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戊二醛交联的亚麻籽壳黏液微球的黏膜黏附性表征

Mucoadhesivity Characterization of Isabgol Husk Mucilage Microspheres Crosslinked by Glutaraldehyde.

作者信息

Sharma Vipin Kumar, Sharma Prince Prashant, Mazumder Bhasker, Bhatnagar Aseem, Singh Thakuri

机构信息

Department of Pharmaceutical Sciences Gurukul Kangri Vishwavidyalaya Haridwar-249404, India.

出版信息

Curr Drug Deliv. 2015;12(6):693-702. doi: 10.2174/1567201812666150212124054.

Abstract

The microspheres of Isabgol husk were prepared by emulsification-crosslinking technique and the gastrointestinal transition behavior of the formulation was studied by gamma scintigraphy. The impact of different process variables such as amount of glutaraldehyde, concentration of Isabgol husk and temperature was studied on surface morphology and mucoadhesion. In vitro mucoadhesive testing of formulations was performed by determination of zeta potential, mucus glycoprotein assay and mucus adsorption isotherms. The effect of feeding on retention of microspheres in the gastrointestinal track (GIT) was studied in albino rabbits by gamma scintigraphy study. The results indicated the formation of microspheres as observed by scanning electron microscopy. The smooth and round surfaces of microspheres were obtained on increasing Isabgol husk and glutaraldehyde amount. The positive zeta potential of all formulations indicated the electrostatic interaction as a mechanism of mucoadhesion between the mucus of GIT membranes and the microspheres surfaces. The influence of electrostatic interaction on mucoadhesion of microspheres was again ascertained when the mucin equilibrium adsorption on preparations indicated well fitness in Langmuir and Freundlich adsorption isotherms. During gamma scintigraphy, the stability of (99m)Tc-sodium pertechnetate was found 98.82% at pH 6.8 and 96.78% at pH 7.2, respectively. It indicated the minimal leaching of bound radionuclide from microspheres during gastrointestinal transition as observed in gamma scintigraphic images of the rabbits. The microspheres retained in GIT even after 24 hrs of oral administration. The results indicated the applicability of Isabgol husk mucilage in the development of mucoadhesive microspheres.

摘要

采用乳化交联技术制备了亚麻籽壳微球,并通过γ闪烁扫描术研究了该制剂在胃肠道中的转运行为。研究了不同工艺变量(如戊二醛用量、亚麻籽壳浓度和温度)对表面形态和黏膜黏附性的影响。通过测定ζ电位、黏液糖蛋白分析和黏液吸附等温线对制剂进行体外黏膜黏附性测试。通过γ闪烁扫描术研究了白化兔进食对微球在胃肠道(GIT)中滞留的影响。扫描电子显微镜观察结果表明微球已形成。随着亚麻籽壳和戊二醛用量的增加,微球表面变得光滑且呈圆形。所有制剂的正ζ电位表明静电相互作用是GIT膜黏液与微球表面之间黏膜黏附的一种机制。当制剂上的黏蛋白平衡吸附表明符合朗缪尔和弗伦德里希吸附等温线时,再次确定了静电相互作用对微球黏膜黏附性的影响。在γ闪烁扫描过程中,发现高锝酸钠(99mTc)在pH 6.8时的稳定性分别为98.82%,在pH 7.2时为96.78%。这表明在兔的γ闪烁扫描图像中观察到,在胃肠道转运过程中,结合的放射性核素从微球中的浸出量极少。口服给药24小时后,微球仍保留在胃肠道中。结果表明亚麻籽壳黏液在黏膜黏附性微球的开发中具有适用性。

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