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十八烷基三氯硅烷包埋的海藻酸钠微球作为小亲水分子的缓释载体。

Octadecyltrichlorosilane Incorporated Alginate Micro-granules as Sustained-Release Carriers for Small Hydrophilic Molecules.

机构信息

Department of Chemical and Biomolecular Engineering, The University of Akron, Akron, OH, 44325-3906, United States.

出版信息

Curr Drug Deliv. 2020;17(4):333-342. doi: 10.2174/1567201817666200210123328.

Abstract

BACKGROUND

Hydrogels are excellent drug carriers, but their inability to retain hydrophilic drugs for a prolonged period of time has greatly limited their usage. Research has mostly focused on intricate designs and manipulations of hydrogels to expand their applications in drug delivery.

OBJECTIVE

In this study, a simple approach by incorporating a hydrophobic agent, octadecyltrichlorosilane (OTS), to alginate hydrogel micro-granules (Alg-Ms), was investigated as an effective technique to prolong the release of small hydrophilic drugs.

METHODS

Sodium Benzoate (SB), a highly water-soluble antimicrobial and anti-inflammatory compound, was used as a model drug. The presence of hydrophobic OTS impeded swelling of these OTS incorporated Alg-Ms (OTS-Alg-Ms), hence sustaining the release of SB.

RESULT

The release data was fitted with Ritger-Peppas and Peppas-Sahlin models and the results showed that SB released from OTS-Alg-Ms with higher OTS content was mainly controlled by Fickian diffusion; with a lower OTS content, OTS-Alg-Ms swelled more easily, the combined diffusion and swelling led to a faster SB release.

CONCLUSION

Thus, by simply tuning the OTS concentration in the solution where Alg-Ms were briefly submerged in a predefined release period, from hours to a few days, small hydrophilic drugs from these OTS-Alg-Ms could be successfully achieved.

摘要

背景

水凝胶是一种出色的药物载体,但由于其无法长时间保留亲水性药物,因此其应用受到了极大限制。研究主要集中在对水凝胶进行复杂的设计和操作,以扩展其在药物输送中的应用。

目的

本研究通过将疏水剂十八烷基三氯硅烷(OTS)掺入藻酸盐水凝胶微颗粒(Alg-Ms)中,探索了一种简单的方法,以有效延长小分子亲水性药物的释放时间。

方法

以苯甲酸钠(SB)作为模型药物,它是一种高水溶性的抗菌和抗炎化合物。存在疏水性 OTS 会阻碍这些掺入 OTS 的 Alg-Ms(OTS-Alg-Ms)的溶胀,从而维持 SB 的释放。

结果

释放数据符合 Ritger-Peppas 和 Peppas-Sahlin 模型,结果表明,具有较高 OTS 含量的 OTS-Alg-Ms 中 SB 的释放主要受 Fickian 扩散控制;较低 OTS 含量的 OTS-Alg-Ms 更容易溶胀,扩散和溶胀的共同作用导致 SB 更快释放。

结论

因此,通过在 Alg-Ms 短暂浸入的溶液中简单地调整 OTS 浓度(在预定义的释放期内,从几小时到几天),可以成功地从这些 OTS-Alg-Ms 中释放小分子亲水性药物。

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