Novel ultra-small micelles based on rebaudioside A: A potential nanoplatform for ocular drug delivery

doi:10.1016/j.ijpharm.2018.10.006

CORC > 自然资源部第一海洋研究所 > 自然资源部第一海洋研究所 > 业务部门 > 海洋生态研究中心

	Novel ultra-small micelles based on rebaudioside A: A potential nanoplatform for ocular drug delivery
	Song, Kaichao 1; Xin, Meng 1,2; Yu, Hongxia 3; Zheng, Zhou 4; Li, Jun 5; Li, Mengshuang 1,6; Guo, Huimin 1; Tan, Youlan 1; Wu, Xianggen 1
刊名	INTERNATIONAL JOURNAL OF PHARMACEUTICS
	2018-12
卷号	552 期号:1-2 页码:265-276
关键词	Rebaudioside A Coumarin-6 Micelle Ocular drug delivery
ISSN号	0378-5173
DOI	10.1016/j.ijpharm.2018.10.006
英文摘要	We investigated if the self-assembled micelles of rebaudioside A (RA) could potentially be utilized as an ocular drug-delivery system in this investigation. RA self-assembled into micelles with ultra-small particle sizes ( < 4 nm) in a homogeneous distribution state (polydispersity index < 0.3). RA had good cellular tolerance and no cytotoxicity was observed at concentrations <= 18.5 mg/ml at 72 h of incubation. RA also did not cause cell apoptosis at concentration <= 12 mg/ml. Coumarin-6 (Cou6)-loaded RA micelles had good cellular tolerance and in vivo non-irritants to the rabbit eyes. RA micelles dramatically improved the cellular uptake of Cou6 (compared to free-Cou6 P < 0.05); an energy-independent, active, intracellular endocytosis pathway was apparently involved, and cellular organelles such as lysosomes, endoplasmic reticuli, and mitochondria were observed with a high distribution of Cou6, while a much more sophisticated endocytosis pathway was apparently involved in the ex vivo corneal endocytosis mechanism tests. The use of RA micelles significantly improved in vivo corneal permeation of the encapsulated Cou6 when compared to free-Cou6 eye drops (P < 0.05). These findings indicate that RA micelle formulations have great potential as a novel ocular drug-delivery system to improve the bioavailability of hydrophobic drugs.
资助项目	Project of Medical and Health Technology Development Program in Shandong Province, China[2017WS633]
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER SCIENCE BV
WOS记录号	WOS:000447985800030
内容类型	期刊论文
源URL	[http://ir.fio.com.cn/handle/2SI8HI0U/2758]
专题	业务部门_海洋生态研究中心
作者单位	1.Qingdao Univ Sci & Technol, Coll Chem Engn, Dept Pharm, Qingdao 266042, Peoples R China; 2.Binshou Med Univ, Yantai Affiliated Hosp, Dept Ophthalmol, Yantai 264100, Peoples R China; 3.Qingdao Univ, Sch Pharm, Dept Pharmacol, Qingdao 266021, Peoples R China; 4.State Ocean Adm, Inst Oceanog 1, Key Lab Marine Bioact Subst, Qingdao 266061, Peoples R China; 5.Shandong Acad Med Sci, Shandong Eye Inst, Qingdao Eye Hosp, Qingdao 266071, Peoples R China; 6.Qingdao Women & Childrens Hosp, Pharm Intravenous Admixture Serv, Qingdao 266034, Peoples R China
推荐引用方式 GB/T 7714	Song, Kaichao,Xin, Meng,Yu, Hongxia,et al. Novel ultra-small micelles based on rebaudioside A: A potential nanoplatform for ocular drug delivery[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2018,552(1-2):265-276.
APA	Song, Kaichao.,Xin, Meng.,Yu, Hongxia.,Zheng, Zhou.,Li, Jun.,...&Wu, Xianggen.(2018).Novel ultra-small micelles based on rebaudioside A: A potential nanoplatform for ocular drug delivery.INTERNATIONAL JOURNAL OF PHARMACEUTICS,552(1-2),265-276.
MLA	Song, Kaichao,et al."Novel ultra-small micelles based on rebaudioside A: A potential nanoplatform for ocular drug delivery".INTERNATIONAL JOURNAL OF PHARMACEUTICS 552.1-2(2018):265-276.