Lipid Technology and Engineering, College of Food Science and Engineering, Henan University of Technology, Lianhua Road 100, Zhengzhou 450001, Henan Province, PR China.
Lipid Technology and Engineering, College of Food Science and Engineering, Henan University of Technology, Lianhua Road 100, Zhengzhou 450001, Henan Province, PR China.
Int J Biol Macromol. 2023 Dec 31;253(Pt 2):126667. doi: 10.1016/j.ijbiomac.2023.126667. Epub 2023 Sep 1.
Surface modification of nanostructured lipid carriers (NLCs) can be an effective way to improve their oral delivery for active ingredients. In this study, four type of guar gum series modified NLCs for the delivery of phytosterols (PS) were constructed and the effects of the polysaccharides on their structure and physicochemical properties were studied. DLS and AFM results revealed that positively charged polysaccharides could bind to PS-NLCs through electrostatic attraction and made the complexes finally take positive charges, while negatively charged polysaccharides were more likely to fill in the gaps of NLC systems to achieve a balance between electrostatic repulsion and intermolecular forces. Although all four polysaccharides exhibited good storage stability and controlled release of PS in simulated intestinal digestion, PS-NLCs modified with partially hydrolyzed cationic guar gum (PHCG) at medium or high concentrations exhibited better gastric stability, mucoadhesion, and cellular uptake, which had considerable significance for improving the oral bioavailability of PS. This might be related to the coating structure of PHCG-PS-NLCs confirmed by AFM, FTIR, and Raman characterization. This study provide a reference value for designing suitable PS-NLC complexes without synthetic surfactants.
纳米结构化脂质载体 (NLCs) 的表面修饰可以是改善其活性成分口服递送的有效方法。在这项研究中，构建了四种类型的瓜尔胶系列改性 NLC 以递送植物甾醇 (PS)，并研究了多糖对其结构和物理化学性质的影响。DLS 和 AFM 结果表明，带正电荷的多糖可以通过静电吸引与 PS-NLC 结合，使复合物最终带正电荷，而带负电荷的多糖更有可能填充 NLC 系统的间隙，以实现静电排斥和分子间力之间的平衡。虽然所有四种多糖都表现出良好的储存稳定性和 PS 在模拟肠消化中的控制释放，但在中高浓度下用部分水解的阳离子瓜尔胶 (PHCG) 修饰的 PS-NLC 表现出更好的胃稳定性、黏膜黏附性和细胞摄取，这对于提高 PS 的口服生物利用度具有重要意义。这可能与 AFM、FTIR 和拉曼表征证实的 PHCG-PS-NLCs 的涂层结构有关。这项研究为设计不含合成表面活性剂的合适 PS-NLC 复合物提供了参考价值。
