Department of Chemistry and Center of Advanced Studies in Chemistry, Panjab University, Chandigarh, India.
Colloids Surf B Biointerfaces. 2013 Jan 1;101:434-41. doi: 10.1016/j.colsurfb.2012.07.006. Epub 2012 Jul 17.
The present study delineates the formulation of niosomes from biocompatible surfactant Tyloxapol and their potential as drug delivery system for anti-tuberculosis drugs. Drug loaded niosomes have a size of 150 nm with a loading efficiency of 97.95±0.2, 98.89±0.2 and 99.50±0.2% for rifampicin (RIF), isoniazid (INH), pyrazinamide (PZA), respectively. Fourier transform infrared spectroscopic studies infer that the drugs are in harmony with the fabricated niosomes since no visible interactions between the drug and niosomes have been detected. The prepared formulations are quite stable as assessed using absorption spectroscopy. TEM images and photoluminescence results reveal that RIF and INH are located in the film bilayer whereas PZA is adsorbed mainly on the surface head groups. In vitro dissolution studies at physiological conditions have been undertaken to compare the release behavior of drugs from the prepared niosomes. Sustained release has been achieved for hydrophilic drugs and an acceptable release in case of RIF. Comparison of regression coefficients of different kinetic models reveal that INH release follows Fickian diffusion mechanism whereas RIF and PZA, a non-Fickian release mechanism. Such a versatile system is expected to reduce dose-related drug toxicity and reach the atelectatic areas.
本研究从生物相容性表面活性剂 Tyloxapol 中描绘了尼奥斯omes 的配方及其作为抗结核药物的药物传递系统的潜力。载药尼奥斯omes 的粒径为 150nm，载药量分别为利福平（RIF）、异烟肼（INH）、吡嗪酰胺（PZA）的 97.95±0.2%、98.89±0.2%和 99.50±0.2%。傅里叶变换红外光谱研究推断，由于药物与尼奥斯omes 之间未检测到可见的相互作用，因此药物与所制备的尼奥斯omes 相协调。使用吸收光谱评估，所制备的制剂非常稳定。TEM 图像和光致发光结果表明，RIF 和 INH 位于膜双层中，而 PZA 主要吸附在表面头基团上。在生理条件下进行了体外溶解研究，以比较从制备的尼奥斯omes 中释放药物的行为。亲水性药物实现了持续释放，而 RIF 的释放则可以接受。不同动力学模型回归系数的比较表明，INH 释放遵循菲克扩散机制，而 RIF 和 PZA 则遵循非菲克释放机制。这种多功能系统有望降低与剂量相关的药物毒性并到达肺不张区域。
