Facile synthesis, characterization, and bioavailability improvement of Losartan Potassium using 3-aminopropyl functionalized magnesium phyllosilicate organoclay

IF 3.2 4区材料科学 Q2 MATERIALS SCIENCE, CERAMICS

Journal of Sol-Gel Science and Technology Pub Date : 2025-08-01 DOI:10.1007/s10971-025-06871-w

Rakesh Dhavale, Dnyaneshwar Mane, Prafull Mane, Avdhut Jadhav, Udaykumar Patil

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Abstract

Hypertension is characterized by elevated blood pressure and tends to be a leading risk factor in cardiovascular conditions and renal dysfunction in India. 3-aminopropyl functionalized magnesium phyllosilicate (AMP) clay containing Losartan potassium (LP) was synthesized using the one-pot sol-gel method for sustained antihypertensive effect. AMP clays containing LP in different drug-to-clay ratios (Losartan Potassium Clay; LPC-1, LPC-2 and LPC-3) resulted in porous organic hybrids for improvement in the bioavailability of LP. Organic clays and LPC-3 were structurally characterized by X-ray diffraction, Fourier transform infrared spectroscopy and scanning electron microscopy. In-vitro dissolution studies resulted in rapid release of LP from LPC-3 in 2 h compared to other compositions. More than 80% LP was released from LPC-3 after 45 min, and complete release at the end of 3 h. LPC-3 showed a 1.5-fold increase in solubility at pH 1.0 compared to the LP alone. AMP clays drew a change in the pH of an aqueous solution to 6.0, resulting in the dissolution of LP. The cellular uptake showed 74% permeation of LP from LPC-3 across Caco-2 cells. Moreover, in-vivo studies revealed an increase in the peak plasma concentration (C_max), area under the plasma concentration-time curve (AUC_0-24h) and reduction in time to reach the peak plasma concentration (T_max) after an oral administration of LPC-3. Thus, the relative bioavailability of LPC-3 was found to be 1.52-fold increase than LP solution. The studies found enhancement in the bioavailability of LP from clay-based organic hybrid after oral administration.

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利用3-氨基丙基功能化层状硅酸镁有机粘土制备氯沙坦钾的简易合成、表征及生物利用度的提高

高血压以血压升高为特征，在印度是心血管疾病和肾功能障碍的主要危险因素。采用一锅溶胶-凝胶法合成含氯沙坦钾（LP）的3-氨基丙基功能化叶根硅酸镁（AMP）粘土，以达到持续降压的效果。含有不同药土比LP的AMP粘土（氯沙坦钾粘土；LPC-1， LPC-2和LPC-3）形成多孔有机杂种，以提高LP的生物利用度。利用x射线衍射、傅里叶变换红外光谱和扫描电镜对有机粘土和LPC-3进行了结构表征。体外溶出度研究表明，与其他组合物相比，LPC-3在2小时内快速释放LP。45 min后LPC-3释放80%以上LP， 3 h后完全释放。LPC-3在pH 1.0时的溶解度比单独的LP提高了1.5倍。AMP粘土使水溶液的pH值变化到6.0，导致LP溶解。细胞摄取显示LPC-3的LP在Caco-2细胞中的渗透率为74%。此外，体内研究显示，口服LPC-3后，血药浓度峰值（Cmax）、血药浓度-时间曲线下面积（AUC0-24h）增加，达到血药浓度峰值（Tmax）的时间缩短。因此，LPC-3的相对生物利用度比LP溶液提高了1.52倍。研究发现，口服粘土基有机混合物后LP的生物利用度增强。

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来源期刊

Journal of Sol-Gel Science and Technology 工程技术-材料科学：硅酸盐

CiteScore

4.70

自引率

4.00%

发文量

280

审稿时长

2.1 months

期刊介绍： The primary objective of the Journal of Sol-Gel Science and Technology (JSST), the official journal of the International Sol-Gel Society, is to provide an international forum for the dissemination of scientific, technological, and general knowledge about materials processed by chemical nanotechnologies known as the "sol-gel" process. The materials of interest include gels, gel-derived glasses, ceramics in form of nano- and micro-powders, bulk, fibres, thin films and coatings as well as more recent materials such as hybrid organic-inorganic materials and composites. Such materials exhibit a wide range of optical, electronic, magnetic, chemical, environmental, and biomedical properties and functionalities. Methods for producing sol-gel-derived materials and the industrial uses of these materials are also of great interest.