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...

Full description

Bibliographic Details
Main Authors: Mengshuang Li, Jie Lan, Xuefei Li, Meng Xin, Hui Wang, Fan Zhang, Xiaohong Lu, Zengfang Zhuang, Xianggen Wu
Format: Article
Language:English
Published: Taylor & Francis Group 2019-01-01
Series:Drug Delivery
Subjects:
Online Access:http://dx.doi.org/10.1080/10717544.2019.1600077
_version_ 1831719217224744960
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
work_keys_str_mv AT mengshuangli novelultrasmallmicellesbasedonginsenosiderb1apotentialnanoplatformforoculardrugdelivery
AT jielan novelultrasmallmicellesbasedonginsenosiderb1apotentialnanoplatformforoculardrugdelivery
AT xuefeili novelultrasmallmicellesbasedonginsenosiderb1apotentialnanoplatformforoculardrugdelivery
AT mengxin novelultrasmallmicellesbasedonginsenosiderb1apotentialnanoplatformforoculardrugdelivery
AT huiwang novelultrasmallmicellesbasedonginsenosiderb1apotentialnanoplatformforoculardrugdelivery
AT fanzhang novelultrasmallmicellesbasedonginsenosiderb1apotentialnanoplatformforoculardrugdelivery
AT xiaohonglu novelultrasmallmicellesbasedonginsenosiderb1apotentialnanoplatformforoculardrugdelivery
AT zengfangzhuang novelultrasmallmicellesbasedonginsenosiderb1apotentialnanoplatformforoculardrugdelivery
AT xianggenwu novelultrasmallmicellesbasedonginsenosiderb1apotentialnanoplatformforoculardrugdelivery