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基于乙基纤维素的阳离子型硫醚的合成与表征及其用于制备黏膜黏附片剂和纳米粒。

Synthesis and Characterization of a Cationic Thiomer Based on Ethyl Cellulose for Realization of Mucoadhesive Tablets and Nanoparticles.

机构信息

Faculty of Pharmacy, Pancasila University, Srengseng Sawah, Jagakarsa, South Jakarta, 12640, Indonesia.

出版信息

Int J Nanomedicine. 2022 May 20;17:2321-2334. doi: 10.2147/IJN.S321467. eCollection 2022.

DOI:10.2147/IJN.S321467
PMID:35645561
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9130100/
Abstract

PURPOSE

Ethyl cellulose (EC) based nanoparticles are being extensively studied for their ability to achieve prolonged drug release and improve drug stability. Within this study, the thiolation of unmodified EC using cysteamine as a ligand was carried out to design nanoparticles with mucoadhesive properties and comparatively strong lipophilic properties.

METHODS

The thiolation was performed via oxidation and reductive amination, whereas the nanoparticles were generated via the ionic gelation followed by the precipitation method.

RESULTS

The number of free thiol groups on EC-cysteamine was in the range of 210-261 µmol per gram of polymer. Tablets based on EC-cysteamine demonstrated mucoadhesive properties 16.7-fold improved compared with those comprising unmodified EC. The mean diameter of the particles was in the range of 94-123 nm and the zeta potential was determined to be -7.97 to -14.70 mV. The nanoparticles remained attached to porcine intestinal mucosa for up to 36% after 3 h of incubation. The formation of nanoparticles improved the stability of EC-cysteamine conjugate against cellulase and provided a zero-order release. Moreover, both EC-cysteamine and the nanoparticles did not show any pronounced cytotoxicity.

CONCLUSION

Accordingly, EC-cysteamine nanoparticles could be a specific type of nanoparticulate delivery system with mucoadhesive properties. The amount of free thiol groups within EC-cysteamine nanoparticles together with their lipophilic properties could be further modified and modulated for a desired release behavior.

摘要

目的

乙基纤维素（EC）基纳米粒子因其能够实现药物的长效释放和提高药物稳定性而受到广泛研究。在本研究中，使用半胱氨酸作为配体对未修饰的 EC 进行巯基化，以设计具有黏膜黏附性能和相对较强亲脂性的纳米粒子。

方法

通过氧化和还原胺化进行巯基化，而纳米粒子则通过离子凝胶化随后沉淀法生成。

结果

EC-半胱氨酸上的游离巯基数量在每克聚合物 210-261µmol 的范围内。基于 EC-半胱氨酸的片剂与包含未修饰的 EC 的片剂相比，黏膜黏附性能提高了 16.7 倍。颗粒的平均直径在 94-123nm 范围内，zeta 电位为-7.97 至-14.70mV。纳米粒子在孵育 3 小时后仍附着在猪肠黏膜上，可达 36%。纳米粒子的形成提高了 EC-半胱氨酸缀合物对纤维素酶的稳定性，并提供了零级释放。此外，EC-半胱氨酸和纳米粒子均未表现出明显的细胞毒性。

结论

因此，EC-半胱氨酸纳米粒子可以是一种具有黏膜黏附性能的特殊类型的纳米颗粒给药系统。EC-半胱氨酸纳米粒子中的游离巯基数量及其亲脂性可以进一步修饰和调节，以获得所需的释放行为。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d860/9130100/6a878021200e/IJN-17-2321-g0011.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d860/9130100/8954b83099f6/IJN-17-2321-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d860/9130100/134a05c69118/IJN-17-2321-g0003.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d860/9130100/e14fa9d43433/IJN-17-2321-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d860/9130100/dbb516345315/IJN-17-2321-g0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d860/9130100/2cf1a4ec095a/IJN-17-2321-g0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d860/9130100/888ce556d7ba/IJN-17-2321-g0008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d860/9130100/6a878021200e/IJN-17-2321-g0011.jpg

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