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Isotretinoin immobilization into silica/ceria nanoparticle to optimize topical acne vulgaris treatment

Grant number: 19/20777-6
Support type:Scholarships in Brazil - Doctorate
Effective date (Start): March 01, 2020
Effective date (End): February 28, 2022
Field of knowledge:Health Sciences - Medicine
Principal Investigator:Eduardo José Nassar
Grantee:Caroline Borges Azevedo
Home Institution: Pró-Reitoria Adjunta de Pesquisa e Pós-Graduação. Universidade de Franca (UNIFRAN). Franca , SP, Brazil


Acne vulgaris is a very common skin disease that affects a large part of the population at some point in life. The main cause of Acne is bacterial infection caused by P. acnes bacteria, and genetic, hormonal, and psychological factors can influence the disease onset. Both in vitro and in vivo studies have shown the therapeutic effect of isotretinoin on the treatment of Acne. However, there are many side effects associated with this therapy in both the oral and topical modes. In this context, developing an effective therapeutic system that can carry isotretinoin is advantageous because it may improve the isotretinoin biological activity and reduce its side effects. Topical Acne therapy involving administration of a drug encapsulated into nanoparticles is a promising method that can help to achieve this purpose. Nanostructured cerium oxide is noteworthy for its antimicrobial, antioxidant, and anti-inflammatory properties, as well as for its easy preparation, chemical stability, biocompatibility, and high absorption in the UV region. The latter property provides the drug with photoprotection. Nanoceria can be combined with other materials, to enhance the biological properties of the combined materials. The characteristics of the final product will depend on the selected material for combination, the proportions, and the synthesis method. Silica nanoparticles are good candidates for association with nanoceria because they are chemically and thermally stable and inert, can be easily dispersed in aqueous solution, and are optically transparent and biocompatible. The silica surface can be modified to accommodate specific molecules that can bind to biological systems. Particle size control is important for certain applications, and the sol-gel methodology is the most suitable synthetic route to prepare these materials. Thus, this work aims to synthesize and to characterize silica and ceria nanoparticles - associated or not - and subsequently immobilize isotretinoin in the matrixes, to evaluate the biological and antibacterial activity of the resulting systems in vitro against sebocyte cells and P. acnes species and to investigate their potential in topical Acne therapy. (AU)