Development of Gefitinib-loaded Solid Lipid Nanoparticles for the Treatment of Breast Cancer: Physicochemical evaluation, Stability and Anticancer Activity in Breast Cancer (MCF-7) Cells.

Abstract
In the current study, the toxic effects of gefitinib-loaded solid lipid nanoparticles (GFTloaded SLNs) upon human breast cancer cell lines (MCF-7) were investigated. GFT-loaded SLNs were\r\nprepared through a single emulsification–evaporation technique using glyceryl tristearate (Dynasan™\r\n114) along with lipoid® 90H (lipid surfactant) and Kolliphore® 188 (water-soluble surfactant). Four\r\nformulae were developed by varying the weight of the lipoid™ 90H (100–250 mg), and the GFTloaded SLN (F4) formulation was optimized in terms of particle size (472 ± 7.5 nm), PDI (0.249), ZP\r\n(−15.2 ± 2.3), and EE (83.18 ± 4.7%). The optimized formulation was further subjected for in vitro\r\nrelease, stability studies, and MTT assay against MCF-7 cell lines. GFT from SLNs exhibited sustained\r\nrelease of the drug for 48 h, and release kinetics followed the Korsmeyer–Peppas model, which\r\nindicates the mechanism of drug release by swelling and/or erosion from a lipid matrix. When pure\r\nGFT and GFT–SLNs were exposed to MCF-7 cells, the activities of p53 (3.4 and 3.7 times), caspase-3\r\n(5.61 and 7.7 times), and caspase-9 (1.48 and 1.69 times) were enhanced, respectively, over those in\r\ncontrol cells. The results suggest that GFT-loaded SLNs (F4) may represent a promising therapeutic\r\nalternative for breast cancer.\r\n

Author
Ibrahim A. Aljuffali , Md. Khalid Anwer , Mohammed Muqtader Ahmed, Ahmed Alalaiwe , Mohammed F. Aldawsari , Farhat Fatima and Shahid Jamil.

DOI
https://doi.org/10.3390/ph16111549

Publisher
Pharmaceuticals

ISSN

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