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Repository of Research and Investigative Information

Baqiyatallah University of Medical Sciences

Targeted nanostructured lipid carrier containing galangin as a promising adjuvant for improving cytotoxic effects of chemotherapeutic agents

(2021) Targeted nanostructured lipid carrier containing galangin as a promising adjuvant for improving cytotoxic effects of chemotherapeutic agents. Naunyn-Schmiedebergs Archives of Pharmacology. pp. 2353-2362. ISSN 0028-1298

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Abstract

Resistance to chemotherapeutic drugs is the main limitation of cancer therapy. The combination use of chemotherapeutic agents and galangin (a naturally active flavonoid) amplifies the effectiveness of cancer treatment. This study aimed to prepare arginyl-glycyl-aspartic acid (RGD) containing nanostructured lipid carrier (NLC-RGD) to improve the bioavailability of galangin and explore its ability in improving the cytotoxic effects of doxorubicin (DOX). Galangin-loaded NLC-RGD was prepared by hot homogenization method and characterized by diverse techniques. Then, cytotoxicity, uptake, and apoptosis induction potential of prepared nanoparticles beside the DOX were evaluated on A549 lung cancer cells. Finally, the expression level of some ABC transporter genes was evaluated in galangin-loaded NLC-RGD-treated cells. Nanoparticles with appropriate characteristics of the delivery system (size: 120 nm, polydispersity index: 0.23, spherical morphology, and loading capacity: 59.3 mg/g) were prepared. Uptake experiments revealed that NLC-RGD promotes the accumulation of galangin into cancerous cells by integrin-mediated endocytosis. Results also showed higher cytotoxicity and apoptotic effects of DOX + galangin-loaded NLC-RGD in comparison to DOX + galangin. Gene expression analysis demonstrated that galangin-loaded NLC-RGD downregulates ABCB1, ABCC1, and ABCC2 more efficiently than galangin. These findings indicated that delivery of galangin by NLC-RGD makes it an effective adjuvant to increase the efficacy of chemotherapeutic agents in cancer treatment.

Item Type: Article
Keywords: Galangin Cancer treatment Nanostructured lipid carrier RGD abc transporters cancer cells flavonoids apoptosis proliferation optimization inhibition rgd Pharmacology & Pharmacy
Page Range: pp. 2353-2362
Journal or Publication Title: Naunyn-Schmiedebergs Archives of Pharmacology
Journal Index: ISI
Volume: 394
Number: 12
Identification Number: https://doi.org/10.1007/s00210-021-02152-9
ISSN: 0028-1298
Depositing User: مهندس مهدی شریفی
URI: http://eprints.bmsu.ac.ir/id/eprint/9701

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