Menezes Paula Dos Passos, Frank Luiza Abrahão, Lima Bruno Dos Santos, de Carvalho Yasmim Maria Barbosa Gomes, Serafini Mairim Russo, Quintans-Júnior Lucindo José, Pohlmann Adriana Raffin, Guterres Sílvia Stanisçuaski, Araújo Adriano Antunes de Souza
Department of Pharmacy, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil.
College of Pharmacy, Federal University of Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil.
Int J Nanomedicine. 2017 Mar 15;12:2069-2079. doi: 10.2147/IJN.S124564. eCollection 2017.
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.
慢性静脉功能不全的特征是血液从外周静脉向中心静脉的慢性反流紊乱,继而出现静脉高压并导致皮肤改变。传统上,非手术治疗依赖于压迫疗法,最近已证明多种类黄酮具有积极作用。利用各种纺织品和纳米技术的更有效药物递送系统也有了发展,以提供新的治疗选择。我们的目标是利用纳米技术开发一种新制剂,将橙皮素(Hst)(一种以前未用于治疗慢性静脉功能不全的物质)浸渍到纺织纤维中,作为静脉疾病的一种可能替代治疗方法。我们采用预制聚合物的界面沉积法制备了纳米胶囊,Hst浓度为0.5mg/mL,然后对颗粒的大小和分布进行了表征。为了定量样品中的Hst,我们开发了一种使用高效液相色谱的分析方法。作为研究的一部分,进行了包封效率(98.81%±0.28%)、显微镜检查、药物释放(游离Hst:104.96%±12.83%;脂质核纳米胶囊-Hst:69.90%±1.33%)、渗透/透过、药物含量(0.46±0.01mg/mL)以及药物浸渍后洗涤纺织品的效果等研究。结果表明,获得了具有合适大小和分布的纳米颗粒,药物能够控释并渗透/透过皮肤层。此外,已确定聚酰胺能够容纳更多的药物,其含量比棉纤维高2.54倍;洗涤一次和洗涤五次后,这种关系高出2.80倍。总之,这是一种有前景的治疗替代方法,有待在临床试验中进一步研究。