Aceclofenac delivery by microencapsulation using LBL self-assembly for delayed release

ABSTRACT

Colonic targeting has gained increasing interest over the past years, not just for the transport of drugs for the treatment of local diseases associated with the colon but also for its potential for transporting peptides and proteins, particularly low molecular weight peptide drugs. Without protection, such peptide drugs are usually digested within the gastric and small intestinal sections. In the present work Layer-By-Layer [LBL] self-assembly was utilized to make Aceclofenac single bilayer microcapsules produced by sequential adsorption of positively charged chitosan and negatively charged Pectin on the external surface of negatively charged Aceclofenac microcrystals. Taguchi approach was applied to determine the best concurrence of composition factors that is concentration of chitosan, pectin, centrifugation speed and incubation time. The microcapsules were characterized for encapsulation efficiency, particle size, zeta potential, scanning electron microscopy and in-vitro release kinetics. Surface electric potential of Aceclofenac microcrystals was found to be negative with zeta potential -1.39 mV, in acetate buffer of pH 4. The primary and the secondary deposit layer of chitosan and pectin was found to have a positive and negative charge with zeta potential of +5.57 mV and -22.8 mV respectively. The sequential changing of surface zeta potential after each deposition is a satisfactory indication of the LBL self-assembly of the oppositely charged polyelectrolytes. The average size and encapsulation efficiency of the optimized single bilayer microcapsules [F5] was found to be 20microm and 63.83%, respectively. The ex-vivo percentage cumulative drug release of [F5] in Phosphate buffer pH 6.8 containing 2-4% w/v colonic fecal matter of male albino rat was found to be 98.40%. The optimized batch of microcapsules showed first order release kinetics [R[2]= 0.950] in presence of colonic fecal matter