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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Combination of microneedles and microemulsions to increase celecoxib topical delivery for potential application in chemoprevention of breast cancer

Full text
Author(s):
Mojeiko, Gabriela [1] ; de Brito, Moacir [1] ; Salata, Giovanna C. [1] ; Lopes, Luciana B. [1]
Total Authors: 4
Affiliation:
[1] Univ Sao Paulo, Inst Biomed Sci, Dept Pharmacol, Av Prof Lineu Presses 1524, Sao Paulo, SP - Brazil
Total Affiliations: 1
Document type: Journal article
Source: International Journal of Pharmaceutics; v. 560, p. 365-376, APR 5 2019.
Web of Science Citations: 3
Abstract

In spite of the high incidence of breast cancer worldwide, there are few strategies for its chemoprevention, and they have limited adherence mainly due to their serious adverse effects. As a new approach for local breast cancer chemoprevention, we developed and optimized microemulsions for topical delivery of celecoxib to the breast skin, and evaluated their combination with microneedles to improve drug penetration for localization in the mammary tissue. Microemulsions containing water at 15% (ME-15), 29% (ME-29) and 60% (ME-60) were obtained and characterized. They were isotropic, displayed Newtonian behavior and particle size smaller than 100 nm. ME-15 and ME-29 increased transepidermal water loss (TEWL) compared to ME-60, and displayed stronger vascular toxicity, evidenced by hemorrhage and lysis in HET-CAM assays. ME-60 was more efficacious at increasing celecoxib cutaneous and percutaneous delivery (1.3-4-fold). Increasing the number of microneedle roller applications from 1 to 8 increased the number of skin punctures and TEWL; its association with ME-60 promoted no further increase in TEWL, but improved (1.6-4-fold) celecoxib cutaneous and percutaneous delivery. Microemulsion incorporation reduced celecoxib IC(50)( )in MCF-7 cells (3.3-fold), suggesting that presence of formulation components in the mammary tissue might improve drug cytotoxicity. (AU)

FAPESP's process: 17/23213-0 - Biorresponsive systems for sustained drug release and breast cancer chemoprevention
Grantee:Giovanna Cassone Salata
Support Opportunities: Scholarships in Brazil - Master
FAPESP's process: 13/16617-7 - Nanostructured systems for topical delivery and co-localization of chemopreventive and chemoterapeutic agents in the skin and breast tissue
Grantee:Luciana Biagini Lopes
Support Opportunities: Research Grants - Young Investigators Grants