Preparation of ropivacaine loaded PLGA microspheres as controlled-release system with narrow size distribution and high loading efficiency
文献类型：期刊论文
| 作者 | Li, Xun1,2; Wei, Yi1 ; Lv, Piping1; Wu, Youbin3; Ogino, Kenji4; Ma, Guanghui1
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| 刊名 | COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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| 出版日期 | 2019-02-05 |
| 卷号 | 562页码:237-246 |
| ISSN号 | 0927-7757 |
| 关键词 | Ropivacaine PLGA microsphere High drug loading Narrow size distribution Reduce cytotoxicity |
| 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. |
| WOS关键词 | BUPIVACAINE ; FORMULATION ; EFFICACY ; ENCAPSULATION ; CYTOTOXICITY ; PARTICLES ; APOPTOSIS ; STRATEGY ; DELIVERY ; DRUGS |
| 资助项目 | National Nature Science Foundation of China[21336010] ; National Key Technology Program[2017ZX09201004014] |
| 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 |
| 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. |
入库方式： OAI收割
来源：过程工程研究所
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