Preparation, Characterization, and Anti-Cancer Activity of Nanostructured Lipid Carriers Containing Imatinib.

Hafiz A Makeen,Hassan A Alhazmi,Muhammad Hadi Sultan,M Intakhab Alam,Rayan A Ahmed,Ahmed A Albarraq,Syam Mohan,Mohamed Ahmed Al-Kasim

doi:10.3390/pharmaceutics13071086

Hafiz A Makeen, Hassan A Alhazmi + Show 6 more

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https://doi.org/10.3390/pharmaceutics13071086

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Journal: Pharmaceutics	Publication Date: Jul 16, 2021
Citations: 12	License type: CC BY 4.0

Affiliation: Jazan University

Abstract

Breast cancer is the most widespread malignancy in women worldwide. Nanostructured lipid carriers (NLCs) have proven effective in the treatment of cancer. NLCs loaded with imatinib (IMA) (NANIMA) were prepared and evaluated for their in vitro efficacy in MCF-7 breast cancer cells. The hot homogenization method was used for the preparation of NANIMAs. An aqueous solution of surfactants (hot) was mixed with a molten mixture of stearic acid and sesame oil (hot) under homogenization. The prepared NANIMAs were characterized and evaluated for size, polydispersity index, zeta potential, encapsulation efficiency, release studies, stability studies, and MTT assay (cytotoxicity studies). The optimized NANIMAs revealed a particle size of 104.63 ± 9.55 d.nm, PdI of 0.227 ± 0.06, and EE of 99.79 ± 0.03. All of the NANIMAs revealed slow and sustained release behavior. The surfactants used in the preparation of the NANIMAs exhibited their effects on particle size, zeta potential, encapsulation efficiency, stability studies, and release studies. The cytotoxicity studies unveiled an 8.75 times increase in cytotoxicity for the optimized NANIMAs (IC50 = 6 µM) when compared to IMA alone (IC50 = 52.5 µM) on MCF-7 breast cancer cells. In the future, NLCs containing IMA will possibly be employed to cure breast cancer. A small amount of IMA loaded into the NLCs will be better than IMA alone for the treatment of breast cancer. Moreover, patients will likely exhibit less adverse effects than in the case of IMA alone. Consequently, NANIMAs could prove to be useful for effective breast cancer treatment.

Highlights

Introduction iationsBreast cancer is the most prevalent malignancy in women worldwide and is curable in approximately 80% of patients with early-stage nonmetastatic disease
The aim of this research was to design and formulate Nanostructured lipid carriers (NLCs) loaded with IMA (NANIMAs), evaluate their in vitro characteristics such as particle size, polydispersity index, zeta potential, encapsulation performance, release performance, stability, and cytotoxicity (MTT assay) studies in MCF-7 breast cancer cells in order to minimize the therapeutic dose of IMA
The results show that the S2TIN formulation achieved a significantly higher cytotoxicity, which was superior compared to the pure compound IMA

Summary

Introduction

Breast cancer is the most prevalent malignancy in women worldwide and is curable in approximately 80% of patients with early-stage nonmetastatic disease. With the treatments presently available, advanced breast cancer with remote organ metastases is considered incurable [1]. Receptor tyrosine kinase overexpression is a typical pathway correlated with different malignancies [2]. At Novartis, imatinib (Figure 1) was synthesized and has emerged as the lead compound against chronic myelogenous leukemia (CML) cells for clinical development [3]. Centered on its application in the treatment of CML and gastrointestinal stromal tumors (GISTs), imatinib is a tyrosine kinase inhibitor that usually inhibits the tyrosine kinase action of BCR-Abl, platelet-derived growth factor receptors (PDGFRs), and KIT4 proteins. Tyrosine kinase receptors play an essential role in tumor

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