PREPARATION, CHARACTERIZATION AND IN VITRO DRUG RELEASE OF POLY (LACTIC-CO-GLYCOLIC ACID) MICROSPHERES LOADED WITH 5-FLUOROURACIL

5-Fluorouracil (5-FU) is one of the most commonly used anti-cancer drugs to treat colorectal, breast, gastric, pancreatic and skin cancer. The clinical application in humans, however, is restricted because of its fast metabolism, short biological half-life, systemic toxicity, and lack of selectivity towards tumor tissues. PLGA microspheres have been a focus of considerable interest for using as biodegradable drug delivery systems that deliver a sustained and controlled release of drugs. In the present research, 5-FU loaded PLGA microspheres have been prepared by a double emulsion solvent evaporation (W/O/W) method. The prepared microspheres were subjected to particle size analysis, scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray diffraction (XRD), encapsulation efficiency, drug loading and in vitro drug release studies. The prepared microspheres were found to have spherical shape with smooth surfaces and average sizes of 18-42 µm. Both the encapsulation efficiency of the drugs ranged from 55% to 76%, which depended on the polymer concentration. An in vitro release study showed an initial burst release, followed by a sustained release for 10 days. The drug release was found to be in good correlation with Higuchi diffusion kinetics (R² > 0.98). The results show that PLGA microspheres are potential carriers for the sustained delivery of 5-FU.