Polymeric Micellar Formulation Enhances Antimicrobial and Anticancer Properties of Salinomycin.

Pharm Res

Pharmacological and Regulatory Sciences Group (PharmaRegSci), Research Institute for Medicines (iMed.ULisboa), Faculdadde de Farmácia da Universidade de Lisboa, Lisbon, Portugal.

Published: April 2019

AI Article Synopsis

  • Salinomycin (SAL) is a powerful compound that can fight infections and cancer, prompting research into improving its delivery through polymeric micelles made from Pluronic® F127.
  • Using a Quality by Design approach, the study examined the effectiveness of these micelles (PM_SAL) against bacteria and cancer cells, showing notable results particularly against MRSA and A549 lung cancer cells.
  • Results indicated PM_SAL not only effectively fought MRSA but also significantly reduced cancer cell migration and interfered with proteins linked to cancer progression, suggesting it could be a valuable new treatment for cancer growth.

Article Abstract

Purpose: Salinomycin (SAL) is a polyether compound that exhibits strong antimicrobial as well as anticancer activity. Nanomedicine has been at the forefront of drug delivery research with the aim of increasing the efficacy, specificity and reduce toxicity of drugs. There is an intersection between infection and cancer, and cancer patients are prone to bacterial infections. In this study, polymeric micelles were prepared using Pluronic® F127 (PM) to encapsulate SAL (PM_SAL) with the view of enhancing antimicrobial and anticancer activity.

Methods: A Quality by Design (QbD) approach was utilized to synthesize PM_SAL, and nanoformulation activity was determined against bacterial (S. aureus, MRSA and E. coli). Effects on cancer cell line A549, i.e. cell viability, prevention of P-gp efflux, vimentin expression, effects on migratory ability of A549 cells. Anticancer activity was determined by ability to eradicate cancer stem-like cells.

Results: PM_SAL demonstrated only efficacy against MRSA, being even higher than that obtained with SAL. In A549 cells, a 15-fold increase in P-gp's expression as well as a significant decrease of the cell's migration, was observed.

Conclusions: PM_SAL can interfere with the oncogenic protein VIM, involved in the crucial mechanisms EMT, downregulating its expression. Altogether data obtained indicates that this antibiotic and the developed polymeric micelle system is a very promising inhibitor of tumor cell growth.

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Source
http://dx.doi.org/10.1007/s11095-019-2615-6DOI Listing

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