Folic acid-chitosan coated stylosin nanostructured lipid carriers: fabrication, in vitro–in vivo assessment in breast malignant cells

Abstract

Synthesis of targeted nanostructure lipid carriers for stylosin (STY-CFN-NPs) delivery to MCF-7 cells. STY-CFN-NPs were formulated via the homogenization and ultra-sonication technique. After evaluating the amount of drug encapsulation and FA binding, the toxicity effect of the STY and STY-CFN-NPs on MCF-7 cells was measured by the MTT method. Cell cycle analysis, AO/PI staining and qPCR to assess the inducing of apoptosis as well as Tubo cancer cell inoculated mouse model for antitumor properties of STY-CFN-NPs were used. Significant increases in nanoparticle size and changes in zeta potential were observed after FA-CS coating on nanoparticles. Slow release of the STY within 144 h as well as the acceptable rate for STY encapsulation efficiency (92.4% and FA binding (52.5%) to the STY-CFN-NPs (PS: 66.26 ± 3.02 nm, ZP: 29.54 ± 1.01 mV and PDI: 0.32 ± 0.01) was reported. STY-CFN-NPs exhibited higher toxicity compared to STY suspension and treatment with STY-CFN-NPs was lead to increased apoptotic cells, stopped cells in the SubG1 phase, and also increased caspase and BAX expression and decreased BCL-2 and BCL-XL expression in in vitro and decreased the size of murine tumors (54.57% in 16 days) in in vivo. The results showed STY-CFN-NPs have good potential for breast cancer management.

Keywords:

• Chitosan
• stylosin
• nanostructured lipid carriers
• breast malignant cell

Acknowledgment

This work was supported by Islamic Azad University, Mashhad, Iran and thus is appreciated by the author.

Author contributions

Masoud Homayouni Tabrizi conceived the presented idea. Soroush Sadeghi, Masoud Homayouni Tabrizi, Amin Farhadi performed the experiments and computations.

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

This research was performed at personal expense in the laboratory of Islamic Azad University of Mashhad.