Microgels of alginate dialdehyde with WGA lectin conjugate for curcumin encapsulation

IF 4.9 3区 医学 Q1 PHARMACOLOGY & PHARMACY Journal of Drug Delivery Science and Technology Pub Date : 2025-02-21 DOI:10.1016/j.jddst.2025.106717
Arlina Prima Putri , Marissa Angelina , Mochamad Chalid , Francesco Picchioni , Hero Jan Heeres
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Abstract

Wheat germ agglutinin (WGA) is a plant-lectin that is potentially attractive to be used in the formulation of drug delivery systems. In this study, we report the synthesis and use of this lectin in a microgel formulation together with a modified alginate for drug delivery purposes. The alginate used in the formulation was obtained by oxidation of Na-alginate and contains reactive aldehyde groups (ADA). These aldehyde groups are essential and able to form a conjugate with lectin (ADAWGA) using a reductive amination protocol. 1H NMR, DOSY, and ATR-FTIR were performed to characterize ADAWGA and confirm that the reaction is successful. Microgels based on ADAWGA were prepared by a micro emulsion technique utilizing calcium chloride as a crosslinking agent. For comparison, microgels with only the alginate and alginates in combination with ADA were also prepared. Microgels with average particle sizes ranging from 285 to 529 nm were obtained. The microgels were loaded with curcumin, a hydrophobic natural polyphenol, and the release pattern was investigated. The result of the release profiles from the curcumin-loaded microgels shown that the profile was fit the Higuchi model, whit the R2 values range from 0.90 to 0.98. Cytotoxicity studies revealed that the microgels exhibit low toxicity toward the MCF-7 cells at low concentrations, making them suitable for drug delivery application.

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海藻酸双醛与WGA凝集素偶联的姜黄素包封微凝胶
小麦胚芽凝集素(WGA)是一种具有潜在吸引力的植物凝集素,可用于药物输送系统的制剂。在这项研究中,我们报道了这种凝集素的合成和微凝胶制剂的使用,连同修饰海藻酸盐用于药物递送目的。配方中使用的海藻酸钠是由海藻酸钠氧化得到的,含有活性醛(ADA)。这些醛基是必需的,能够形成与凝集素(ADAWGA)结合使用还原性胺化协议。1H NMR, DOSY和ATR-FTIR对ADAWGA进行了表征,并证实了该反应是成功的。以氯化钙为交联剂,采用微乳液法制备了ADAWGA微凝胶。为了比较,还制备了仅含海藻酸盐的微凝胶和海藻酸盐与ADA复合的微凝胶。得到了平均粒径为285 ~ 529 nm的微凝胶。在微凝胶中加入疏水的天然多酚姜黄素,并研究其释放模式。姜黄素微凝胶的释放曲线符合Higuchi模型,R2值在0.90 ~ 0.98之间。细胞毒性研究表明,微凝胶在低浓度下对MCF-7细胞表现出低毒性,使其适合于药物递送应用。
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来源期刊
CiteScore
8.00
自引率
8.00%
发文量
879
审稿时长
94 days
期刊介绍: The Journal of Drug Delivery Science and Technology is an international journal devoted to drug delivery and pharmaceutical technology. The journal covers all innovative aspects of all pharmaceutical dosage forms and the most advanced research on controlled release, bioavailability and drug absorption, nanomedicines, gene delivery, tissue engineering, etc. Hot topics, related to manufacturing processes and quality control, are also welcomed.
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