ABSTRACT

In this study, solid dispersion (SD) techniques were used to enhance sorafenib (SFN) dissolution and bioavailability. Three different methods were used to prepare the sorafenib SD formulation. The formulations were evaluated for pre-formulation studies, solubility studies, percent practical yield, percent drug content, and in-vitro release. In addition to FTIR, XRD, SEM, and stability studies, the best formulation based on drug release was further characterized. For formulations prepared by surface solid dispersion (SSD1-SSD15), melt granulation (SD1-SD14), or liquid solid compact (LSC1-LSC14), greater than 90% solubility within one hour was reported with comparison to pure drug. Among different formulations of sorafenib, the LSC14 formulation had the best drug release of 99.94 percent, prepared by the liquisolid compact technique. FTIR analysis indicates no noteworthy interaction among the drug and excipients. The XRD and SEM images results indicated the conversion of sorafenib from crystalline to amorphous state on LSC formulation. Stability studies proved that formulation was stable for 3 months. The in vivo bioavailability studies conducted in rats indicate that Cmax of the sorafenib SD (25.76±1.22 ng/ml) was significant (p<0.05) as compared to pure suspension (7.25±1.75 ng/ml). The Tmax of LSC14 and pure drug was 1.0±0.05 and 1.5±0.2 h, respectively. AUC0-? infinity for sorafenib LSC14 was higher (103.61±1.05 ng.h/ml) than the pure drug suspension 32.4±1.72 ng.h/ml indicating that the optimised formulation was significantly higher (p<0.05) as compared to drug suspension formulation. Keywords: Sorafenib, Tumour, Solid Dispersions, Solubility, Liquisolid Compact, bioavailabity studies
Publication date: 25/09/2021

https://ijbpas.com/pdf/2021/September/MS_IJBPAS_2021_SEPT_SPCL_1044.pdf

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https://doi.org/10.31032/IJBPAS/2021/10.9.1044