用于控制 2 型糖尿病的新型琥珀酰化羧甲基瓜尔胶纳米载体格列美脲

Q3 Medicine
Harsh Yadav , Biswajit Maji , Sabyasachi Maiti
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引用次数: 0

摘要

在这项研究中,瓜尔胶(GG)被化学改性为羧甲基衍生物,然后使用亲核催化剂 4-二甲氨基吡啶(DMAP)与辛烯基琥珀酸酐(OSA)进行酯化,使衍生物具有两亲特性。傅立叶变换红外光谱(FTIR)对羧甲基瓜尔胶(CMGG)和琥珀酰化 CMGG 进行了表征。使用 DMAP/OSA 比率为 0.5:1 合成的两性瓜尔豆胶(CMGGOSA-I)无毒。两亲瓜尔胶在水中自组装形成纳米载体,其平均直径为 430 nm,Zeta 电位为 -19.0 mV。透射电子显微镜(TEM)图像显示,所开发的 CMGGOSA-I 纳米载体呈球形。在两亲性 CMGG 的存在下,格列美脲的水溶性提高了约 67 倍。按照樋口动力学,纳米载体在模拟胃肠液中释放格列美脲的时间超过 24 小时。对药物释放数据进行的 Korsmeyer-Peppas 建模显示,药物释放是溶胀和扩散机制共同作用的结果。在链脲佐菌素诱导的糖尿病大鼠模型中,纳米载体的抗糖尿病活性优于纯药物悬浮液,其抗糖尿病活性可持续 24 小时。总之,新合成的两亲性 CMGG 纳米载体具有药物控释特性,有望控制 2 型糖尿病。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Novel succinoylated carboxymethyl guar gum nanocarriers of glimepiride for controlling type-2 diabetes

In this study, guar gum (GG) was chemically modified to its carboxymethyl derivative, which was then esterified with octenyl succinic anhydride (OSA) using a nucleophilic catalyst 4-dimethylaminopyridine (DMAP) to render the derivative amphiphilic characteristics. The carboxymethyl guar gum (CMGG) and succinoylated CMGG was characterized using Fourier transform infrared spectroscopy (FTIR) spectroscopy. The amphiphilic CMGG synthesized using DMAP/OSA ratio of 0.5:1 (CMGGOSA-I), was found to be non-toxic. The amphiphilic guar gum self-assembled in water to form nanocarriers with mean diameter of 430 ​nm and zeta potential of −19.0 ​mV. Transmittance electron microscope (TEM) image showed spherical nature of the developed CMGGOSA-I nanocarriers. In presence of amphiphilic CMGG, the aqueous solubility of glimepiride was enhanced by about 67-fold. The nanocarriers released glimepiride in simulated gastrointestinal fluids for a period of more than 24 ​h, following Higuchi's kinetics. Korsmeyer-Peppas modeling of the drug release data revealed that a combination of swelling and diffusion mechanism was operative in the event of drug release. In streptozotocin-induced diabetic rat model, the nanocarriers outperformed pure drug suspensions in terms of anti-diabetic activity, which lasted up to 24 ​h. Overall; the newly synthesized amphiphilic CMGG nanocarriers demonstrated controlled drug release properties and showed promise for controlling type-2 diabetes.

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来源期刊
Medicine in Novel Technology and Devices
Medicine in Novel Technology and Devices Medicine-Medicine (miscellaneous)
CiteScore
3.00
自引率
0.00%
发文量
74
审稿时长
64 days
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