International Journal of Nanomedicine (Mar 2017)
Hesperetin-loaded lipid-core nanocapsules in polyamide: a new textile formulation for topical drug delivery
Abstract
Paula dos Passos Menezes,1 Luiza Abrahão Frank,2 Bruno dos Santos Lima,1 Yasmim Maria Barbosa Gomes de Carvalho,1 Mairim Russo Serafini,1 Lucindo José Quintans-Júnior,3 Adriana Raffin Pohlmann,4 Sílvia Stanisçuaski Guterres,2 Adriano Antunes de Souza Araújo1 1Department of Pharmacy, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil; 2College of Pharmacy, Federal University of Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil; 3Department of Physiology, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil; 4Institute of Chemistry, Federal University of Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil Abstract: Chronic venous insufficiency is characterized by chronic reflux disorder of blood from the peripheral to the central vein, with subsequent venous hypertension and resulting changes in the skin. Traditionally, nonsurgical treatments relied on the use of compression therapy, and more recently a variety of flavonoids have been shown to have positive effects. There have also been developments of more effective drug delivery systems using various textiles and nanotechnology to provide new therapeutic options. Our objective was to use nanotechnology to develop a new formulation containing hesperetin (Hst), a substance not previously used in the treatment of chronic venous insufficiency, impregnated into textile fibers as a possible alternative treatment of venous diseases. We prepared the nanocapsules using the interfacial deposition of preformed polymer method with an Hst concentration of 0.5 mg/mL and then characterized the size and distribution of particles. To quantify the Hst in the samples, we developed an analytical method using high-performance liquid chromatography. Studies of encapsulation efficiency (98.81%±0.28%), microscopy, drug release (free-Hst: 104.96%±12.83%; lipid-core nanocapsule-Hst: 69.90%±1.33%), penetration/permeation, drug content (0.46±0.01 mg/mL) and the effect of washing the textile after drug impregnation were performed as part of the study. The results showed that nanoparticles of a suitable size and distribution with controlled release of the drug and penetration/permeation into the skin layers were achieved. Furthermore, it was established that polyamide was able to hold more of the drug, with a 2.54 times higher content than the cotton fiber; after one wash and after five washes, this relation was 2.80 times higher. In conclusion, this is a promising therapeutic alternative to be further studied in clinical trials. Keywords: lipid-core nanocapsules, polymer, hesperetin, fabrics, impregnation, medical textiles, polyamide, poly(ε-caprolactone)