Controlled Release of Caffeic Acid and Pinocembrin by Use of nPSi-βCD Composites Improves Their Antiangiogenic Activity
Dina Guzmán-Oyarzo,
Jacobo Hernández-Montelongo,
Carlos Rosas,
Pamela Leal,
Helga Weber,
Marysol Alvear,
Luis A. Salazar
Affiliations
Dina Guzmán-Oyarzo
Center of Molecular Biology and Pharmacogenetics, Department of Basic Sciences, Scientific and Technological Bioresource Nucleus (BIOREN-UFRO), Universidad de La Frontera, Avenida Francisco Salazar 01145, Temuco 4811230, Chile
Jacobo Hernández-Montelongo
Bioproducts and Advanced Materials Research Center (BioMA), Faculty of Engineering, Universidad Católica de Temuco, Avenida Rudecindo Ortega 02950, Temuco 4813302, Chile
Carlos Rosas
Escuela de Medicina, Facultad de Medicina y Ciencia, Universidad San Sebastián, General Lagos 1163, Valdivia 5110693, Chile
Pamela Leal
Center of Excellence in Translational Medicine (CETM) and Scientific and Technological Bioresource Nucleus (BIOREN-UFRO), Universidad de La Frontera, Temuco 4810296, Chile
Helga Weber
Center of Excellence in Translational Medicine (CETM) and Scientific and Technological Bioresource Nucleus (BIOREN-UFRO), Universidad de La Frontera, Temuco 4810296, Chile
Marysol Alvear
Department of Chemical Sciences and Natural Resources, Faculty of Engineering and Sciences, Universidad de La Frontera, Avenida Francisco Salazar 01145, Temuco 4811230, Chile
Luis A. Salazar
Center of Molecular Biology and Pharmacogenetics, Department of Basic Sciences, Scientific and Technological Bioresource Nucleus (BIOREN-UFRO), Universidad de La Frontera, Avenida Francisco Salazar 01145, Temuco 4811230, Chile
Although polyphenols have great pharmacological potential, the main disadvantage is that they have low bioavailability at the desired site. Thus, the use of biocompatible systems for drug delivery is a strategy that is currently gaining great interest. The objective of this study is to evaluate the effect of microencapsulation of caffeic acid and pinocembrin on the antioxidant and antiangiogenic activity of both polyphenols, by the use of nPSi-βCD composite microparticles. For this HUVEC, cells were exposed to H2O2 and to treatments with polyphenols in solution and loaded in the composite microparticle. The polyphenols were incorporated into a microparticle using nanoporous silicon, chitosan and a β-cyclodextrin polymer as the biomaterial. The evaluation of the antiangiogenic effect of the treatments with polyphenols in solution and microencapsulated was carried out through functional tests, and the changes in the expression of target genes associated with the antioxidant pathway and angiogenesis was performed through qPCR. The results obtained show that the caffeic acid and pinocembrin have an antioxidant and antiangiogenic activity, both in solution as microencapsulated. In the caffeic acid, a greater biological effect was observed when it was incorporated into the nPSi-βCD composite microparticle. Our results suggest that the nPSi-βCD composite microparticle could be used as an alternative oral drug administration system.