Anantaworasakul Phunsuk, Chaiyana Wantida, Michniak-Kohn Bozena B, Rungseevijitprapa Wandee, Ampasavate Chadarat
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.
Innovation Center for Holistic Health, Nutraceuticals, and Cosmeceuticals, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.
Pharmaceutics. 2020 May 19;12(5):463. doi: 10.3390/pharmaceutics12050463.
The aim of this study was to develop lipid-based nanoparticles that entrapped a high concentration of capsaicin (0.25%) from a capsicum oleoresin extract. The solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were strategically fabricated to entrap capsaicin without a hazardous solvent. Optimized nanosize lipid particles with high capsaicin entrapment and loading capacity were achieved from pair-wise comparison of the solid lipid mixtures consisting of fatty esters and fatty alcohols, representing small and large crystal-structure molecules combined with a compatible liquid lipid and surfactants (crystallinity index = 3%). This report was focused on selectively captured capsaicin from oleoresin in amorphous chili extract-loaded NLCs with 85.27% ± 0.12% entrapment efficiency (EE) and 8.53% ± 0.01% loading capacity (LC). The particle size, polydispersity index, and zeta potential of chili extract-loaded NLCs were 148.50 ± 2.94 nm, 0.12 ± 0.03, and -29.58 ± 1.37 mV, respectively. The favorable zero-order kinetics that prolonged capsaicin release and the significantly faster transdermal penetration of the NLC attributed to the reduction in skin irritation of the concentrated capsaicin NLCs, as illustrated by the in vitro EpiDerm three-dimensional human skin irritation test and hen's egg test chorioallantoic membrane assay (HET-CAM).
本研究的目的是开发基于脂质的纳米颗粒，其能从辣椒油树脂提取物中包封高浓度的辣椒素（0.25%）。固态脂质纳米粒（SLNs）和纳米结构脂质载体（NLCs）经过精心制备，以在无有害溶剂的情况下包封辣椒素。通过对由脂肪酸酯和脂肪醇组成的固态脂质混合物进行两两比较，获得了具有高辣椒素包封率和载药量的优化纳米尺寸脂质颗粒，其中脂肪酸酯和脂肪醇分别代表大小不同的晶体结构分子，并与相容的液态脂质和表面活性剂结合（结晶度指数 = 3%）。本报告重点关注从无定形辣椒提取物负载的NLCs中的辣椒油树脂中选择性捕获辣椒素，其包封率（EE）为85.27% ± 0.12%，载药量（LC）为8.53% ± 0.01%。负载辣椒提取物的NLCs的粒径、多分散指数和zeta电位分别为148.50 ± 2.94 nm、0.12 ± 0.03和 -29.58 ± 1.37 mV。体外EpiDerm三维人体皮肤刺激性试验和鸡胚绒毛尿囊膜试验（HET-CAM）表明，NLCs具有良好的零级动力学，可延长辣椒素释放，且其经皮渗透明显更快，这归因于浓缩辣椒素NLCs对皮肤刺激性的降低。
