4.5 Article

Polymeric Micellar Formulation Enhances Antimicrobial and Anticancer Properties of Salinomycin

期刊

PHARMACEUTICAL RESEARCH
卷 36, 期 6, 页码 -

出版社

SPRINGER/PLENUM PUBLISHERS
DOI: 10.1007/s11095-019-2615-6

关键词

Antibiotics; cancer stem cells; nanomedicines; polymericmicelles; quality by design; salinomycin

资金

  1. European Comission [ENMed/0009/2015, ENMed/0065/2016]
  2. Fundacao para a Ciencia e Tecnologia (FCT), Portugal [ENMed/0009/2015, ENMed/0065/2016]
  3. COST Action [MP1404]
  4. Fundação para a Ciência e a Tecnologia [ENMed/0065/2016, ENMed/0009/2015] Funding Source: FCT

向作者/读者索取更多资源

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 (R) 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, down-regulating 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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