Sivakumar S. Moni*, Mohammad F. Alam*, Mohammed M. Safhi , Muhammad H. Sultan, Hafiz A. Makeen and Mohamed E. Elmobark Pages 659 - 666 ( 8 )
Background: Sorafenib is the first oral therapeutic agent to show the activity against human hepatocellular carcinoma. Sorafenib leads to severe toxicity due to the multiple-dose regimen. Reducing the overall dose of sorafenib through injectable dosage form to release sustainably is of therapeutically more important to combat drug-induced toxicity.
Objective: The purpose of this study was to formulate and evaluate the physical parameters of sorafenib- loaded Sodium Selenite Nanoparticles (SSSNP).
Methods: Two different methods: chemical crosslinking and solvent evaporation were applied for the formulation of nanoparticles using various crosslinkers such as formaldehyde, magnesium sulfate, tripolyphosphate, dextran sulfate, and aluminum hydroxide. Physical characterization was performed with zeta potential analysis, polydispersity index, particle size and scanning electron microscopic studies for morphological analysis for all the formulated nanoparticles developed using the chemical crosslinking technique based ionic interaction.
Results: Tripolyphosphate was selected as an ideal crosslinker and used for nanoparticle formulation with the solvent evaporation technique. Based on the physical characterization, SSSNP was formulated successfully with the solvent evaporation technique using tripolyphosphate as a cross-linker. The zeta potential of SSSNP was -37.5 mV, PDI was approximately 0.3 to 0.4, and the observed size (diameter) was in the range of 208 nm to 0.2 μm. Furthermore, the particles were smooth in morphology and appeared as crystals.
Conclusion: The novel injectable sorafenib loaded sodium selenite nanoparticle dosage form will serve better than conventional oral dosage form to elicit a safe therapeutic effect.
Hepatoma, sorafenib, sodium selenite, nanoparticles, formulation and development, physical characterization.
Department of Pharmaceutics, College of Pharmacy, Jazan University, Jazan, Department of Pharmacology and Toxicology, College of Pharmacy, Jazan University, Jazan, Department of Pharmacology and Toxicology, College of Pharmacy, Jazan University, Jazan, Department of Pharmaceutics, College of Pharmacy, Jazan University, Jazan, Pharmacy Practice Research Unit, Clinical Pharmacy Department, Faculty of Pharmacy, Jazan University, Department of Pharmaceutics, College of Pharmacy, Jazan University, Jazan