FORMULATION DESIGN AND CHARACTERIZATION OF IMMUNOSUPPRESANT DRUG-LOADED SOLID LIPID NANOPARTICLES FOR ORAL DELIVERY

Abstract

Aim: To develop the preparation of immunosuppressant drug based Solid lipid nanoparticles with lipids Stearic acid and Glyceryl monostereateby hot homogenization method to improve the Sustained release properties of the Immunosuppresant Drug.

Object: To develop sustained release oral product namely solid lipid nanoparticles of immunosuppressant drug by hot homogenization method using Stearic acid and Glyceryl monostereate as lipids which served to modulate drug release and improve overall bioavailability. Poloxamer 188 and soya lecithin work together as a surfactant to enhance the drug's oral bioavailability by overcoming its poor water solubility and absorption issues used in various proportions to reduce the dosing frequency and there by improve the patient compliance.

Methodology: Immunosuppressant drug based Solid lipid nanoparticles were developed by using Stearic acid and Glyceryl monostereate lipids and surfactant Poloxamer 188 and soya lecithin as release modifier in different ratios by hot homogenization method. The solid lipid nanoparticles were evaluated for surface morphology and shape by scanning electron microscopy (SEM), % yield, Zeta potential, encapsulation efficiency and in vitro drug release. The SLN were also analyzed by Fourier Transform Infra-Red Spectroscopy (FTIR) to determine drug-lipid-surfactant interaction.

Result and Discussion: Prepared solid lipid nanoparticles containing immunosuppressant drug by hot homogenization method and examined the effects of various factors (concentration of lipids, concentration of surfactants and concentration of drug). Poloxamer 188 used as surfactant in SLNs improves the dissolution rate and solubility of poorly water-soluble immunosuppressant drug, a key factor for enhancing its oral absorption. For slowing the drug release hydrophilic surfactant tween 80 was added in different concentration so that the drug was released constantly for 24 hours. Formulated SLNs were evaluated for particle size, drug entrapment, Zeta potential, DSC study, XRD study, release kinetic and stability study. Particle size distribution of both in placebo and drug loaded formulations were measured by an optical microscope and particle size of optimized SLNs was determined by scanning electron microscopy. Results shows that no significant drug-lipid-Surfactant interactions were observed in FTIR studies. Drug release profile of immunosuppressant drug SLNs were performed by using dialysis method in phosphate buffer pH 6.8 for 24 hrs and exhibited zero order kinetics. The study demonstrated that proper selection of lipids and method of preparation (by hot homogenization) would lead to production of SLNs with best characteristic properties. The drug loaded batches were found to be stable when stored at room temperature for 45 days.

Conclusion: Immunosuppressant drug based solid lipid nanoparticles are promising pharmaceutical dosage forms by providing sustained release drug delivery systems and also improve its bioavailability. The Sustained release effect of SLNs depends on the lipid concentration and type of surfactant used in the formulation. The entire process is feasible in an industrial scale and demands pilot study.