PolyMorphine: An innovative biodegradable polymer drug for extended pain relief

JOURNAL OF CONTROLLED RELEASE

卷:162

Article

Rosario-Melendez, Roselin¹  Harris, Carolyn L.^2,3  Delgado-Rivera, Roberto¹  Yu, Lei^2,3  Uhrich, Kathryn E.¹ 

[1] Rutgers State Univ, Dept Chem & Chem Biol, Piscataway, NJ 08854 USA

[2] Rutgers State Univ, Dept Genet, Piscataway, NJ 08854 USA

[3] Rutgers State Univ, Ctr Alcohol Studies, Piscataway, NJ 08854 USA

关键词: Morphine;    Biodegradable;    Polymer;    Extended release;    Pain treatment;    Prodrug;   

DOI  :  10.1016/j.jconrel.2012.07.033

来源: Elsevier

【 摘 要 】

Morphine, a potent narcotic analgesic used for the treatment of acute and chronic pain, was chemically incorporated into a poly(anhydride-ester) backbone. The polymer termed PolyMorphine, was designed to degrade hydrolytically releasing morphine in a controlled manner to ultimately provide analgesia for an extended time period. PolyMorphine was synthesized via melt-condensation polymerization and its structure was characterized using proton and carbon nuclear magnetic resonance spectroscopies, and infrared spectroscopy. The weight-average molecular weight and the thermal properties were determined. The hydrolytic degradation pathway of the polymer was determined by in vitro studies, showing that free morphine is released. In vitro cytocompatibility studies demonstrated that PolyMorphine is non-cytotoxic towards fibroblasts. In vivo studies using mice showed that PolyMorphine provides analgesia for 3 days, 20 times the analgesic window of free morphine. The animals retained full responsiveness to morphine after being subjected to an acute morphine challenge. (C) 2012 Elsevier B. V. All rights reserved.

【 授权许可】

Free