Preparation, characterization and in silico modeling of biodegradable nanoparticlescontaining cyclosporine A and coenzyme Q10

Abstract

Combination therapy will soon become a reality, particularly for those patientsrequiring poly-therapy to treat co-existing disease states. This becomes all the moreimportant with the increasing cost, time and complexity of the drug discovery processprompting one to look at new delivery systems to increase the efficacy, safety andpatient compliance of existing drugs. Along this line, we attempted to designnano-scale systems for simultaneous encapsulation of cyclosporine A (CsA) andcoenzyme Q10 (CoQ10) and model their encapsulation and release kinetics. Thein vitro characterization of the co-encapsulated nanoparticles revealed that thesurfactant nature, concentration, external phase volume, droplet size reduction methodand drug loading concentration can all influence the overall performance of thenanoparticles. The semi-quantitative solubility study indicates the strong influence ofCoQ10 on CsA entrapment which was thought to be due to an increase in thelipophilicity of the overall system. The in vitro dissolution profile indicates the influenceof CoQ10 on CsA release (64%) to that of individual particles of CsA, wherethe release is faster and higher (86%) on 18th day. The attempts to model theencapsulation and release kinetics were successful, offering a possibility to use suchmodels leading to high throughput screening of drugs and their nature, aloneor in combination for a particular polymer, if chi-parameters are understood.