Preparation and Evaluation of Dapsone Nanoparticles

Abstract

Objective: Preparation of Dapsone nanoparticles to get optimized solubility, rate of dissolution and then more bioavailability.Methods: Dapsone nanoparticles were prepared using solvent-antisolvent precipitation method. A Certain amount of drug was dissolved in water-miscible solvent (ethanol or methanol), then this solution was injected at certain speed (ml/min.) into water containing stabilizer. Upon injection, precipitation of Dapsone nanoparticles will occur immediately accompanied with stirring for 30 min. at 50˚C, and then the selective formula is lyophilized. Different formulas of Dapsone nanoparticles were prepared at different polymer types, drug: polymer ratios and different organic solvent types. Characterization of these formulas involve measurement of particle size, particle morphology, saturation solubility, release profile, crystallinity, physical and chemical compatibilities between the drug and involved stabilizers. Results: Results show that the best formula of nanoparticle (F3) prepared by dissolving 16.6 mg/ml of Dapsone in ethanol, then 3ml was injected into to a 25 ml of water with PVP (polyvinyl pyrrolidone) as a stabilizer at ratio 1:4 (drug: stabilizer) then lyophilized to obtain nanoparticles. The best formula characterized by particle size around 28.5 nm, poly-dispersity (= 0.009), specific surface area (= 78.18), without physical or chemical incompatibility, and the dissolution rate was significantly higher than that of the raw Dapsone powder.