Abstract
Imatinib (IMT) is a tyrosine kinase enzyme inhibitor and extensively used for the treatment of gastrointestinal stromal tumors (GISTs). A nanostructured lipid carrier system (NLCS) containing IMT was developed by using emulsification–sonication methods. The characterization of the developed formulation was performed in terms of its particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, loading capacity, sterility, syringeability, stability, in vitro release kinetics with mathematical models, cellular uptake studies with flow cytometry, fluorescence microscopy and cytotoxicity for CRL-1739 cells. The particle size, PDI, loading capacity and zeta potential of selected NLCS (F16-IMT) were found to be 96.63 ± 1.87 nm, 0.27 ± 0.15, 96.49 ± 1.46% and −32.7 ± 2.48 mV, respectively. F16-IMT was found to be stable, thermodynamic, sterile and syringeable through an 18 gauze needle. The formulation revealed a Korsmeyer–Peppas drug release model of 53% at 8 h, above 90% of cell viability, 23.61 µM of IC50 and induction of apoptosis in CRL-1739 cell lines. In the future, F16-IMT can be employed to treat GISTs. A small amount of IMT loaded into the NLCSs will be better than IMT alone for therapy for GISTs. Consequently, F16-IMT could prove to be useful for effective GIST treatment.
Highlights
Cancer has become a common disease, and it can lead to death
Solubility studies were carried out in water, surfactants and lipids, which can be used in the preparation of nanostructured lipid carrier system (NLCS)
This work defines preformulation and formulation studies that resulted in the new development of NLCSs containing IMT
Summary
Cancer has become a common disease, and it can lead to death. It has affected life expectancy according to the disease level in most developed countries in this century [1,2].Current therapies for cancer disease include chemotherapy, radiotherapy and surgery.Among them, surgery is an invasive method that can be used in some cases. Cancer has become a common disease, and it can lead to death. It has affected life expectancy according to the disease level in most developed countries in this century [1,2]. The techniques of chemotherapy and radiotherapy show multidrug resistance and severe adverse effects in patients. These effects may decrease the achievement of treatment as well as reducing patient compliance. Nanotechnological products have great potential for the delivery of numerous anti-cancer agents. They have demonstrated benefits over traditional chemotherapy [3]
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