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Construction of injectable micron-sized polymorphic vesicles for prolonged local anesthesia with weekly sustained release of ropivacaine.
Tan, Xin; Ke, Peng; Chen, Ziying; Zhou, Yi; Wu, Linjie; Bao, Xiaoyan; Qin, Yaxin; Jiang, Ruolin; Han, Min.
Afiliación
  • Tan X; Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
  • Ke P; Department of Anesthesiology, Fujian Provincial Hospital, Fujian Shengli Clinical Medical College, Fujian Medical University, Fuzhou 350108, China.
  • Chen Z; Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
  • Zhou Y; National Narcotic Laboratory Zhejiang Regional Center, Hangzhou 310000, China.
  • Wu L; Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
  • Bao X; Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
  • Qin Y; Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
  • Jiang R; Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
  • Han M; Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China; Department of Radiation Oncology, Key Laboratory of Cancer Prevention and Intervention, The Second Afliated Hospital, College of Medicine, Zhejiang University, Hangzhou 310058, China; Hangzho
Int J Pharm ; 661: 124378, 2024 Aug 15.
Article en En | MEDLINE | ID: mdl-38925241
ABSTRACT
Currently, to overcome the short half-life of the local anesthetic ropivacaine, drug delivery systems such as nanoparticles and liposomes have been used to prolong the analgesic effect, but they are prone to abrupt release from the site of administration or have poor slow-release effects, which increases the risk of cardiotoxicity. In this study, injectable lipid suspensions based on ropivacaine-docusate sodium hydrophobic ion pairing (HIP) were designed to significantly prolong the duration of analgesia. The resulting ion-paired lipid suspension (HIP/LIPO) had a micrometer scale and a high zeta potential, which facilitates stable in situ retention. The strong interaction between docusate sodium and ropivacaine was verified using thermal and spectroscopic analyses, and the formation of micron-sized polymorphic vesicles was attributed to the mutual stabilizing interactions between ropivacaine-docusate sodium HIP, docusate sodium and lecithin. The HIP/LIPO delivery system could maintain drug release for more than 5 days in vitro and achieve high analgesic efficacy for more than 10 days in vivo, reducing the side effects associated with high drug doses. The stable HIP/LIPO delivery system is a promising strategy that offers a clinically beneficial alternative for postoperative pain management and other diseases.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Preparaciones de Acción Retardada / Liberación de Fármacos / Ropivacaína / Anestésicos Locales Límite: Animals Idioma: En Revista: Int J Pharm Año: 2024 Tipo del documento: Article País de afiliación: China Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Preparaciones de Acción Retardada / Liberación de Fármacos / Ropivacaína / Anestésicos Locales Límite: Animals Idioma: En Revista: Int J Pharm Año: 2024 Tipo del documento: Article País de afiliación: China Pais de publicación: Países Bajos