Assessment of biodegradable controlled release rod systems for pain relief applications

Abstract

Control of chronic, severe pain is a difficult and important clinical problem for most patients, especially those with cancer. Although current applications are insufficient for a satisfactory solution to this problem, the rate of disease incidence is increasing worldwide, thus making the problem more apparent. Based on this fact, this study was designed with the ultimate goal of formulating a controlled release system of pain relievers, mainly opioids, for the local treatment of pain to achieve satisfactory, fast, and less side effect-related relief and to provide a better life status for chronic pain patients. Two copolymers of a biodegradable polymer poly(L-lactide-coglycolide) (PLGA) were used to prepare an implantable rod type drug release system containing either an analgesic or anesthetic type of pain reliever. In vitro drug release kinetics of these systems were studied. It was observed that release from PLGA 85 : 15 was more zero-order than it was from PLGA 50 :50. A zero-order release rate was obtained for codeine, hydromorphone, and bupivacaine from PLGA (85 :15) rods. They, however, were released from PLGA (50 :50) rods with Higuchi kinetics. The drug solubility was also influential on release rate, as shown by the zero-order morphine release from PLGA (50 :50) rods. Scanning electron micrographs (SEMs) of the monolithic rods revealed erosion of the rods and the removal of drug crystals from the rod structure.

Keywords:

• KEY WORDS
• PLGA
• MORPHINE
• HYDROMORPHONE
• CODEINE
• BUPIVACAINE
• CONTROLLED RELEASE
• POLYMERIC ROD