Department of Pharmaceutics, School of Pharmacy, Hamadan University of Medical Sciences, Hamadan, Iran.
Department of Pharmacology and Toxicology, Hamadan University of Medical Sciences, Hamadan, Iran.
Drug Dev Ind Pharm. 2020 Jul;46(7):1163-1176. doi: 10.1080/03639045.2020.1779286. Epub 2020 Jun 18.
Propolis is a natural resinous product and exerts anti-inflammatory properties. The aim of this study is formulation and characterization of solid lipid nanoparticles (SLNs) encapsulating propolis flavonoids (PFs), intended for topical treatment of skin edema. The nanoparticles were prepared and statistically optimized using Box-Behnken response surface methodology. The release profile of the optimized nanoparticles was investigated. Cytotoxicity of nanoparticles on HSF-PI 18 cell line was determined. Permeation and penetration of nanoparticles across the incised skin were measured. Finally, the nanoparticles were incorporated into a pharmaceutical hydrogel formulation and the efficacy in reduction of skin edema was determined. The size, PdI, zeta potential, entrapment efficiency (EE%) and loading efficiency (LE %) of the optimized nanoparticles were 111.3 ± 19.35 nm, 0.34 ± 0.005, -24.17 ± 3.3 mV, 73.5 ± 0.86%, and 3.2 ± 0.27%, respectively. Data obtained through release study suggested a burst release followed by a prolonged release behavior up to 24 h post incubation time interval. The prepared SLNs exhibited no cytotoxicity on HSF-PI 18 cell line. permeation and penetration study of nanoparticles across the incised skin showed approximately a 2.5-fold and a 3-fold increase in cumulative amount of transport and cumulative amount of skin penetration, respectively. Finally, studies in rat models, showed a threefold reduction in volume of the edema in animals treated with SLNs. The obtained data revealed that the prepared SNs entrapping PFs, exert high skin targeting effects, prolonged anti-inflammatory properties and therefore high efficiency in treatment of skin edema.
蜂胶是一种天然的树脂状产物，具有抗炎特性。本研究的目的是制备并表征包封蜂胶类黄酮（PFs）的固体脂质纳米粒（SLNs），用于皮肤水肿的局部治疗。使用 Box-Behnken 响应面法对纳米粒进行了制备和统计学优化。考察了优化纳米粒的释放特性。测定了纳米粒对 HSF-PI 18 细胞系的细胞毒性。测量了纳米粒穿过切开皮肤的渗透和穿透。最后，将纳米粒掺入药用水凝胶制剂中，并测定其减少皮肤水肿的功效。优化后的纳米粒的粒径、PdI、Zeta 电位、包封效率（EE%）和载药量（LE%）分别为 111.3±19.35nm、0.34±0.005、-24.17±3.3mV、73.5±0.86%和 3.2±0.27%。通过释放研究获得的数据表明，在孵育时间间隔 24 小时后，存在突释随后是延长释放行为。所制备的 SLNs 对 HSF-PI 18 细胞系无细胞毒性。纳米粒穿过切开皮肤的渗透和穿透研究表明，累积传输量和累积皮肤穿透量分别增加了约 2.5 倍和 3 倍。最后，在大鼠模型中的研究表明，用 SLNs 治疗的动物的水肿体积减少了三倍。所得数据表明，包封 PFs 的 SNs 具有高皮肤靶向作用、延长抗炎特性，因此在治疗皮肤水肿方面具有高效性。
