Preparation and Evaluation of Oral Microsponge Drug Delivery System of Ketoconazole

Abstract

Abstract:In oral applications, the microsponge system has been shown to increase the rate ofsolubilization of poorly water-soluble drugs by entrapping such drugs in the microspongesystem's pores.Because these pores are very small, the drug is in effect reduced tomicroscopic particles and increased surface area thus greatly increases the rate ofsolubilization.This investigation was done to increase solubility and then bioavialibility of poorlysoluble ketoconazole (BCS class II drug) by preparing it as microsponges by quasi emulsionsolvent technique using different types of Eudragits as Eudragit E 100, Eudragit RS orEudragi tRL. Physicochemical interaction between drug and excipients as individual one,physical mixture and prepared microsponge has been evaluated using Fourier transforminfrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) which indicates theabsence of interaction between them. The1: 0.1 ratio drug: Eudragit E 100 at stirring rate of2000 rpm (F1b) was found to give the best production yield of 80.46±2.41, entrapmentefficiency of 70.84%±1.71, and smallest particle size of 57.42±2.26 μm. Scanning electronmicroscopy of F1b at magnification of 1000x and 50000x shows the presence of drug asnanocrystals inside microsponge. All prepared formulas shows good flow properties indicatedthe possibility of capsule formulation which show significant (P<0.05) high drug releasepercent in 0.1 HCl compared with traditional Nizoral® oral tablet (83.15%±1.10) but EudragitE (F1b ) shows the best drug release percent of 100±0.91 at 20 minutes. Finally, the overallobtained data revealed the feasibility of preparing fast release ketaconazole as microspongesin oral capsules dosage form.