FORMULATION AND EVALUATION OF GEFITINIB NANO CRYSTALS

Abstract

Nanotechnology will affect our lives tremendously over the next decade in very different fields,including medicine and pharmacy. Transfer of materials into the nanodimension changes their physical properties which were used in pharmaceutics to develop a new innovative formulation principle for poorly soluble drugs like gefitinib, an anticancer agent,is taken as a model drug characterized by poor solubility and bioavailability.In this study an attempt was made for preparation of nanocrystals using bottom up technique. PVP and Tween-80 were used as stabilizer and surfactant at different concentrations, and all the 9 formulations were prepared by precipitation method.The obtained nanocrystals were evaluated by determining their particle size, zeta potential, poly dispersity index, fourier transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRD), drug pay load and in-vitro diffusion studies.The particle sizes of the obtained nanocrystals are in below 100nm with low polydispersity indices.Zeta potential is sufficiently high to obtain a stable colloidal nanosuspension. FTIR, and XRPD studies revealed the differential properties of nanocrystals. The formation of nanocrystals was confirmed by FTIR spectroscopy. The crystalline nature of the nanocrystals was determined by XRPD.The in-vitro diffusion studies were performed in phosphate buffer.Tween 80 releases 90% of the drug within 3 hrs but in case of PVP and combination of PVP and tween 80,the release was extended to 4 hrs.PVP releases only 80% of drug in 4 hrs but combination of PVP and Tween formulations release maximum amount of drug i.e., 99% within 4 hrs.The drug payload was above 80% in all the 9 formulations. In conclusion gefitinib nanocrystals prepared with tween 80 and PVP showed enhanced and sustained diffusion rate when compared to the other formulations.