Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, 65000, Thailand.
The Center of Excellence for Innovation in Chemistry (PERCH-CIC), Commission on High Education, Ministry of Education, Phitsanulok, Thailand.
J Biomed Mater Res B Appl Biomater. 2018 Feb;106(2):734-741. doi: 10.1002/jbm.b.33884. Epub 2017 Mar 21.
This study aimed to compare the intestinal permeation of curcumin-loaded polymer coated nanostructured lipid carriers (NLCs) and uncoated NLCs using the Caco-2 cell model. The uncoated NLCs were prepared using a warm microemulsion technique, while polymer-coated NLCs were prepared with the same method but were followed by coating particle surface with polyethylene glycol (PEG) 400 or polyvinyl alcohol (PVA). After lyophilization, all formulations possessed a mean size of <400 nm with a zeta potential of ∼-30 mV and a high entrapment efficacy up to 90%. All NLCs formulation showed significantly improvement in curcumin water solubility, more than 60-folds as compared to curcumin dispersion. In addition, they could protect curcumin from degradation in basic pH, 90% curcumin remaining after 6 h incubation in culture medium. In vitro permeation studies revealed that PEG-NLCs and PVA-NLCs provided significantly higher apparent permeation coefficient (P ) value than uncoated NLCs. Moreover, after 6 months storage at 4 °C in the absence of sunlight, the physical, and chemical stabilities of the lyophilized curcumin-loaded polymer coated NLCs and uncoated NLCs could be maintained, i.e., the mean particle size and the amount of curcumin showed no significant changes (p > 0.05) compared to those freshly prepared formulations. Considered overall, polymer coated NLCs are an important strategy to improve the oral bioavailability of curcumin. © 2017 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 106B: 734-741, 2018.
本研究旨在使用 Caco-2 细胞模型比较姜黄素负载聚合物包被纳米结构脂质载体（NLC）和未包被 NLC 的肠道渗透。未包被的 NLC 是通过温微乳液技术制备的，而聚合物包被的 NLC 是用相同的方法制备的，但随后在粒子表面涂覆聚乙二醇（PEG）400 或聚乙烯醇（PVA）。冷冻干燥后，所有制剂的平均粒径均<400nm，表面电位约为-30mV，包封效率高达 90%。所有 NLC 制剂均显著提高了姜黄素的水溶性，比姜黄素分散体高 60 多倍。此外，它们可以保护姜黄素在碱性 pH 下降解，在培养基中孵育 6 小时后仍有 90%的姜黄素残留。体外渗透研究表明，PEG-NLC 和 PVA-NLC 提供的表观渗透系数（P）值明显高于未包被的 NLC。此外，在 4°C 避光条件下储存 6 个月后，冻干的载姜黄素聚合物包被的 NLC 和未包被的 NLC 的物理和化学稳定性得以维持，即与新鲜制备的制剂相比，平均粒径和姜黄素的量没有明显变化（p>0.05）。总体考虑，聚合物包被的 NLC 是提高姜黄素口服生物利用度的重要策略。©2017 年威利期刊公司。生物医学材料研究杂志 B：应用生物材料，106B：734-741，2018。
