FORMULATION AND EVALUATION OF POORLY SOLUBLE ETRAVIRINE BY SPRAY DRYING METHOD
Keywords:Etravirine, Spray drying method, Soluplus, Povidone, Amorphous form
Objective: Current research work deals with the enhancement of solubility and dissolution of Poorly soluble Etravirine, which is belongs to BCS class-IV by Spray drying method (SD), which has been found to be the most widely used method in enhancing the solubility and rate of dissolution of poorly soluble drug substances.
Methods: Etravirine is belongs to BCS class-IV. It is insoluble in water and practically insoluble across the pH range of 1 - 6.8 of the major concerns with the Etravirine is its poor solubility, which results into poor bioavailability after oral administration. SD method has been proven to be an efficient method for conversion of poorly soluble crystalline polymorphic form into highly soluble amorphous form and make it useful for formulating lab scale batches to commercial batches. Hence, Spray drying method was chosen for converting poorly soluble crystalline form of Etravirine into highly soluble amorphous form using various carriers like Soluplus and Povidone (drug to polymer in 1:2 and 2:1 ratios) to increase its aqueous solubility and rate of drug release.
Results: There is almost 4 fold and 15 fold increases in the solubility of Etravirine prepared by SD as compared with Etravirine (crystalline form) in purified water and in pH 6.8 Phosphate buffer, respectively. From the characterization of spray dried powder of SD4 by Fourier Transform Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Powder X-ray diffraction (p-XRD), Scanning electron microscopy (SEM) concluded that crystalline Etravirine has been converted into an amorphous form. Faster and high drug release was found in the formulation of SD4.
Conclusion: The obtained results suggested that Spray drying method might be an efficacious approach for converting poorly soluble crystalline polymorphic form into highly soluble amorphous form and ultimately results in enhancing the therapeutic potential of Etravirine.
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