Preparation and Evaluation of Oral Microsponge Drug Delivery System of Ketoconazole

Abstract

In oral applications, the microsponge system has been shown to increase the rate of solubilization of poorly water-soluble drugs by entrapping such drugs in the microsponge system's pores.Because these pores are very small, the drug is in effect reduced to
microscopic particles and increased surface area thus greatly increases the rate of
solubilization.
This investigation was done to increase solubility and then bioavialibility of poorly soluble ketoconazole (BCS class II drug) by preparing it as microsponges by quasi emulsion
solvent technique using different types of Eudragits as Eudragit E 100, Eudragit RS or Eudragi tRL. Physicochemical interaction between drug and excipients as individual one,
physical mixture and prepared microsponge has been evaluated using Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) which indicates the
absence of interaction between them. The1: 0.1 ratio drug: Eudragit E 100 at stirring rate of 2000 rpm (F1b) was found to give the best production yield of 80.46±2.41, entrapment efficiency of 70.84%±1.71, and smallest particle size of 57.42±2.26 μm. Scanning electron microscopy of F1b at magnification of 1000x and 50000x shows the presence of drug as nanocrystals inside microsponge. All prepared formulas shows good flow properties indicated the possibility of capsule formulation which show significant (P<0.05) high drug release percent in 0.1 HCl compared with traditional Nizoral® oral tablet (83.15%±1.10) but Eudragit E (F1b ) shows the best drug release percent of 100±0.91 at 20 minutes. Finally, the overall obtained data revealed the feasibility of preparing fast release ketaconazole as microsponges in oral capsules dosage form.