Development, Optimization, and Characterization of Melt Sonocrystallized Agglomerates of BCS Class II Drug

Abstract

The objective of this study was to improve the drug's solubility, dissolution rate, and processability properties. The selected BCS Class II drug, Valsartan, is widely employed in the treatment of hypertension; however, its limited solubility has posed significant challenges to its therapeutic efficacy. The melt sonocrystallization (MSC) technique was adopted, utilizing a probe ultra sonicator, with the sonication time (1, 2, and 3 minutes) and amplitude level (60%, 70%, and 80%) varied through a 32factorial design. Successful preparation of MSC agglomerates of Valsartan was achieved, exhibiting satisfactory yield and drug content. Evaluation of the MSC agglomerates exhibited significant enhancements in solubility and drug release compared to the pure valsartan. These improvements were attributed to the formation of porous agglomerates, resulting in improved micrometric properties. Complementary analysed through DSC and X-ray Diffraction confirmed a reduction in drug crystallinity with the increase in sonication time and amplitude. Moreover, FT-IR investigations verified the chemical stability of valsartan during the MSC process, ensuring the preservation of its chemical integrity. In conclusion, this study highlights the promising potential of melt sonocrystallization as a cost-effective approach to enhance the solubility, dissolution rate, and processability of BCS Class II drugs, exemplified by valsartan. The comprehensive insights provided herein offer valuable contributions to pharmaceutical formulation practices, potentially leading to optimized therapeutic efficacy and bioavailability of poorly water-soluble drugs.

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