Borcan Florin, Len Adél, Dehelean Cristina A, Dudás Zoltán, Ghiulai Roxana, Iftode Andrada, Racoviceanu Roxana, Soica Codruta M
Department I, Faculty of Pharmacy, "Victor Babes" University of Medicine and Pharmacy, 300041 Timisoara, Romania.
Neutron Spectroscopy Department, Centre for Energy Research, H-1121 Budapest, Hungary.
Nanomaterials (Basel). 2020 Dec 28;11(1):51. doi: 10.3390/nano11010051.
THE Herpes simplex viruses (HSV-1, HSV-2) are responsible for a wide variety of conditions, from cutaneous-mucosal to central nervous system (CNS) infections and occasional infections of the visceral organs, some of them with a lethal end. Acyclovir is often used intravenously, orally, or locally to treat herpetic infections but it must be administered with caution to patients with kidney disease and to children of early age. The main objectives of this study were to synthesize and evaluate new polyurethane nanoparticles that might be used as proper transmembrane carriers for acyclovir. Polyurethane particles were obtained by a polyaddition process: a mixture of two aliphatic diisocyanates used as organic phase was added to a mixture of butanediol and polyethylene glycol used as aqueous phase. Two different samples (with and without acyclovir, respectively) were synthesized and characterized by UV-Vis spectra in order to assess the encapsulation efficacy and the release profile, FT-IR, DSC, SEM, and SANS for structural characterization, as well as skin irritation tests. Nearly homogeneous samples with particle sizes between 78 and 91 nm have been prepared and characterized revealing a medium tendency to form clusters and a high resistance to heat up to 300 °C. The release profile of these nanoparticles is characteristic to a drug delivery system with a late discharge of the loaded active agents. Very slight increases in the level of transepidermal water loss and erythema were found in a 15-day evaluation on human skin. The results suggest the synthesis of a non-irritative carrier with a high encapsulation efficacy that can be successfully used for the transmembrane transfer of acyclovir.
单纯疱疹病毒（HSV - 1、HSV - 2）可引发多种病症，从皮肤黏膜感染到中枢神经系统（CNS）感染，偶尔还会感染内脏器官，其中一些感染会导致致命后果。阿昔洛韦常用于静脉注射、口服或局部治疗疱疹感染，但对于肾病患者和幼儿必须谨慎使用。本研究的主要目的是合成并评估新型聚氨酯纳米颗粒，其可作为阿昔洛韦合适的跨膜载体。聚氨酯颗粒通过加成聚合过程获得：将用作有机相的两种脂肪族二异氰酸酯混合物加入用作水相的丁二醇和聚乙二醇混合物中。合成了两个不同的样品（分别含有和不含阿昔洛韦），并通过紫外可见光谱评估包封效率和释放曲线，通过傅里叶变换红外光谱（FT - IR）、差示扫描量热法（DSC）、扫描电子显微镜（SEM）和小角中子散射（SANS）进行结构表征，以及进行皮肤刺激性测试。制备并表征了粒径在78至91纳米之间的近乎均匀的样品，结果表明其形成聚集体的倾向中等，并且在高达300℃的温度下具有高耐热性。这些纳米颗粒的释放曲线是药物递送系统的典型特征，即负载的活性剂延迟释放。在对人体皮肤进行的15天评估中，发现经皮水分流失水平和红斑仅有非常轻微的增加。结果表明合成了一种具有高包封效率且无刺激性的载体，可成功用于阿昔洛韦的跨膜转运。
