Puglia Carmelo, Lauro Maria Rosaria, Offerta Alessia, Crascì Lucia, Micicchè Lucia, Panico Anna Maria, Bonina Francesco, Puglisi Giovanni
Department of Drug Sciences, University of Catania, Catania, Italy.
Department of Pharmacy, University of Salerno, Fisciano (SA), Italy.
Planta Med. 2017 Mar;83(5):398-404. doi: 10.1055/s-0042-105293. Epub 2016 Apr 28.
Sesamol is a natural phenolic compound extracted from seed oil. Sesamol is endowed with several beneficial effects, but its use as a topical agent is strongly compromised by unfavorable chemical-physical properties. Therefore, to improve its characteristics, the aim of the present work was the formulation of nanostructured lipid carriers as drug delivery systems for topical administration of sesamol.Two different nanostructured lipid carrier systems have been produced based on the same solid lipid (Compritol® 888 ATO) but in a mixture with two different kinds of oil phase such as Miglyol® 812 (nanostructured lipid carrier-M) and sesame oil (nanostructured lipid carrier-PLUS). Morphology and dimensional distribution of nanostructured lipid carriers have been characterized by differential scanning calorimetry and photon correlation spectroscopy, respectively. The release pattern of sesamol from nanostructured lipid carriers was evaluated determining drug percutaneous absorption through excised human skin. Furthermore, an oxygen radical absorbance capacity assay was used to determine their antioxidant activity.From the results obtained, the method used to formulate nanostructured lipid carriers led to a homogeneous dispersion of particles in a nanometric range. Sesamol has been encapsulated efficiently in both nanostructured lipid carriers, with higher encapsulation efficiency values (> 90 %) when sesame oil was used as the oil phase (nanostructured lipid carrier-PLUS). evidences show that nanostructured lipid carrier dispersions were able to control the rate of sesamol diffusion through the skin, with respect to the reference formulations.Furthermore, the oxygen radical absorbance capacity assay pointed out an interesting and prolonged antioxidant activity of sesamol, especially when vehiculated by nanostructured lipid carrier-PLUS.
芝麻酚是一种从芝麻油中提取的天然酚类化合物。芝麻酚具有多种有益作用,但其作为局部用药因不良的化学物理性质而受到严重限制。因此,为改善其特性,本研究的目的是制备纳米结构脂质载体作为芝麻酚局部给药的药物递送系统。基于相同的固体脂质(Compritol® 888 ATO),但与两种不同的油相(Miglyol® 812,纳米结构脂质载体-M;芝麻油,纳米结构脂质载体-PLUS)混合,制备了两种不同的纳米结构脂质载体系统。分别通过差示扫描量热法和光子相关光谱法对纳米结构脂质载体的形态和尺寸分布进行了表征。通过测定药物经切除的人体皮肤的经皮吸收,评估了芝麻酚从纳米结构脂质载体中的释放模式。此外,使用氧自由基吸收能力测定法来确定其抗氧化活性。从所得结果来看,用于制备纳米结构脂质载体的方法导致颗粒在纳米范围内均匀分散。芝麻酚在两种纳米结构脂质载体中均被有效包封,当使用芝麻油作为油相时(纳米结构脂质载体-PLUS),包封效率更高(>90%)。有证据表明,相对于参比制剂,纳米结构脂质载体分散体能够控制芝麻酚通过皮肤的扩散速率。此外,氧自由基吸收能力测定法表明芝麻酚具有有趣且持久的抗氧化活性,尤其是当由纳米结构脂质载体-PLUS载运时。