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一种源自艾草种子的具有刺激响应性、高孔隙率且无毒的智能水凝胶:刺激响应性溶胀/去溶胀、智能药物递送及增强醋氯芬酸的生物利用度。

A stimuli-responsive, superporous and non-toxic smart hydrogel from seeds of mugwort (): stimuli responsive swelling/deswelling, intelligent drug delivery and enhanced aceclofenac bioavailability.

作者信息

Farid-Ul-Haq Muhammad, Hussain Muhammad Ajaz, Haseeb Muhammad Tahir, Ashraf Muhammad Umer, Hussain Syed Zajif, Tabassum Tahira, Hussain Irshad, Sher Muhammad, Bukhari Syed Nasir Abbas, Naeem-Ul-Hassan Muhammad

机构信息

Department of Chemistry, University of Sargodha Sargodha 40100 Pakistan

College of Pharmacy, University of Sargodha Sargodha 40100 Pakistan.

出版信息

RSC Adv. 2020 May 27;10(34):19832-19843. doi: 10.1039/d0ra03176c. eCollection 2020 May 26.

Abstract

seeds extrude hydrogel (AVH), which shows extraordinary swelling in water, at pH 6.8, and 7.4, which follows second-order kinetics. AVH exhibits reversible swelling/deswelling in ethanol and normal saline as well at pH 7.4 and pH 1.2. Therefore, AVH shows stimuli-responsiveness in different physiological conditions, solvents, and electrolytes. The superporous nature of AVH in swollen/freeze-dried sculpture is exposed in their SEM micrographs. AVH-based aceclofenac tablet formulations offer sustained-release under simulated conditions of the gastrointestinal tract (GIT) in terms of pH and transit time. Pharmacokinetic studies also show the delay and prolonged plasma concentration with of 8 h, therefore, such formulations can be used to enhance the bioavailability of aceclofenac. The swelling behavior of the AVH tablet is also assessed using MRI. The fate of the AVH tablet is monitored by X-ray during the transit through the GIT. Acute toxicity studies of AVH indicate the absence of any toxicity which reveals the safety profile of AVH. Therefore, AVH can be used for oral, topical and ophthalmic drug delivery systems. These results establish the potential of AVH as a stimuli sensitive, pH-dependent, and sustained-release biomaterial for targeted drug delivery.

摘要

种子挤出的水凝胶(AVH)在水、pH值为6.8和7.4的条件下表现出非凡的溶胀,遵循二级动力学。AVH在乙醇、生理盐水以及pH值为7.4和1.2的条件下表现出可逆的溶胀/去溶胀。因此,AVH在不同的生理条件、溶剂和电解质中表现出刺激响应性。AVH在溶胀/冻干雕塑中的超大孔性质在其扫描电子显微镜图像中得以展现。基于AVH的醋氯芬酸片剂制剂在胃肠道(GIT)模拟条件下,就pH值和转运时间而言,呈现出缓释效果。药代动力学研究还表明,其血浆浓度延迟且延长,达8小时,因此,此类制剂可用于提高醋氯芬酸的生物利用度。AVH片剂的溶胀行为也通过磁共振成像进行评估。在AVH片剂通过胃肠道的过程中,通过X射线监测其命运。AVH的急性毒性研究表明不存在任何毒性,这揭示了AVH的安全性。因此,AVH可用于口服、局部和眼科给药系统。这些结果证实了AVH作为一种用于靶向给药的刺激敏感、pH值依赖性和缓释生物材料的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/482b/9054136/e8b0942e9e4e/d0ra03176c-f1.jpg

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