Chitosan Oligosaccharide Modified Bovine Serum Albumin Nanoparticles for Improving Oral Bioavailability of Naringenin.

IF 2.8 4区医学 Q2 PHARMACOLOGY & PHARMACY

Current drug delivery Pub Date : 2024-01-01 DOI:10.2174/1567201820666230718143726

Ruiyue Fang, Yiqi Liao, Huishuang Qiu, Yuxin Liu, Shiyuan Lin, Hui Chen

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引用次数: 0

Abstract

Introduction: With the rapid development of nanotechnology, the research and development of nano-drugs have become one of the development directions of drug innovation. The encapsulation of the nanoparticles can change the biological distribution of the drug in vivo and improve the bioavailability of the drug in vivo. Naringenin is poorly soluble in water and has a low bioavailability, thus limiting its clinical application. The main purpose of this study was to develop a nano-sized preparation that could improve the oral bioavailability of naringenin.

Methods: Chitosan oligosaccharide modified naringenin-loaded bovine serum albumin nanoparticles (BSA-COS@Nar NPs) were prepared by emulsification solvent evaporation and electrostatic interaction. The nanoparticles were characterized by HPLC, laser particle size analyzer, transmission electron microscope and X-ray diffraction analysis. The release in vitro was investigated, and the behavior of nanoparticles in rats was also studied. The caco-2 cell model was established in vitro to investigate the cytotoxicity and cellular uptake of nanoparticles.

Results: BSA-COS@Nar NPs were successfully prepared, and the first-order release model was confirmed in vitro release. In vivo pharmacokinetic results indicated that the area under the drug concentration- time curve (AUC) of BSA-COS@Nar NPs was 2.37 times more than free naringenin. Cytotoxicity and cellular uptake results showed that BSA-COS@Nar NPs had no significant cytotoxic effect on Caco- 2 cells and promoted cellular uptake of the drug.

Conclusion: BSA-COS@Nar NPs could improve the in vivo bioavailability of naringenin.

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壳聚糖低聚糖修饰牛血清白蛋白纳米颗粒用于提高柚皮苷的口服生物利用度

导言：随着纳米技术的飞速发展，纳米药物的研究与开发已成为药物创新的发展方向之一。纳米颗粒的封装可以改变药物在体内的生物分布，提高药物在体内的生物利用度。柚皮苷难溶于水，生物利用度低，因此限制了其临床应用。本研究的主要目的是开发一种纳米级制剂，以提高柚皮苷的口服生物利用度：方法：通过乳化溶剂蒸发和静电作用制备了壳聚糖寡糖修饰的柚皮苷负载牛血清白蛋白纳米颗粒（BSA-COS@Nar NPs）。通过高效液相色谱、激光粒度分析仪、透射电子显微镜和 X 射线衍射分析对纳米颗粒进行了表征。研究了纳米颗粒在体外的释放情况，并对其在大鼠体内的行为进行了研究。在体外建立了 caco-2 细胞模型，以研究纳米颗粒的细胞毒性和细胞吸收：结果：成功制备了 BSA-COS@Nar NPs，体外释放证实了一阶释放模型。体内药代动力学结果表明，BSA-COS@Nar NPs的药物浓度-时间曲线下面积（AUC）是游离柚皮苷的2.37倍。细胞毒性和细胞吸收结果表明，BSA-COS@Nar NPs 对 Caco- 2 细胞无明显细胞毒性作用，并能促进细胞对药物的吸收：结论：BSA-COS@Nar NPs 可提高柚皮苷的体内生物利用度。

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

Current drug delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.10

自引率

4.20%

发文量

170

期刊介绍： Current Drug Delivery aims to publish peer-reviewed articles, research articles, short and in-depth reviews, and drug clinical trials studies in the rapidly developing field of drug delivery. Modern drug research aims to build delivery properties of a drug at the design phase, however in many cases this idea cannot be met and the development of delivery systems becomes as important as the development of the drugs themselves. The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance. The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.