Synthesis and characterization of fullerene-based nanocarrier for targeted delivery of quercetin to the brain.

IF 3 Q2 PHARMACOLOGY & PHARMACY Therapeutic delivery Pub Date : 2024-01-01 Epub Date: 2024-09-05 DOI:10.1080/20415990.2024.2365620
Amit Kumar Palai, Amit Kumar, Farhan Mazahir, Ankita Sharma, Awesh K Yadav
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Abstract

Aim: Preparation of quercetin fullerene conjugate (QFC) for nose-to-brain delivery and their in vitro and ex vivo characterizations.Methods: Carboxylated fullerene was converted into acetylated fullerene and quercetin was conjugated and physically adsorbed on acetylated fullerene.Results: The particle size and zeta potential of QFC and chitosan-coated QFC (CC-QFC) were found to be 179.2 ± 1.10, 293.4 ± 2.757, -5.28 ± 1.43 and 11.6 ± 0.4 respectively. The entrapment efficiency, loading efficiency of QFC were found to be 85.55% and 42.77%. The MTT assay revealed 80.69% SH-SY5Y cell viability at a concentration of 50 μg/ml. CC-QFC showed remarkable (89.20%) ex vivo mucoadhesive properties compared with QFC (66.67%). Further study showed no significant ciliotoxicity by CC-QFC.Conclusion: The obtained results suggested the potential of CC-QFC for treatment in Alzheimer's disease.

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用于向大脑定向输送槲皮素的富勒烯基纳米载体的合成与表征。
目的:制备用于鼻脑给药的槲皮素富勒烯共轭物(QFC)及其体内外表征:方法:将羧化富勒烯转化为乙酰化富勒烯,将槲皮素共轭并物理吸附在乙酰化富勒烯上:QFC和壳聚糖包覆QFC(CC-QFC)的粒度和ZETA电位分别为179.2 ± 1.10、293.4 ± 2.757、-5.28 ± 1.43和11.6 ± 0.4。QFC 的夹带效率和负载效率分别为 85.55% 和 42.77%。MTT 检测显示,浓度为 50 μg/ml 的 SH-SY5Y 细胞存活率为 80.69%。与 QFC(66.67%)相比,CC-QFC 的体外粘附性更强(89.20%)。进一步研究表明,CC-QFC 没有明显的纤毛毒性:结论:研究结果表明,CC-QFC 具有治疗阿尔茨海默病的潜力。
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来源期刊
Therapeutic delivery
Therapeutic delivery PHARMACOLOGY & PHARMACY-
CiteScore
5.50
自引率
0.00%
发文量
25
期刊介绍: Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.
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