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一种源自种子的智能水凝胶:pH响应性、开关切换、药物持续释放及转运检测

A Smart Hydrogel from Seeds: pH Responsiveness, On-off Switching, Sustained Drug Release, and Transit Detection.

作者信息

Ali Arshad, Hussain Muhammad Ajaz, Haseeb Muhammad Tahir, Bukhari Syed Nasir Abbas, Muhammad Gulzar, Sheikh Fatima Akbar, Farid-Ul-Haq Muhammad, Ahmad Naveed

机构信息

Institute of Chemistry, University of Sargodha, Sargodha 40100, Pakistan.

College of Pharmacy, University of Sargodha, Sargodha 40100, Pakistan.

出版信息

Curr Drug Deliv. 2023;20(3):292-305. doi: 10.2174/1567201819666220509200019.

DOI:10.2174/1567201819666220509200019
PMID:35579145
Abstract

BACKGROUND

The use of synthetic and semi-synthetic materials in drug delivery systems has associated drawbacks like costly synthesis, toxicity, and biocompatibility issues. Therefore, there is a need to introduce novel materials to overcome such issues. Naturally occurring and water-swellable polysaccharides are advantageous in overcoming the above-mentioned issues. Therefore, we are reporting a novel hydrogel (SSH) isolated from the seeds of Salvia spinosa as a sustained release material.

METHODS

SSH was explored for its pH-dependent and salt-responsive swelling before and after compression in a tablet form. Stimuli-responsive swelling and deswelling were also monitored at pH 7.4 and pH 1.2 in deionized water (DW) and normal saline and DW and ethanol. The sustained-release potential of SSH-based tablets was monitored at gastrointestinal tract (GIT) pH. The transit of SSH tablets was ascertained through an X-ray study.

RESULTS

The swelling of SSH in powder and tablet form was found in the order of DW > pH 7.4 > pH 6.8 > pH 1.2. An inverse relation was found between the swelling of SSH and the concentration of the salt solution. The SSH showed stimuli-responsive swelling and de-swelling before and after compression, indicating the unaltered nature of SSH even in a closely packed form, i.e., tablets. Sustained release of theophylline (< 80%) was witnessed at pH 6.8 and 7.4 during the 12 h study following zeroorder kinetics, and radiographic images also showed 9 h retention in GIT.

CONCLUSION

These investigations showed the potential of SSH as a pH-sensitive material for sustained and targeted drug delivery.

摘要

背景

在药物递送系统中使用合成材料和半合成材料存在一些相关缺点,如合成成本高、毒性以及生物相容性问题。因此,需要引入新型材料来克服这些问题。天然存在的且具有水溶胀性的多糖在克服上述问题方面具有优势。因此,我们报道了一种从刺萼鼠尾草种子中分离出的新型水凝胶(SSH)作为一种缓释材料。

方法

研究了片剂形式的SSH在压缩前后的pH依赖性和盐响应性溶胀。还在pH 7.4和pH 1.2的去离子水(DW)、生理盐水以及DW和乙醇中监测了刺激响应性溶胀和消溶胀情况。在胃肠道(GIT)pH值下监测了基于SSH的片剂的缓释潜力。通过X射线研究确定了SSH片剂的转运情况。

结果

发现粉末状和片剂形式的SSH溶胀顺序为DW > pH 7.4 > pH 6.8 > pH 1.2。SSH的溶胀与盐溶液浓度之间呈反比关系。SSH在压缩前后均表现出刺激响应性溶胀和消溶胀,这表明即使在紧密堆积形式(即片剂)下,SSH的性质也未改变。在12小时的研究中,在pH 6.8和7.4时,茶碱的缓释率(< 80%)符合零级动力学,并且射线图像也显示在胃肠道中保留了9小时。

结论

这些研究表明SSH作为一种pH敏感材料在持续和靶向药物递送方面具有潜力。

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