BioScience Trends. 2009;3(6):287-295. (DOI: )

Development of implants for sustained release of 5-fluorouracil using low molecular weight biodegradable polymers.

Hanafy AFH, El-Egaky AM, Mortada SA, Molokhia AM


SUMMARY

Anticancer drugs have poor efficacy especially against solid tumors that hinder drug penetration into the tumor. Thus, the dose has to be increased, but toxicity is a limiting factor. Local administration of a polymeric biodegradable poly-L-lactic acid (PLA) and poly(L-lactic acid-co-glycolic acid) copolymer (PLGA) implant containing an anticancer drug may be an acceptable method of concentrating the drug near the tumor site. This work sought to synthesize low molecular weight PLA and PLGA by polycondensation to yield polymers with good physical properties to make them suitable for use in implantable therapy. The synthesized polymers were characterized by determining their molecular weight, melting point, and percentage crystallinity using DSC. Fourier transformationinfra red spectrum (FT-IR), nuclear magnetic resonance (NMR) and specific optical rotation measurement were also used to characterize the synthesized polymers. Morphological characteristics were assessed using scanning electron microscopy (SEM). Implants were manufactured using compression (C) and injection molding (IM) and were loaded with 12 mg 5-fluorouracil (5-FU) per 120 mg implant. In vitro release patterns of all implants were assessed in phosphate buffered saline pH 7.4 (PBS 7.4) at 37


KEYWORDS: Poly-L-lactic acid (PLA), poly(L-lactic acid-coglycolic acid) copolymer (PLGA), 5-fluorouracil (5-FU), implants, injection molding, compression, dissolution

Full Text: