Solubility Enhancement of a Model Drug Quercetin by Nanotechnology Based Formulation Approach

Abstract

Approximately, 40% of drug candidates have poor water solubility and its oral delivery is frequently associated with implications of low bioavailability, hepatic first pass metabolism, enzymatic degradation, high intra- and inter subject variability, and lack of dose proportionality. Interests of solid lipid nanoparticles (SLN) to improve the oral bioavailability of such drugs (PWSD) are well known and documented in literature. Different batches of SLNs were prepared by emulsification-ultrasonication methods by changing process parameters, and finally on the basis of nanoparticle size, polydispersity index (PDI), zeta potential (ZP), encapsulation efficiency (EE), an optimum system was designed. The optimized formulation demonstrated particle size, polydispersity index, zeta potential and encapsulation efficiency; 327 nm, 0.118, 32.3 mV, and 57.9%, respectively. The optimized formulation has shown the highest zeta potential (-32.3. mV) confers its stability. In-vitro release of drug showed significant improvement in the release of quercetin from SLN formulation as compared to plain drug. Furthermore, quercetin-loaded SLN were found to be stable at 4 °C for 1 months of study period. The formulation was successfully prepared by proposed method that can be used as a potential carrier for successful delivery of poorly water-soluble drugs associated with poor oral bioavailability.