| Abstrakt: |
Purpose: Gefitinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that has been authorized for the treatment of non-small lung cancer; however, its applications are not restricted. Instead, it can also be utilized for the treatment of other ailments, such as arthritis, breast cancer, and skin cancer. Their application is limited due to biopharmaceutical issues, as they belong to the second class of BCS and trigger first-pass metabolism. Methods: In the present study, a gefitinib-phospholipid complex (GB-PC-90G) was developed using the solvent evaporation method through a job plot. The FTIR, DSC, and SEM morphologies confirmed and characterized the complexes. A dissolution study was performed at pH 1.2 and revealed improved drug release through complexation. The complex was loaded into a nanoemulsion (GB-PC90G@NE) using caproyl 90, Transcutol HP, and Tween 80 as the oil, surfactant, and co-surfactant, respectively. These parameters were optimized using Box–Behnken design (BBD) software, and the formulation underwent in vitro characterization. Results: Globule size and zeta potential for optimized batch were 165.6 nm and − 24.4 mV respectively. The SEM morphology indicated spherical nanoparticles. In vitro release at pH 7.4 showed the sustained release behavior of the drug from the nanoemulsion within 24 h compared to a non-complexed drug. Moreover, stability study data confirmed that complex-loaded nanoemulsions were stable for at least 3 months at 4 ℃ and 25 ℃. Conclusion: Finally, it was concluded that GB-PC90G@NE enhanced gefitinib's biopharmaceutical performance and hydrophilicity. In the future, this complex-loaded nanoemulsion will be subjected to ex vivo and in vivo studies to manage arthritis. [ABSTRACT FROM AUTHOR] |
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