Shen Jing, Zhang Jiangtao, Wu Weitai, Banerjee Probal, Zhou Shuiqin
Department of Chemistry of The College of Staten Island and PhD Program in Chemistry of Graduate Center, The City University of New York, 2800 Victory Boulevard, Staten Island, NY 10314, USA.
Department of Chemistry, Yunnan Normal University, Kunming 650092, China.
Gels. 2023 Sep 18;9(9):762. doi: 10.3390/gels9090762.
Curcumin, a nontoxic and cheap natural medicine, has high therapeutic efficacy for many diseases, including diabetes and cancers. Unfortunately, its exceedingly low water-solubility and rapid degradation in the body severely limit its bioavailability. In this work, we prepare a series of biocompatible poly(vinyl anisole)@nonlinear poly(ethylene glycol) (PVAS@PEG) core-shell nanogels with different PEG gel shell thickness to provide high water solubility, good stability, and controllable sustained release of curcumin. The PVAS nanogel core is designed to attract and store curcumin molecules for high drug loading capacity and the hydrophilic nonlinear PEG gel shell is designed to offer water dispersibility and thermo-responsive drug release. The nanogels prepared are monodispersed in a spherical shape with clear core-shell morphology. The size and shell thickness of the nanogels can be easily controlled by changing the core-shell precursor feeding ratios. The optimized PVAS@PEG nanogels display a high curcumin loading capacity of 38.0 wt%. The nanogels can stabilize curcumin from degradation at pH = 7.4 and release it in response to heat within the physiological temperature range. The nanogels can enter cells effectively and exhibit negligible cytotoxicity to both the B16F10 and HL-7702 cells at a concentration up to 2.3 mg/mL. Such designed PVAS@PEG nanogels have great potential to be used for efficient drug delivery.
姜黄素是一种无毒且廉价的天然药物，对包括糖尿病和癌症在内的多种疾病具有很高的治疗效果。不幸的是，其极低的水溶性和在体内的快速降解严重限制了其生物利用度。在这项工作中，我们制备了一系列具有不同聚乙二醇（PEG）凝胶壳厚度的生物相容性聚（乙烯基苯甲醚）@非线性聚（乙二醇）（PVAS@PEG）核壳纳米凝胶，以提供高水溶性、良好的稳定性以及姜黄素的可控缓释。PVAS纳米凝胶核被设计用于吸引和储存姜黄素分子以实现高载药量，而亲水性非线性PEG凝胶壳则被设计用于提供水分散性和热响应性药物释放。所制备的纳米凝胶呈单分散球形，具有清晰的核壳形态。通过改变核壳前驱体进料比，可以轻松控制纳米凝胶的尺寸和壳厚度。优化后的PVAS@PEG纳米凝胶显示出38.0 wt%的高姜黄素载药量。纳米凝胶可以在pH = 7.4时稳定姜黄素不被降解，并在生理温度范围内响应热而释放姜黄素。纳米凝胶能够有效地进入细胞，并且在浓度高达2.3 mg/mL时对B16F10和HL - 7702细胞均表现出可忽略不计的细胞毒性。这种设计的PVAS@PEG纳米凝胶在高效药物递送方面具有巨大的应用潜力。
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