Preparation of ropivacaine loaded PLGA microspheres as controlled-release system with narrow size distribution and high loading efficiency

doi:10.1016/j.colsurfa.2018.11.014

	Preparation of ropivacaine loaded PLGA microspheres as controlled-release system with narrow size distribution and high loading efficiency
	Li, Xun 1,2; Wei, Yi1 ; Lv, Piping 1; Wu, Youbin 3; Ogino, Kenji 4; Ma, Guanghui 1
刊名	COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
	2019-02-05
卷号	562 页码:237-246
关键词	Ropivacaine PLGA microsphere High drug loading Narrow size distribution Reduce cytotoxicity
ISSN号	0927-7757
DOI	10.1016/j.colsurfa.2018.11.014
英文摘要	Ropivacaine loaded microspheres offer an attractive alternative for prolonging the duration of local anesthetics for the pain management. However, traditional microcapsulation methods could not provide microspheres with desired drug loading efficiency and a narrow size distribution, leading to poor patient compliance as well as preparation repeatability. In this study, we proposed to combine O/W emulsion method with novel premix membrane emulsification technique. After the optimization of fabrication procedure, ropivacaine loaded microspheres with narrow size distribution (span 0.469), high drug loading efficiency (49%) and an ideal constant release behavior have been obtained. Especially, it was found that solidification process affected the internal structure of microspheres and the physical state of encapsulated ropivacaine. Furthermore, it was interested that lower polymer molecular weight resulted in higher encapsulation efficiency, which was not consistent with reported results. It was found that this was ascribed to the interaction of PLGA-ropivacaine. All these aspects had considerable influences on the characteristics of microspheres. In addition, the cytotoxicity on different cell lines (SHSY5Y and HaCaT cells) was detected qualitatively and quantitatively. It showed that ropivacaine loaded microspheres did reduce the Reactive oxygen species (ROS) and cytotoxicity prominently compared to free ropivacaine, which could be attributed to the sustained and steady drug release behavior. This study provided some pioneering ideas for encapsulating small molecule drug with poor solubility. The optimized microspheres could be chosen as an ideal candidate for the ropivacaine sustained release with its better drug adherence, lower toxicity of drug burst release and best therapeutic effect.
资助项目	National Nature Science Foundation of China[21336010] ; National Key Technology Program[2017ZX09201004014]
WOS关键词	BUPIVACAINE ; FORMULATION ; EFFICACY ; ENCAPSULATION ; CYTOTOXICITY ; PARTICLES ; APOPTOSIS ; STRATEGY ; DELIVERY ; DRUGS
WOS研究方向	Chemistry
语种	英语
出版者	ELSEVIER SCIENCE BV
WOS记录号	WOS:000454428500029
资助机构	National Nature Science Foundation of China ; National Key Technology Program
内容类型	期刊论文
源URL	[http://ir.ipe.ac.cn/handle/122111/27653]
专题	中国科学院过程工程研究所
通讯作者	Wei, Yi; Ma, Guanghui
作者单位	1.Chinese Acad Sci, Inst Proc Engn, State Key Lab Biochem Engn, PLA Key Lab Biopharmaceut Prod & Formulat Engn, Beijing 100190, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Yichang Humanwell Pharmaceut Co Ltd, Yichang 443008, Peoples R China 4.Tokyo Univ Agr & Technol, Grad Sch Bioapplicat Syst Engn, Koganei, Tokyo 1848588, Japan
推荐引用方式 GB/T 7714	Li, Xun,Wei, Yi,Lv, Piping,et al. Preparation of ropivacaine loaded PLGA microspheres as controlled-release system with narrow size distribution and high loading efficiency[J]. COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS,2019,562:237-246.
APA	Li, Xun,Wei, Yi,Lv, Piping,Wu, Youbin,Ogino, Kenji,&Ma, Guanghui.(2019).Preparation of ropivacaine loaded PLGA microspheres as controlled-release system with narrow size distribution and high loading efficiency.COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS,562,237-246.
MLA	Li, Xun,et al."Preparation of ropivacaine loaded PLGA microspheres as controlled-release system with narrow size distribution and high loading efficiency".COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS 562(2019):237-246.