An Innovative Formulation Based on Nanostructured Lipid Carriers for Imatinib Delivery: Pre-Formulation, Cellular Uptake and Cytotoxicity Studies

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.

Cannabidiol-Loaded Nanostructured Lipid Carriers (NLCs) for Dermal Delivery: Enhancement of Photostability, Cell Viability, and Anti-Inflammatory Activity

“…From Table 4 , the release kinetics for CBD-NLCs were consistent with Higuchi’s model because the r 2 values were higher than 0.95 for all formulations, indicating that CBD was slowly released from the CBD-NLC matrix at a rate proportional to the square root of time. As shown in the literature, the release kinetics of NLCs generally follow the Higuchi and Korsmeyer–Peppas models [ 24 , 40 , 41 , 42 ]. The Korsmeyer–Peppas model assumes that the release is controlled by diffusion [ 43 ], while the Higuchi model shows a direct relationship between the cumulative amount of drug released and the square root of time [ 44 ].…”

Nanostructured lipid carriers containing benznidazole: physicochemical, biopharmaceutical and cellular in vitro studies

“…As in our case there is no polymer relaxation involved, it may be hypothesized that the burst effect could be slightly affecting the global kinetics of the process [35]. Although this description has its limitations, it has been widely used to describe drug release from similar lipidic formulations [35][36][37][38].…”

Solid Lipid Nanoparticles: Review of the Current Research on Encapsulation and Delivery Systems for Active and Antioxidant Compounds

“… The morphological characterization of SLNs by SEM ( A ) and TEM ( B ) [ 45 ]. The morphological characterization of NLCs by SEM ( C ) [ 70 ], and TEM ( D ) [ 71 ]. …”