Vitamin B3 Containing Polymers for Nanodelivery

IF 4.4 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Prosper P. Mapfumo, Jana I. Solomun, Friedrich Becker, Elisabeth Moek, Meike N. Leiske, Lenhard K. Rudolph, Johannes C. Brendel, Anja Traeger
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Abstract

Polymeric nanoparticles (NPs) with an integrated dual delivery system enable the controlled release of bioactive molecules and drugs, providing therapeutic advantages. Key design targets include high biocompatibility, cellular uptake, and encapsulating efficiency. In this study, a polymer library derived from niacin, also known as vitamin B3 is synthesized. The library comprises poly(2-(acryloyloxy)ethyl nicotinate) (PAEN), poly(2-acrylamidoethyl nicotinate) (PAAEN), and poly(N-(2-acrylamidoethyl)nicotinamide) (PAAENA), with varying hydrophilicity in the backbone and pendant group linker. All polymers are formulated, and those with increased hydrophobicity yield NPs with homogeneous spherical distribution and diameters below 150 nm, as confirmed by scanning electron microscopy and dynamic light scattering. Encapsulation studies utilizing a model drug, neutral lipid orange (NLO), reveal the influence of polymer backbone on encapsulation efficiency. Specifically, efficiencies of 46% and 96% are observed with acrylate and acrylamide backbones, respectively. Biological investigations showed that P(AEN) and P(AAEN) NPs are non-toxic up to 300 µg mL−1, exhibit superior cellular uptake, and boost cell metabolic activity. The latter is attributed to the cellular release of niacin, a precursor to nicotinamide adenine dinucleotide (NAD), a central coenzyme in metabolism. The results underline the potential of nutrient-derived polymers as pro-nutrient and drug-delivery materials.

Abstract Image

用于纳米输送的含维生素 B3 的聚合物。
集成了双重给药系统的聚合物纳米粒子可促进生物活性分子和药物的控制释放,具有治疗优势。关键的设计目标包括高生物相容性、细胞吸收和封装效率。在这项研究中,我们合成了一个多样化的聚合物库,该聚合物库源自烟酸,这是一种与代谢途径和疗法密不可分的维生素 B3。该库由聚(2-(丙烯酰氧基)乙基烟酸酯)、聚(2-丙烯酰胺基乙基烟酸酯)和聚(N-(2-丙烯酰胺基乙基)烟酰胺)组成。经动态光散射和扫描电子显微镜分别确认,疏水性较高的聚合物配制成的纳米颗粒直径小于 150 纳米,呈均匀球形分布。使用模型药物中性脂质橙(NLO)进行的封装研究表明,聚合物骨架对效率有显著影响,酯骨架的影响范围为 46%,丙烯酰胺骨架的影响范围为 96%。生物学研究表明,这些纳米颗粒在 300 µg mL-1 以下无毒,并表现出卓越的细胞吸收能力。有趣的是,聚(2-(丙烯酰氧基)乙基烟酸酯)和聚(2-丙烯酰胺基乙基烟酸酯)提高了细胞的代谢活性。这是因为细胞释放了烟酸,烟酸是烟酰胺腺嘌呤二核苷酸(NAD)的前体,而NAD是新陈代谢的核心辅酶。研究结果凸显了营养素衍生聚合物作为营养素和药物输送材料的潜力。本文受版权保护。保留所有权利。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Macromolecular bioscience
Macromolecular bioscience 生物-材料科学:生物材料
CiteScore
7.90
自引率
2.20%
发文量
211
审稿时长
1.5 months
期刊介绍: Macromolecular Bioscience is a leading journal at the intersection of polymer and materials sciences with life science and medicine. With an Impact Factor of 2.895 (2018 Journal Impact Factor, Journal Citation Reports (Clarivate Analytics, 2019)), it is currently ranked among the top biomaterials and polymer journals. Macromolecular Bioscience offers an attractive mixture of high-quality Reviews, Feature Articles, Communications, and Full Papers. With average reviewing times below 30 days, publication times of 2.5 months and listing in all major indices, including Medline, Macromolecular Bioscience is the journal of choice for your best contributions at the intersection of polymer and life sciences.
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