Development of Formulation and Evaluation of Niosomal Drug Delivery System for Improved Anti Cancer Activity

Abstract

Niosomal formulations containing 5- Fluorouracil and leucovorin were successfully prepared with different surfactants like Span 40, Span 60, Tween 40 and Tween 60 by thin film hydration technique. The evaluation parameters revealed that 5-Fluorouracil and leucovorin niosomes shows reduced particle size distribution with better entrapment efficiency. Niosomes has negative surface charges which indicate excellent stability. In vitro release of 5-Fluorouracil and Leucovorin from niosomes was carried out. Formulation F4 was shown better sustained release among other formulations. In vitro release kinetics study was done for formulation F4 to find out the release mechanism. The release of 5-FU from niosomal formulation follow Non Fickian type diffusion, whereas release LV from niosomal formulations follows Fickian diffusion mechanism. The result suggests that niosomal formulation can provide consistent and prolonged release of the entrapped drug molecules. Niosomal delivery system can provide sustained action of the entrapped drug and reduce the side effects associated with frequent administration of the drug and potentiate the therapeutic effects of the drug. Further, preclinical evaluation of prepared 5-FU+ LV niosomes displayed efficient anticancer potential in DMH induced colon cancer by restoration of altered biochemical levels. Furthermore, 5-FU+ LV niosomes displayed marked. IMPACT OF THE STUDY: Attempt has been made to incorporate 5-Fluorouracil and Leucovorin niosomes in blend of surfactants to provide sustained release of the entrapped drug for colon delivery system. The niosomes designed and prepared in the current study elicits reduced particle size distribution with marked entrapment efficiency. Further, the prepared niosomes displayed better sustained release as that of the marketed formulation containing 5-FU+LV and 5-FU alone. The highlights of the study, was the marked anti-colon cancer activity exhibited by the 5-FU+LV niosomes in a preclinical model as that of the market formulation 5-FU+LV and 5-FU alone.