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Sucrose Acetate Isobutyrate as an In situ Forming Implant for Sustained Release of Local Anesthetics

[ Vol. 16 , Issue. 4 ]

Author(s):

Hanmei Li, Yuling Xu, Yuna Tong, Yin Dan, Tingting Zhou, Jiameng He, Shan Liu* and Yuxuan Zhu*   Pages 331 - 340 ( 10 )

Abstract:


Objective: In this study, an injectable Sucrose Acetate Isobutyrate (SAIB) drug delivery system (SADS) was designed and fabricated for the sustained release of Ropivacaine (RP) to prolong the duration of local anesthesia.

Methods: By mixing SAIB, RP, and N-methyl-2-pyrrolidone, the SADS was prepared in a sol state with low viscosity before injection. After subcutaneous injection, the pre-gel solution underwent gelation in situ to form a drug-released depot.

Result: The in vitro release profiles and in vivo pharmacokinetic analysis indicated that RP-SADS had suitable controlled release properties. Particularly, the RP-SADS significantly reduced the initial burst release after subcutaneous injection in rats.

Conclusion: In a pharmacodynamic analysis of rats, the duration of nerve blockade was prolonged by over 3-fold for the RP-SADS formulation compared to RP solution. Additionally, RP-SADS showed good biocompatibility in vitro and in vivo. Thus, the SADS-based depot technology is a safe drug delivery strategy for the sustained release of local anesthetics with long-term analgesia effects.

Keywords:

In situ-forming implant, sucrose acetate isobutyrate, ropivacaine, sustained release, biocompatibility, drug.

Affiliation:

College of Pharmacy and Biological Engineering, Chengdu University, Chengdu 610106, College of Pharmacy and Biological Engineering, Chengdu University, Chengdu 610106, Department of Nephrology, The Third People's Hospital of Chengdu, Chengdu, 610031, College of Pharmacy and Biological Engineering, Chengdu University, Chengdu 610106, College of Pharmacy and Biological Engineering, Chengdu University, Chengdu 610106, College of Pharmacy and Biological Engineering, Chengdu University, Chengdu 610106, Department of Laboratory Medicine, Affiliated Hospital of University of Electronic Science and Technology, Sichuan Academy of Medical Sciences and Sichuan Provincial People's Hospital, Chengdu 610072, Personalized Drug Therapy Key Laboratory of Sichuan Province, Sichuan Academy of Medical Science & Sichuan Provincial People’s Hospital, University of Electronic Science and Technology of China, Chengdu 610072

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