Development of Temozolamide Solid Lipid Nanoparticles: Formulation, in vitro characterization and invivo pharmacokinetic studies in animals

Abstract

In this work, water-soluble prodrugs with reduced T1/2 were encapsulated into nanobeads via surfactant polymer ionic-gelation cross linking and targeted to the colon using Eudragit-S-100. FT-IR, DSC were used to characterise Capecitabine and nanobeads. Zeta Sizer, SEM, Drug loading, Entrapment efficiency, in-vitro and in-vivo pharmacokinetic investigations described Capecitabine nanobeads. The weight fluctuation, hardness, and friability of Capecitabine nanobead tablets were tested. The optimization of formulation and process variables by 23 factorial design using Expert-Design software shows that increasing the speed of the Hi-Speed Homogenizer (a process variable) decreases the size of the Capecitabine nanobeads. The concentration of Calcium chloride (Cacl2 percent, a formulation variable) also affects the size of the beads, and 3 percent Cacl2 is the best concentration for preparing Capecitabine nanobeads. Capecitabine and nanobeads' physicochemical properties were confirmed. DSC showed that Capecitabine and polymers were compatible, and the medication was somewhat amorphous and distributed in polymer matrix. Characterization of Capecitabine nanobeads characteristics showed that F2 is superior to F1 and F3.