Research Journal of Pharmacy and Technology

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Solid Dispersion Technique for Solubility Improvement of Ketoconazole for Vaginal Delivery


Affiliations
1 Department of Pharmaceutics, Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune, India
     

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The activity of any drug depends on bioavailability of drug. As biological barriers permit only dissolved molecules, it is essential to have sufficient solubility in biological fluid. Vaginitis is a very common gynecological problem in women of all age groups and mostly indicated as mixed vaginal infection. Ketoconazole is a topical antifungal drug used to treat vaginitis and has poor solubility (BCS class- II). In the present study, an attempt has been made to improve the solubility of ketoconazole by solid dispersions (SD) prepared by kneading and spray drying techniques using hydrophilic carrier; Soluplus, Poloxamer 188 and β-cyclodextrin. The SD prepared by soluplus with spray drying method exhibited higher solubility than those prepared by kneading method. SD was further characterized by FTIR, DSC, and XRD analysis. Fourier transform infrared spectroscopy study confirmed the formation of SD complex of ketoconazole and soluplus. Polymer entrapped the drug and formed amorphous state which was confirmed by DSC studies. The surface morphology of the SD by X-ray diffraction confirmed conversion of drug from crystalline form to amorphous. Conclusively, Soluplus looks to be a promising carrier to improve the solubility of poorly soluble drugs.

Keywords

Solid Dispersions, Kneading, Spray-Drying, Ketoconazole, Soluplus, Poloxamer 188, Β-cyclodextrin.
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  • Solid Dispersion Technique for Solubility Improvement of Ketoconazole for Vaginal Delivery

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Authors

J. G. Mahore
Department of Pharmaceutics, Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune, India
S. S. Deshkar
Department of Pharmaceutics, Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune, India
P. P. Kumare
Department of Pharmaceutics, Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune, India

Abstract


The activity of any drug depends on bioavailability of drug. As biological barriers permit only dissolved molecules, it is essential to have sufficient solubility in biological fluid. Vaginitis is a very common gynecological problem in women of all age groups and mostly indicated as mixed vaginal infection. Ketoconazole is a topical antifungal drug used to treat vaginitis and has poor solubility (BCS class- II). In the present study, an attempt has been made to improve the solubility of ketoconazole by solid dispersions (SD) prepared by kneading and spray drying techniques using hydrophilic carrier; Soluplus, Poloxamer 188 and β-cyclodextrin. The SD prepared by soluplus with spray drying method exhibited higher solubility than those prepared by kneading method. SD was further characterized by FTIR, DSC, and XRD analysis. Fourier transform infrared spectroscopy study confirmed the formation of SD complex of ketoconazole and soluplus. Polymer entrapped the drug and formed amorphous state which was confirmed by DSC studies. The surface morphology of the SD by X-ray diffraction confirmed conversion of drug from crystalline form to amorphous. Conclusively, Soluplus looks to be a promising carrier to improve the solubility of poorly soluble drugs.

Keywords


Solid Dispersions, Kneading, Spray-Drying, Ketoconazole, Soluplus, Poloxamer 188, Β-cyclodextrin.

References