Department of Chemical and Biomolecular Engineering, The University of Akron, Akron, OH, 44325-3906, United States.
Curr Drug Deliv. 2020;17(4):333-342. doi: 10.2174/1567201817666200210123328.
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.
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.
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.
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.
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.
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。
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。
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。
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。
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。