 1071-7544 1521-0464 |
language | English |
last_indexed | 2024-12-21T02:35:10Z |
publishDate | 2019-01-01 |
publisher | Taylor & Francis Group |
record_format | Article |
series | Drug Delivery |
spelling | doaj.art-3b2812d03b654edca3e8034564404b162022-12-21T19:18:50ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642019-01-0126148148910.1080/10717544.2019.16000771600077Novel ultra-small micelles based on ginsenoside Rb1: a potential nanoplatform for ocular drug deliveryMengshuang Li0Jie Lan1Xuefei Li2Meng Xin3Hui Wang4Fan Zhang5Xiaohong Lu6Zengfang Zhuang7Xianggen Wu8Qingdao University of Science and TechnologyShandong Eye Institute, Shandong Academy of Medical SciencesQingdao University of Science and TechnologyQingdao University of Science and TechnologyQingdao University of Science and TechnologyQingdao University of Science and TechnologyQingdao University of Science and TechnologyQingdao University of Science and TechnologyQingdao University of Science and TechnologyObjectives: Ginsenosides Rb1 (Rb1) could form micelles in aqueous solutions. Self-assembled Rb1 micelles could potentially be utilized as ocular drug delivery system, and it was postulated that the encapsulation of a medicine within Rb1 micelles might strengthen the drug’s therapeutic action and reduce side effects. Methods: Diclofenac-loaded Rb1 micelles (Rb1-Dic micelles) were formulated, optimized, and then further evaluated for in vitro cytotoxicity/in vivo ocular irritation, in vivo corneal permeation, and in vivo anti-inflammatory efficacy. Results: Rb1 self-assembled into micelles with ultra-small particle size (<8 nm) in a homogeneous distribution state (polydispersity index [PDI] < 0.3). Diclofenac was highly encapsulated into the micelles according to the weight ratios of Rb1 to diclofenac. The ophthalmic solution of Rb1-Dic micelle was simple to prepare. Rb1 had good cellular tolerance, and it also improved the cellular tolerance of the encapsulated diclofenac. Rb1-Dic micelles also showed non-irritants to the rabbit eyes. The use of Rb1 micelles significantly improved the in vivo corneal permeation as well as the anti-inflammatory efficacy of diclofenac when compared to commercial diclofenac eye drops. Conclusion: Rb1 micelle formulations have great potential as a novel ocular drug delivery system to improve the bioavailability of drugs such as diclofenac.http://dx.doi.org/10.1080/10717544.2019.1600077ginsenoside rb1diclofenacmicelleocular drug delivery |
spellingShingle | Mengshuang Li Jie Lan Xuefei Li Meng Xin Hui Wang Fan Zhang Xiaohong Lu Zengfang Zhuang Xianggen Wu Novel ultra-small micelles based on ginsenoside Rb1: a potential nanoplatform for ocular drug delivery Drug Delivery ginsenoside rb1 diclofenac micelle ocular drug delivery |
title | Novel ultra-small micelles based on ginsenoside Rb1: a potential nanoplatform for ocular drug delivery |
title_full | Novel ultra-small micelles based on ginsenoside Rb1: a potential nanoplatform for ocular drug delivery |
title_fullStr | Novel ultra-small micelles based on ginsenoside Rb1: a potential nanoplatform for ocular drug delivery |
title_full_unstemmed | Novel ultra-small micelles based on ginsenoside Rb1: a potential nanoplatform for ocular drug delivery |
title_short | Novel ultra-small micelles based on ginsenoside Rb1: a potential nanoplatform for ocular drug delivery |
title_sort | novel ultra small micelles based on ginsenoside rb1 a potential nanoplatform for ocular drug delivery |
topic | ginsenoside rb1 diclofenac micelle ocular drug delivery |
url | http://dx.doi.org/10.1080/10717544.2019.1600077 |
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