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首页> 美国卫生研究院文献>International Journal of Nanomedicine >Fabrication appraisal and transdermal permeation of sildenafil citrate-loaded nanostructured lipid carriers versus solid lipid nanoparticles
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Fabrication appraisal and transdermal permeation of sildenafil citrate-loaded nanostructured lipid carriers versus solid lipid nanoparticles

机译：枸sil酸西地那非纳米脂质载体与固体脂质纳米粒的制备鉴定和透皮渗透

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Although sildenafil citrate (SC) is used extensively for erectile dysfunction, oral delivery of SC encounters many obstacles. Furthermore, the physicochemical characteristics of this amphoteric drug are challenging for delivery system formulation and transdermal permeation. This article concerns the assessment of the potential of nanomedicine for improving SC delivery and transdermal permeation. SC-loaded nanostructured lipid carriers (NLCs) and solid lipid nanoparticles (SLNs) were fabricated using a modified high-shear homogenization technique. Nanoparticle optimization steps included particle size analysis, entrapment efficiency (EE) determination, freeze-drying and reconstitution, differential scanning calorimetry, in vitro release, stability study and high-performance liquid chromatography analysis. Transdermal permeation of the nanocarriers compared with SC suspension across human skin was assessed using a modified Franz diffusion cell assembly. Results revealed that SLNs and NLCs could be optimized in the nanometric range (180 and 100 nm, respectively) with excellent EE (96.7% and 97.5%, respectively). Nanoparticles have significantly enhanced in vitro release and transdermal permeation of SC compared with its suspensions. Furthermore, transdermal permeation of SC exhibited higher initial release from both SLN and NLC formulations followed by controlled release, with promising implications for faster onset and longer drug duration. Nanomedicines prepared exhibited excellent physical stability for the study period. Solid nanoparticles optimized in this study successfully improved SC characteristics, paving the way for an efficient topical Viagra® product.
机译：尽管枸sil酸西地那非（SC）被广泛用于勃起功能障碍，但口服SC遇到许多障碍。此外，该两性药物的物理化学特性对于递送系统制剂和透皮渗透是具有挑战性的。本文涉及对纳米药物改善SC传递和透皮渗透的潜力的评估。使用改良的高剪切均质化技术制备了负载SC的纳米结构脂质载体（NLC）和固体脂质纳米颗粒（SLN）。纳米颗粒的优化步骤包括粒度分析，包封率（EE）测定，冷冻干燥和重构，差示扫描量热法，体外释放，稳定性研究和高效液相色谱分析。使用改良的Franz扩散池组件评估了纳米载体与SC悬浮液在人皮肤上的透皮渗透性。结果表明，SLN和NLC可以在纳米级（分别为180和100 nm）中得到最佳的EE（分别为96.7％和97.5％）优化。与悬浮液相比，纳米颗粒显着增强了SC的体外释放和透皮渗透。此外，SC的透皮渗透表现出从SLN和NLC制剂中较高的初始释放，然后是受控释放，对于更快的起效和更长的药物持续时间有希望的暗示。在研究期间，制备的纳米药物表现出优异的物理稳定性。在这项研究中优化的固体纳米颗粒成功改善了SC特性，为高效的局部伟哥®产品铺平了道路。

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