Development, Characterization and Evaluation of Gefitinib-Containing Phospholipid Complex

Abstract

Objective: To develop, characterize and evaluations of gefitinib loaded phospholipid complex as a nano carrier.

Material and methodology: Gefitinib phospholipid complex was prepared by solvent evaporation method. Gefitinib, phospholipid and complexing solvent (methanol) in different ratios used in the preparation. The batch code from F1 to F7 were prepared in different molar ratio (drug: egg lecithin E80) with 10 ml methanol solvent for each formulation.

Results: The optimized formulation F5 was obtained from F1 to F7 with yellowish thick layer appearance, drug content 95.188±0.532, with uniform regular rigid vesicles. The particle size of F5 was 162.63 nm with PDI 23.9% and zeta potential was -34.5 mV was obtained. The maximum in-vitro diffusion study of formulation F5 was calculated up to 24 hr. was 76.191±0.486, the formulation F5 follows Krosmeyer-peppas kinetics with R² value 0.9826.

Conclusion: Phospholipid complex formulation of gefitinib was prepared by using the reflux technique method. For optimization of phospholipid complex, different formulations (F1 to F8) were prepared using the various quantities of lipid. Formulation (F5) with maximum n-octanol solubility, drug content and optimum size considered as optimized formulation. The shape and size of the optimized F5 formulation was confirmed through microscope and particle size and found that most of the particles were well identified. Optimized formulation in vitro drug release was studied in phosphate buffer saline (PBS) pH 6.8 using dialysis method. The results showed that the drug release of F5 formulation followed Krosmeyer-Peppas which describes that the gefitinib follows a controlled mechanism for release from phospholipid complex.