Pro Transferosome Loaded Gefitinib Novel Tablet for pulmonary drug delivery: Optimization and characterization

Abstract

The aim of this study is to optimize and characterize gefitinib-loaded Protransferosome tablets for pulmonary drug delivery. Gefitinib is a chemotherapy drug used primarily for the treatment of certain types of non-small cell lung cancer (NSCLC). It is a member of the tyrosine kinase inhibitor (TKI) class of medications. Gefitinib works by targeting and inhibiting the epidermal growth factor receptor (EGFR) tyrosine kinase, which has impact on the growth and proliferation of malignant cells. The extensive surface region of the respiratory system provides an ideal site for localized anti-cancer drug delivery within the lungs. Gefitinib loaded Protransferosomes (PT) were prepared by using rotary film evaporation method. The Box-Behnken statistical design was utilized to optimize the formulation and identify the variable parameters that impact the vesicle size, zeta potential and entrapment efficiency. Finally, the formulated Gefitinib Protransferosomes was undergo direct compression method. which was evaluated for weight variation test, Thickness test, Hardness test, disintegration test, Friability test, and Dissolution test. The GFT-loaded LMH powders, particularly O GFT PTS (lipid phase-to-carrier ratio of 1:25 w/w), showed remarkable flowability, as indicated by a favorable angle of repose (AOR) and a excellent compressibility index due to their small and homogeneous particle size. The prepared GFT PT had high encapsulation efficiencies (EE%) ranging from 52.2 ± 0.66 % to 75.6 ± 1.12 %, with Vesicle sizes varying from 3.153 ± 0.153 μm to 5.39 ± 0.684 μm, and zeta potentials ranging from −26.6 mV to −35.9 mV. Scanning electron microscopy discovered that the protransferosomes were circular in shape. In-vitro release studies conducted over 1 h for the optimal formulation shown a better cumulative drug release (CDR) of 94.24 % for Gefitinib. Stability results showed no significant changes in weight variation, hardness, friability, thickness, or dissolution tests. The development and optimization of Protransferosome-loaded tablets show promising results for pulmonary drug delivery. The optimized formulation demonstrates improved drug delivery performance, with the potential for enhanced therapeutic efficacy in respiratory conditions. Further studies and clinical evaluations may be required to validate these findings in practical applications.