中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Preparation of novel ropivacaine hydrochloride-loaded PLGA microspheres based on post-loading mode and efficacy evaluation

文献类型:期刊论文

作者Wen, Kang1,2; Na, Xiangming1,2; Yuan, Miaomiao2,3; Bazybek, Nardana1,2; Li, Xun1,2; Wei, Yi2; Ma, Guanghui1,2
刊名COLLOIDS AND SURFACES B-BIOINTERFACES
出版日期2022-02-01
卷号210页码:8
关键词ropivacaine hydrochloride microspheres self-healing sciatic nerve blockade model
ISSN号0927-7765
DOI10.1016/j.colsurfb.2021.112215
英文摘要Low encapsulation efficiency of the drug usually exist in hydrophilic drug which was embedded by hydrophobic materials directly in traditional method. In order to solve this problem, a novel preparation strategy which called "post-loading mode" was innovatively designed in this study: ropivacaine hydrochloride (ROP), a hydrophilic drug used in the field of anesthesia and analgesia, was encapsulated into the pre-prepared porous Poly (lactic-coglycolic acid) (PLGA) microspheres; the porous PLGA microspheres (PLGA-Ms) with self-healing characteristic were used to obtain ROP-PLGA-Ms (with particle size around were 38 mu m), in which drug loading (DL) was 8.72%. A rat sciatic nerve block model was established to evaluate the efficacy of ROP-PLGA-Ms. Exparel (R), a bupivacaine liposome suspension approved by the FDA, was defined as reference agents in this study. The results showed that the injection of ROP, Exparel (R), and ROP-PLGA-Ms were injected to the peripheral sciatic nerve could lead to motor dysfunction and sensory nerve block unanimously, and the onset time was less than 10 min for all cases. In addition, in comparison with ROP injection and Exparel (R), the nerve block time of ROP-PLGA-Ms was significantly prolonged (P < 0.05). Effective analgesia duration of ROP-PLGA-Ms was about 5 h, 2.5 and 1.7 folds longer than that of ROP injection and Exparel (R), respectively. The rats in each group could recover eventually within 8 h after administration. H&E showed that no inflammatory reaction was observed at the injection location. Analysis of blood biochemistry showed an insignificant difference between the microsphere experimental group and the negative group, which further indicated the safety of microsphere bioformulation.
WOS关键词SELF-HEALING ENCAPSULATION ; DRUG-DELIVERY SYSTEMS ; LOCAL-ANESTHETICS ; RELEASE ; DEXMEDETOMIDINE ; BUPIVACAINE ; BLOCK
资助项目National Key Technology Program[2017ZX09201004014]
WOS研究方向Biophysics ; Chemistry ; Materials Science
语种英语
WOS记录号WOS:000734889800001
出版者ELSEVIER
资助机构National Key Technology Program
源URL[http://ir.ipe.ac.cn/handle/122111/51546]  
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.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
2.Chinese Acad Sci, Inst Proc Engn, State Key Lab Biochem Engn, Beijing 100190, Peoples R China
3.Wuhan Inst Technol, Wuhan 430205, Peoples R China
推荐引用方式
GB/T 7714
Wen, Kang,Na, Xiangming,Yuan, Miaomiao,et al. Preparation of novel ropivacaine hydrochloride-loaded PLGA microspheres based on post-loading mode and efficacy evaluation[J]. COLLOIDS AND SURFACES B-BIOINTERFACES,2022,210:8.
APA Wen, Kang.,Na, Xiangming.,Yuan, Miaomiao.,Bazybek, Nardana.,Li, Xun.,...&Ma, Guanghui.(2022).Preparation of novel ropivacaine hydrochloride-loaded PLGA microspheres based on post-loading mode and efficacy evaluation.COLLOIDS AND SURFACES B-BIOINTERFACES,210,8.
MLA Wen, Kang,et al."Preparation of novel ropivacaine hydrochloride-loaded PLGA microspheres based on post-loading mode and efficacy evaluation".COLLOIDS AND SURFACES B-BIOINTERFACES 210(2022):8.

入库方式: OAI收割

来源:过程工程研究所

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