Formulation and Evaluation of Lovastatin Loaded Nanosponges for the treatment of Hyperlipidemia

Abstract

The present investigations was aimed to improve the solubility, to release the drug in a controlled manner for extended period of time, reduce dose dependent side effects and improve the bioavailability of a poorly water soluble BCS class II drug of Lovastatin by formulating it as Nanosponges drug delivery system. Lovastatin Nanosponges were formulated by emulsion solvent evaporation method using Eudragit RS 100 and Ethyl Cellulose as a polymers, PVA as a stabilizer and finally enclosed in hard gelatin Capsules. The prepared Nanosponges were evaluated for FTIR, particle size, polydispersity index (PDI), zeta potential, morphological characteristics by scanning electron microscopy (SEM), production yield, entrapment efficiency, solubility studies, in vitro drug release studies, release kinetics study, stability studies, Flow property and porosity. The optimized formulation filled in capsules and Post formulation parameters of capsule were determined. FTIR studies showed no interaction between drug and excipients. Percentage yield of all the formulation (F1-F10) was found to be in the range of 85.83 to 99.85%. The entrapment efficiency of all the formulations was found to be in the range of 61.68 to 91.18%, among all the formulations F3 (90.04%) and F8 (91.18%) shows high entrapment efficiency. The solubility of all formulation improved (from insoluble to slightly soluble) compared to pure drug of Lovastatin. Among all the formulations F3 (98.15%) and F8 (97.57%) shown complete drug release at the end of 12th hrs. The average particle size of optimized formulation F3 and F8 was found to be 727.0 nm and 769.5 nm respectively. SEM images of optimized formulation showed that the Nanosponges were spherical with numerous pores on their surface, uniform and spongy in nature. The release kinetics of the optimized formulation was best fitted into Higuchi model and showed zero order drug release with Non Fickian diffusion. Stability studies indicated that the formulation is stable as per ICH guidelines. The flow property measurements for optimized formulation observed good were its filled in capsules. Post formulation parameters of capsule were comply with official specifications. They concluded that the both polymers used were efficient carriers for Lovastatin Nanosponges.