The present study was aimed at the overall improvement in the efficacy, reduction in toxicity and enhancement of therapeutic index of 5-fluorouracil. Magnetically responsive biodegradable microparticulate delivery system of 5-fluorouracil has been developed by phase separation emulsion polymerization technique by using bovine serum albumin. The formulations were evaluated with respect to particle size analysis, entrapment efficiency, magnetite content, in-vitro magnetic responsiveness, in-vitro drug release studies, in-vivo drug targeting studies and stability studies. The formulated magnetic microspheres were found to be spherical with average particle size of 3-12 µm in diameter and incorporation efficiency up to 56.37. Result of X-ray diffractrometry confirmed the presence of magnetite in prepared 5-fluorouracil magnetic microspheres. The total percentage of Fe2O3 in the microspheres was found to be 42.53 to 55.48. In-vitro drug release after 24 hours was 89.60, 82.22, 78.41 and 76.35 for formulation F1, F2, F3 and F4 respectively. Results of in-vitro magnetic responsiveness and in-vivo tissue targeting proved that the retention of microspheres in presence of magnetic field was significantly high than those in the absence of the magnetic field. Stability studies revealed that 4°C is the most suitable temperature for storage of 5-fluorouracil loaded magnetic microspheres. Overall, this study shows that the magnetic albumin microspheres can be retained at their target site in-vivo, following the application of magnetic field and are capable of releasing their drug content for an extended period of time.
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