Preparation, characterization and in vivo efficacy evaluation of ropivacaine O/W emulsion by premix membrane emulsification
文献类型：期刊论文
| 作者 | Yuan, Miaomiao1; Na, Xiangming2,3; Liu, Jingxuan2; Zhang, Youhong1; Wei, Yi2 ; Ma, Guanghui2,3
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| 刊名 | COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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| 出版日期 | 2022-05-05 |
| 卷号 | 640页码:9 |
| ISSN号 | 0927-7757 |
| 关键词 | Ropivacaine emulsion Premix membrane emulsion Sciatic nerve blockade model Cutaneous trunci pinprick model Safety evaluation |
| DOI | 10.1016/j.colsurfa.2022.128316 |
| 英文摘要 | Ropivacaine (ROP), a new type of amide local anesthetic (LA) with low cardiac and neurotoxicity, is used to treat postoperative pain. However, ROP has a short half-life (t1/2 = 1.8 h) and the analgesic duration of a single-dose injection last only 3-4 h, which cannot meet clinical needs. In order to solve the problem, we combined an O/W emulsion method with a premix membrane emulsion technique to prepare sustained-release ropivacaine-loaded emulsion (ROP-E) with narrow droplets size distribution. As a result, the ROP-E about 8.385 mu m with a span value of 0.737 was obtained. Moreover, the sciatic nerve block model and the cutaneous trunci pinprick model were established to evaluate the efficacy of ROP-E in vivo. The results of the sciatic nerve model showed that the sensory nerve block duration (4.27 h) of ROP-E was significantly prolonged, which was 2.15 and 1.42 folds of ROP injection and Exparel (R) formulation, respectively. Similarly, the motor nerve block duration (3.62 h) was 1.8 and 1.46 folds of ROP injection and Exparel (R) formulation, respectively. Effective analgesia duration of ROP-E was about 18 h, 2.25 folds longer than that of ROP injection in the cutaneous trunci pinprick model. Besides, the ROP-E displayed excellent stability according to the droplet size, drug loading concentration, in vivo and in vitro release. H&E and blood biochemistry showed an insignificant difference between the ROP-E and the ROP injection, which further indicated the safety of ROP-E. These results suggested that ROP-E may be useful for sustained release of local anesthetics to prolong analgesia without causing systemic toxicity. |
| WOS关键词 | SCIATIC-NERVE BLOCK ; POSTOPERATIVE PAIN RELIEF ; CUTANEOUS ANALGESIA ; LOCAL-ANESTHETICS ; SIZE DISTRIBUTION ; BUPIVACAINE ; RELEASE ; RAT ; INHIBITION ; LEVOBUPIVACAINE |
| 资助项目 | National Key Technology Program[2017ZX09201004014] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| 出版者 | ELSEVIER |
| WOS记录号 | WOS:000772831700004 |
| 资助机构 | National Key Technology Program |
| 源URL | [http://ir.ipe.ac.cn/handle/122111/52449]  |
| 专题 | 中国科学院过程工程研究所 |
| 通讯作者 | Zhang, Youhong; Wei, Yi; Ma, Guanghui |
| 作者单位 | 1.Wuhan Inst Technol, Sch Environm Ecol & Bioengn, East Lake New Technol Dev Zone, 206 Guanggu 1st Rd, Wuhan 430074, Peoples R China 2.Chinese Acad Sci, Inst Proc Engn, State Key Lab Biochem Engn, Beijing 100190, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yuan, Miaomiao,Na, Xiangming,Liu, Jingxuan,et al. Preparation, characterization and in vivo efficacy evaluation of ropivacaine O/W emulsion by premix membrane emulsification[J]. COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS,2022,640:9. |
| APA | Yuan, Miaomiao,Na, Xiangming,Liu, Jingxuan,Zhang, Youhong,Wei, Yi,&Ma, Guanghui.(2022).Preparation, characterization and in vivo efficacy evaluation of ropivacaine O/W emulsion by premix membrane emulsification.COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS,640,9. |
| MLA | Yuan, Miaomiao,et al."Preparation, characterization and in vivo efficacy evaluation of ropivacaine O/W emulsion by premix membrane emulsification".COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS 640(2022):9. |
入库方式： OAI收割
来源：过程工程研究所
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