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| Novel insights on the encapsulation mechanism of PLGA terminal groups on ropivacaine | |
Li, Xun1,2; Wei, Yi1 ; Wen, Kang1,2; Han, Qingzhen3; Ogino, Kenji4; Ma, Guanghui1
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| 2021-03-01 | |
| Source Publication | EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
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| ISSN | 0939-6411 |
| Volume | 160Pages:143-151 |
| Abstract | Currently, the influences of free terminal groups (hydroxyl, carboxyl and ester) of PLGA on encapsulating active pharmaceutical ingredient are relatively ambiguous even though PLGA types were defined as critical quality attributes in vast majority of design of experiment process. In this study, emulsion method combined with premix membrane emulsification technique has been used to encapsulate ropivacaine (RVC), a small molecule local anesthetic in clinical. Based on the narrow particle size distribution, the influences and mechanisms of the terminal groups on properties of ropivacaine loaded microspheres have been investigated in detail. It was found that microspheres prepared by PLGA with hydroxyl or ester groups exhibited lower encapsulation efficiency but faster in vitro release rate than that of carboxyl groups. In the meanwhile, on microcosmic level analysis by quartz crystal microbalance with dissipation, atomic force microscope and confocal laser scanning microscopy, we attributed this distinction to the specific interaction between ropivacaine and different terminal groups. Subsequently, the reaction activation centers were verified by density functional simulation calculation and frontier molecular orbital theory at molecular level. Additionally, pharmacokinetics and pharmacodynamic research of infiltration anesthesia model were performed to compare sustained release ability, duration and intensity of the anesthetic effect in vivo. Finally, potential safety and toxicity were evaluated by the biochemical analysis. This study not only provides a novel mechanism of drug encapsulation process but also potential flexible selections in terms of various anesthesia indications in clinical. |
| Keyword | Terminal groups Ropivacaine Specific interactions Pharmacokinetics Pharmacodynamic |
| DOI | 10.1016/j.ejpb.2021.01.015 |
| Language | 英语 |
| Funding Project | National Key Technology Program[2017ZX09201004014] ; National Natural Science Foundation of China[21336010] ; National Key Research and Development Program of China[2017YFC0210303] |
| WOS Research Area | Pharmacology & Pharmacy |
| WOS Subject | Pharmacology & Pharmacy |
| Funding Organization | National Key Technology Program ; National Natural Science Foundation of China ; National Key Research and Development Program of China |
| WOS ID | WOS:000620605900005 |
| Publisher | ELSEVIER |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.ipe.ac.cn/handle/122111/43635 |
| Collection | 中国科学院过程工程研究所 |
| Corresponding Author | Wei, Yi; Ma, Guanghui |
| Affiliation | 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.Chinese Acad Sci, Inst Proc Engn, Res Dept Environm Technol & Engn, State Key Lab Multiphase Complex Syst, Beijing 100190, Peoples R China 4.Tokyo Univ Agr & Technol, Grad Sch Bioapplicat Syst Engn, Koganei, Tokyo 1848588, Japan |
| Recommended Citation GB/T 7714 | Li, Xun,Wei, Yi,Wen, Kang,et al. Novel insights on the encapsulation mechanism of PLGA terminal groups on ropivacaine[J]. EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS,2021,160:143-151. |
| APA | Li, Xun,Wei, Yi,Wen, Kang,Han, Qingzhen,Ogino, Kenji,&Ma, Guanghui.(2021).Novel insights on the encapsulation mechanism of PLGA terminal groups on ropivacaine.EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS,160,143-151. |
| MLA | Li, Xun,et al."Novel insights on the encapsulation mechanism of PLGA terminal groups on ropivacaine".EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS 160(2021):143-151. |
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