Improvement of the solubility and dissolution of ketoprofen using natural bile salts

The aim of this work was to improve the solubility and dissolution of the poorly water soluble ketoprofen(KP) using natural solubilizers, The physical mixture(PM) and lyophilized solid dispersion(LSD) of drug were prepared using different carriers namely shark bile salts(S.B) , fresh water fish(Tilabia nilotica) bile salts(F) , polysorbate 80(P.S) and sodium lauryl sulphate(SLS) . The solubility and dissolution of KP in distilled water were investigated as a function of solubilizer concentration(0-3%w/w) in the prepared PMs and LSDs . In a concentration of 2%w/w solubilizer , the drug solubility and dissolution were improved dramatically. In LSDs the solubility increased from 14 mg/ml to 81 mg/ml and 63 mg/ml when using shark bile and polysorbate 80 respectively . Dissolution was found to be a function of solubility especially in case of natural solubilizers and polysorbate 80 . Simple and mixed micellar solubilization was the main mechanism suggested for the increased solubility and dissolution of the drug. Results were confirmed by surface tension measurements of the aqueous solution of the plain drug , its PM and LSD . DSC , IR and XRPD studies suggested possible interactions between KP and some of the used solubilizers. The results suggested that shark bile salts revealed promising technique in enhancing the solubility and dissolution of the poorly water soluble drugs as KP and application in the field of dosage form design in digestive therapy. The kinetic study revealed that , the drug release from all formulations followed zero order kinetics.

Author(s): Mohammed M. A. M. Nafady

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