Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Pampa, Uruguaiana, RS, Brasil.
Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Pampa, Uruguaiana, RS, Brasil; Programa de Pós-Graduação em Bioquímica, Universidade Federal do Pampa, Uruguaiana, RS, Brasil.
Biomed Pharmacother. 2022 Sep;153:113410. doi: 10.1016/j.biopha.2022.113410. Epub 2022 Jul 15.
Biodegradable polymeric nanocapsules (NC) present incredible characteristics as drug nanocarriers that optimize drug targeting. However, However, a more detailed isolated effect of polymer-based nanoparticles as drug carriers is required. This work aimed to evaluate the per se effect of blank-NC (NC-B) with different surface characteristics both in vitro and in vivo toxicity. NC1-B (Polysorbate 80 coated poly(ɛ-caprolactone) NC), NC2-B (polyethylene glycol 6000 coated poly(ɛ-caprolactone) NC), NC3-B (chitosan-coated poly(ɛ-caprolactone) NC) and NC4-B (Eudragit® RS100 NC) were prepared by nanoprecipitation method. Formulations were characterized by particle size, zeta potential, and pH. The in vitro cytotoxicity tests against tumor cell lines were performed (HepG2 and MCF-7). Antiviral activity was evaluated by MTT in Vero cells infected with HSV-1 (KOS strain). In vivo evaluation was performed in apomorphine-induced stereotypy in Wistar rats and locomotor activity distance, head movements, and rearing behavior were measured. NC1-B, NC2-B, NC3-B, and NC4-B had a diameter under 350 nm. The pH and zeta potential of formulations varied according to their coating. For in vitro evaluation of antitumor activity and antiviral activity, one-way ANOVA showed no significant differences in cell viability. In vivo tests showed low neurological effects. In conclusion, different surface characteristics of NC-B did not demonstrate toxicity against the evaluated cell lines HepG2 and MCF-7, antiviral effect against HSV-1, and the neurological effects in a stereotyping model were low and may be attributed to the per se effect of NC-B.
可生物降解的聚合物纳米胶囊 (NC) 作为药物纳米载体具有令人难以置信的特性,可优化药物靶向。然而,需要更详细地研究聚合物纳米粒子作为药物载体的单独作用。本工作旨在评估具有不同表面特性的空白 NC (NC-B) 在体外和体内的毒性的单独作用。NC1-B (聚山梨酯 80 包覆的聚 (ε-己内酯) NC)、NC2-B (聚乙二醇 6000 包覆的聚 (ε-己内酯) NC)、NC3-B (壳聚糖包覆的聚 (ε-己内酯) NC) 和 NC4-B (Eudragit® RS100 NC) 通过纳米沉淀法制备。通过粒径、Zeta 电位和 pH 值对配方进行了表征。对肿瘤细胞系 (HepG2 和 MCF-7) 进行了体外细胞毒性试验。通过 MTT 在感染 HSV-1 (KOS 株) 的 Vero 细胞中评估了抗病毒活性。在诱导 Wistar 大鼠阿扑吗啡诱导刻板行为的体内评价中,测量了运动活动距离、头部运动和竖起行为。NC1-B、NC2-B、NC3-B 和 NC4-B 的直径均小于 350nm。根据其涂层,配方的 pH 值和 Zeta 电位有所不同。对于抗肿瘤活性和抗病毒活性的体外评价,单因素方差分析显示细胞活力无显著差异。体内试验表明神经毒性较低。总之,NC-B 的不同表面特性对评估的 HepG2 和 MCF-7 细胞系没有表现出毒性、对 HSV-1 的抗病毒作用以及刻板模型中的神经毒性较低,这可能归因于 NC-B 的单独作用。