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负载L-抗坏血酸和百里醌的壳聚糖纳米粒的合成与优化

Synthesis and Optimization of Chitosan Nanoparticles Loaded with L-Ascorbic Acid and Thymoquinone.

作者信息

Othman Nurhanisah, Masarudin Mas Jaffri, Kuen Cha Yee, Dasuan Nurul Azira, Abdullah Luqman Chuah, Md Jamil Siti Nurul Ain

机构信息

Department of Chemistry, Faculty of Science, Universiti Putra Malaysia, Serdang 43400, Selangor, Malaysia.

Department of Cell and Molecular Biology, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, Serdang 43400, Selangor, Malaysia.

出版信息

Nanomaterials (Basel). 2018 Nov 7;8(11):920. doi: 10.3390/nano8110920.

Abstract

The combination of compounds with different classes (hydrophobic and hydrophilic characters) in single chitosan carrier is a challenge due to the hydrophilicity of chitosan. Utilization of l-ascorbic acid (LAA) and thymoquinone (TQ) compounds as effective antioxidants is marred by poor bioavailability and uptake. Nanoparticles (NPs) solved the problem by functioning as a carrier for them because they have high surface areas for more efficient delivery and uptake by cells. This research, therefore, synthesized chitosan NPs (CNPs) containing LAA and TQ, CNP-LAA-TQ via ionic gelation routes as the preparation is non-toxic. They were characterized using electron microscopy, zetasizer, UV⁻VIS spectrophotometry, and infrared spectroscopy. The optimum CNP-LAA-TQ size produced was 141.5 ± 7.8 nm, with a polydispersity index (PDI) of 0.207 ± 0.013. The encapsulation efficiency of CNP-LAA-TQ was 22.8 ± 3.2% for LAA and 35.6 ± 3.6% for TQ. Combined hydrophilic LAA and hydrophobic TQ proved that a myriad of highly efficacious compounds with poor systemic uptake could be encapsulated together in NP systems to increase their pharmaceutical efficiency, indirectly contributing to the advancement of medical and pharmaceutical sectors.

摘要

由于壳聚糖具有亲水性,因此在单一壳聚糖载体中组合不同类别的化合物(具有疏水和亲水特性)是一项挑战。l-抗坏血酸(LAA)和百里醌(TQ)化合物作为有效的抗氧化剂,其生物利用度和摄取率较低,影响了它们的应用。纳米颗粒(NPs)通过作为它们的载体解决了这个问题,因为纳米颗粒具有高表面积,能更有效地被细胞递送和摄取。因此,本研究通过离子凝胶法合成了含有LAA和TQ的壳聚糖纳米颗粒(CNPs),即CNP-LAA-TQ,因为该制备方法无毒。使用电子显微镜、zeta电位仪、紫外可见分光光度法和红外光谱对它们进行了表征。所制备的最佳CNP-LAA-TQ尺寸为141.5±7.8 nm,多分散指数(PDI)为0.207±0.013。CNP-LAA-TQ对LAA的包封率为22.8±3.2%,对TQ的包封率为35.6±3.6%。亲水性的LAA和疏水性的TQ相结合证明,许多全身摄取性差但高效的化合物可以一起包裹在纳米颗粒系统中,以提高它们的药物效率,间接地推动医学和制药领域的发展。

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