An Investigation on Enhancement of Solubility of 5 Fluorouracil by Applying Complexation Technique- Characterization, Dissolution and Molecular-Modeling Studies

Kavitha, K.; Srinivasa Rao, A.; Nalini, C. N.
March 2013
Journal of Applied Pharmaceutical Science;Mar2013, Vol. 3 Issue 3, p162
Academic Journal
The drug 5 fluorouracil is sparingly soluble in water. The aqueous solubility and dissolution rate of 5-fluorouracil can be increased by inclusion complexation with ß-cyclodextrin. Molecular-modeling studies support the formation of stable molecular inclusion complexation of 5-fluorouracil with ß-cyclodextrin monomer (1:1). Complexes were prepared by physical mixture, kneading, co evaporation and freeze drying methods. Two ratios 1:1 and 1:2 were formulated. These eight complexes were subjected to Phase-solubility study, molecular modeling and dissolution study. The complexes formed were confirmed by DSC studies. Phase solubility profile indicated that the solubility of 5-fluorouracil increased in the presence of ß-cyclodextrin monomer. Results obtained by different characterization techniques clearly indicate that the freeze-drying method leads to formation of solid state complexes between 5-fluorouracil and ß-cyclodextrin. The complexation of 5-fluorouracil with ß- cyclodextrin lends an ample credence for better therapeutic efficacy.


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