含有美金刚、他克林和肉桂酸的聚合物药物偶联物:治疗阿尔茨海默病的有前途的纳米疗法。

IF 3 4区医学 Q2 CHEMISTRY, APPLIED

Journal of microencapsulation Pub Date : 2023-01-01 DOI:10.1080/02652048.2023.2167011

Tobeka Naki, William Morwa Reagile Matshe, Mohammed Olusegun Balogun, Suprakas Sinha Ray, Samuel Ayodele Egieyeh, Blessing Atim Aderibigbe

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引用次数: 0

摘要

目的:制备含有美金刚、他卡因和E)- n -(3-氨基丙基)肉桂酸的聚合物-药物偶联物，这是一种治疗神经退行性疾病的有前景的药物。方法:采用1HNMR、粒度分析、SEM、LC-MS、TEM/EDX、XRD等方法对其进行表征，并进行体外抗乙酰胆碱酯酶和药物释放研究。结果:1H NMR分析显示药物偶联成功，药物质量百分比在1.3 ~ 6.0% w/w范围内。药物在20-36%范围内持续释放10 h。结合物对乙酰胆碱酯酶(AChE)活性的抑制作用显著，IC50值在13 ~ 44.4µm范围内，优于他克林(IC50 =1698.8µm)。对接研究进一步证实，将药物偶联到聚合物中可以提高其抗乙酰胆碱酯酶活性。结论:药物释放谱、颗粒大小和体外研究表明，缀合物是治疗神经退行性疾病的有希望的治疗药物。

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Polymer drug conjugates containing memantine, tacrine and cinnamic acid: promising nanotherapeutics for the treatment of Alzheimer's disease.

Aim: To prepare polymer-drug conjugates containing a combination of memantine, tacrine, and E)-N-(3-aminopropyl)cinnamide, promising therapeutics for the treatment of neurodegenerative disorders.

Methods: The conjugates were characterised by ¹HNMR, particle size analysis, SEM, LC-MS, TEM/EDX, and XRD, followed by in vitro anti-acetylcholinesterase and drug release studies.

Results: ¹H NMR analysis revealed successful drug conjugation with drug mass percentages in the range of 1.3-6.0% w/w. The drug release from the conjugates was sustained for 10 h in the range of 20-36%. The conjugates' capability to inhibit acetylcholinesterase (AChE) activity was significant with IC₅₀ values in the range of 13-44.4 µm which was more effective than tacrine (IC₅₀ =1698.8 µm). The docking studies further confirmed that the conjugation of the drugs into the polymer improved their anti-acetylcholinesterase activity.

Conclusion: The drug release profile, particle sizes, and in vitro studies revealed that the conjugates are promising therapeutics for treating neurodegenerative disorders.

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来源期刊

Journal of microencapsulation 工程技术-工程：化工

CiteScore

6.30

自引率

2.60%

发文量

审稿时长

3 months

期刊介绍： The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.