FORMULATION AND OPTIMIZATION OF SOLID SELF-NANOEMULSIFYING SYSTEM USING POROUS CARRIERS FOR ORAL DELIVERY OF CINNARIZINE
Keywords:
Pseudo-ternary phase diagram, Self-nanoemulsion, Porous carriers, Bioavailability studyAbstract
Objective: The present study aims to utilize the nanotechnology technique to formulate the Cinnarizine (CNZ) in the form of solid self-nano emulsifying system to enhance the dissolution and hence the bioavailability.
Methods: Screening study for solubility of CNZ in different vehicles was carried out. The selected system was optimized for saturated solubility, globule size, zeta potential, polydispersity index (PDI) and self-emulsification time. The solidified nanoemulsion was prepared using; Aeroperl 300, Aerosil 200, hydrophilic nanosilica and Neusilin US2 as porous carrier materials. The compressed CNZ tablets were evaluated regarding their physicochemical characteristics, in-vitro release, and bioavailability study.
Results: Self nano-emulsifying system composed of Labrafil (oil), tween 80 (surfactant), and transcutol (cosurfactant) was successfully developed with a droplet size range of 11.37-92.58 nm. The in-vitro release results revealed that the developed formulation improved the release of CNZ and enhanced the bioavailability in the rabbits (190%) more than the commercial product (Stugeron® tablets).
Conclusion: Solid self-nano-emulsifying system of CNZ was successfully developed by different ratios of Labrafil (oil), tween 80 (surfactant), transcutol (cosurfactant) and solidified by the adsorption on hydrophilic nano silica and the optimized formula could be expected to increase and improve the bioavailability of CNZ.
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