Fabrication and Properties of Gelatin/Chitosan Microspheres Loaded with 5-Fluorouracil

Abstract

The use of microspheres as drug delivery vehicles for anticancer therapeutics has great potential to revolutionize the future of cancer therapy. The present paper describes the influence of process variables on the encapsulation and loading efficiency of 5-Fluorouracil (5-FU) in gelatin/chitosan (Gel/Cs) microspheres. The influences of preparation parameters, including the contents of the emulsifier Span-80, the cross-linking agent and 5-FU, and the stirring speed, on drug loading and encapsulation efficiency of the microspheres were investigated. The experimental results indicated that drug loading and encapsulation efficiency of microspheres increased with increasing concentration of the cross-linking agent; and then decreased when the concentration of the cross-linking agent was higher than 0.3 ml·g⁻¹ of Gel/Cs. Drug loading and encapsulation efficiency increased with increasing concentration of Span-80; they reached the maximum value when the concentration of the emulsifier was 0.012 g·ml⁻¹. The loading and encapsulation efficiency of the microspheres also increased with increasing stirring speed. In addition, drug loading and encapsulation efficiency increased with increasing concentration of 5-FU; however, the encapsulation efficiency decreased when the concentration of 5-FU was higher than 40 mg·ml⁻¹.

Keywords:

• chitosan
• encapsulation efficiency
• gelatin
• loading efficiency
• microspheres
• 5-FU

Acknowledgments

This work was financially supported by the National Natural Science Fund of China (No. 51273062), Hunan Provincial Natural Science Foundation of China (No. 12JJA003), the Scientific Research Fund of Hunan Provincial Education Department (No. 11B045) and the Aid Program for Science and Technology Innovative Research Team in Higher Educational Institutions of Hunan Province.