Osmotically balanced, large unilamellar liposomes that enable sustained bupivacaine release for prolonged pain relief in in vivo rat models.

ABSTRACT: To efficiently prolong analgesic effects, we developed osmotically balanced, large unilamellar liposomes (~ 6 μm in diameter) in which highly concentrated bupivacaine (up to 30 mg/mL) was encapsulated, and their sustained bupivacaine release was highly effective in relieving postoperative pain over 24 h in a rat model. Our reverse-phase evaporation method based on non-toxic alcohol, ethanol, enabled simple and cost-effective production of bupivacaine-loaded liposomes, of which osmotic pressure was readily balanced to improve the structural stability of the enlarged unilamellar liposomes along with extension of their shelf life (> a month). The in vitro release profile verified that the release duration of the bupivacaine-loaded liposomes extended up to 6 days. For the in vivo study, male S

SUBMITTER: Yoo H 

PROVIDER: S-EPMC8187397 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature