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Preparation of novel ropivacaine hydrochloride-loaded PLGA microspheres based on post-loading mode and efficacy evaluation
Wen, Kang1,2; Na, Xiangming1,2; Yuan, Miaomiao1,3; Bazybek, Nardana1,2; Li, Xun1,2; Wei, Yi1; Ma, Guanghui1,2
2022-02-01
Source PublicationCOLLOIDS AND SURFACES B-BIOINTERFACES
ISSN0927-7765
Volume210Pages:8
AbstractLow 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.
Keywordropivacaine hydrochloride microspheres self-healing sciatic nerve blockade model
DOI10.1016/j.colsurfb.2021.112215
Language英语
WOS KeywordSELF-HEALING ENCAPSULATION ; DRUG-DELIVERY SYSTEMS ; LOCAL-ANESTHETICS ; RELEASE ; DEXMEDETOMIDINE ; BUPIVACAINE ; BLOCK
Funding ProjectNational Key Technology Program[2017ZX09201004014]
WOS Research AreaBiophysics ; Chemistry ; Materials Science
WOS SubjectBiophysics ; Chemistry, Physical ; Materials Science, Biomaterials
Funding OrganizationNational Key Technology Program
WOS IDWOS:000734889800001
PublisherELSEVIER
Citation statistics
Document Type期刊论文
Identifierhttp://ir.ipe.ac.cn/handle/122111/51547
Collection中国科学院过程工程研究所
Corresponding AuthorWei, Yi; Ma, Guanghui
Affiliation1.Chinese Acad Sci, Inst Proc Engn, State Key Lab Biochem Engn, Beijing 100190, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
3.Wuhan Inst Technol, Wuhan 430205, Peoples R China
Recommended Citation
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.
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