Abstract

FORMULATION AND EVALUATION OF MICROPARTICLES FORMED BY AMPHIPHILLIC CRYSTALLIZATION TECHNIQUE: OPTIMIZATION OF PROCESS PARAMETER

Ujwala S. Desai*, Dhaval B. Bhavsar

Abstract

The objective of the current work was to develop a crystallization process for the production of microparticles of aceclofenac with a controlled particle size distribution (PSD) to enhance its solubility. The strategy of increasing the in vitro dissolution has the potential to enhance the oral bioavailability when using nanosized crystalline drugs. Solvation of aceclofenac in aqueous poly(ethylene glycol) 400 (PEG 400) was investigated using UV spectroscopy and FTIR. Aceclofenac was crystallized from PEG 400 solutions by the addition of water under a variety of conditions of supersaturation and stirring speed. The crystals were filtered, dried at room temperature. A logarithmic increase in solubility of aceclofenac was observed with increasing concentration of PEG 400 in water enabling the aqueous antisolvent crystallization of aceclofenac from PEG. A central composite design, study showed the particle size to decrease with increasing supersaturation. The physicochemical properties of pure drug and microparticles were characterized by X-ray powder diffraction (XRPD), Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetric (DSC), scanning electron microscopy (SEM) as well as, measuring the particle size. The DSC and XRPD results indicated that this process did not affect the intrinsic crystalline properties of drug. Amphiphilic crystallization provided a novel method to produce microparticles of aceclofenac with a controlled size range.

Keywords: Aceclofenac, microparticles, amphiphillic crystallization, particle size, solubility, dissolution rate.