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

(E-pub Ahead of Print)

Author(s): Hanmei Li , Yuling Xu, Yuna Tong, Yin Dan, Tingting Zhou, Jiameng He, Shan Liu*, Yuxuan Zhu*.

Journal Name: Current Drug Delivery

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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. 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. 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. 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, pharmacokinetic analysis, injectable sucrose acetate isobutyrate (SAIB)

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(E-pub Ahead of Print)
DOI: 10.2174/1567201816666181119112952
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