Synthesis, characterization and antiviral efficacy of valacyclovir loaded polymeric nanoparticles against wild-type herpes simplex virus type 2.

Oluwafemi Samuel Obisesan, Lesego Tshweu, Lindiwe Nkabinde-Thete, Bathabile Ramalapa, Mpho Phehello Ngoepe, Roux Saartjie, Hazel Tumelo Mufhandu
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Abstract

Herpes simplex virus type 2 (HSV-2) remains a significant public health concern due to its high rates of mortality and morbidity. While various chemotherapeutic options exist for treating HSV-2, they are often inadequate as none provide a definitive cure, and there is a growing issue of drug-resistant strains. The introduction of nanomedicine for antiviral drug delivery offers a promising avenue to enhance the effectiveness of these treatments. This study explored an innovative approach to treating HSV-2 by encapsulating valacyclovir in biodegradable polycaprolactone (PCL) using a double emulsion technique. The formulated valacyclovir-loaded polymeric nanoparticles were characterized, revealing monodispersed particles with an average hydrodynamic size ranging from 154.9 ± 2.1 to 232.8 ± 6.2 nm, along with an encapsulation efficiency of 50%-66% and a drug loading capacity of 11.6%-13.9%. Additionally, there is no significant cytotoxicity of the test compounds to Vero cells at 0.3 mg ml-1concentration with a cell viability within the range of 85 ± 13.6%-100 ± 4.8%. The antiviral activity of both the free drug (valacyclovir) and the valacyclovir-loaded polymeric nanoparticles was assessed in HSV-2 infected Vero cells. The results demonstrated that the valacyclovir-loaded nanoparticles exhibited a 1.2-1.3fold (p< 0.005) increase in antiviral efficacy compared to the free drug. This study thus presents a novel nanotechnology-based treatment approach for HSV-2, offering enhanced antiviral effectiveness over traditional treatments.

负载Valacyclovir的聚合纳米颗粒的合成、表征及其对2型单纯疱疹病毒的抗病毒作用
2型单纯疱疹病毒(HSV-2)由于其高死亡率和发病率,仍然是一个重大的公共卫生问题。虽然有各种化疗方案可用于治疗2型单纯疱疹病毒,但它们往往是不够的,因为没有一种能提供明确的治愈方法,而且耐药菌株的问题日益严重。纳米药物用于抗病毒药物递送的引入为提高这些治疗的有效性提供了一条有希望的途径。本研究探索了一种采用双乳技术将valacyclovir包封在可生物降解的聚己内酯(PCL)中治疗HSV-2的创新方法。对制备的valacyclovir负载聚合物纳米颗粒进行了表征,其单分散颗粒的平均水动力尺寸为154.9±2.1 ~ 232.8±6.2 nm,包封效率为50 ~ 66%,载药量为11.6 ~ 13.9%。此外,在HSV-2感染的Vero细胞中,评估了游离药物(valacyclovir)和负载valacyclovir的聚合纳米颗粒的抗病毒活性。结果表明,与游离药物相比,负载valacyclovir的纳米颗粒的抗病毒功效提高了1.2-1.3倍。因此,这项研究提出了一种新的基于纳米技术的HSV-2治疗方法,比传统治疗方法具有更高的抗病毒效果。
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