Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, India.
Drug Dev Ind Pharm. 2010 Aug;36(8):933-45. doi: 10.3109/03639040903585143.
To develop and characterize self-nanoemulsifying drug delivery system (SNEDDS) of the poorly water-soluble drug, glibenclamide (GBD).
Solubility of GBD was determined in various vehicles. Phase diagrams were constructed to identify efficient self-emulsification region using oils, surfactants, and cosurfactants in aqueous environment. Formulations were assessed for drug content, spectroscopic clarity, emulsification time, contact angle, zeta potential, particle size, and dissolution studies. On the basis of similarity and dissimilarity of particle size distribution, formulations were further characterized using principal component analysis and agglomerative hierarchy cluster analysis.
Among the formulations prepared and evaluated, optimized formulation showed mean particle size between 15.65 and 32.70 nm after 24 hour postdilution in various media. Dilution volume had no significant effect on particle size. Transmission electron microscopy of these formulations confirmed the spherical shape of globules with no signs of coalescence of globules and precipitation of drug. The relevance of difference in t(50%) and percent dissolution efficiency were evaluated statistically by two-way ANOVA. Infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction studies indicated compatibility between drug, oil, and surfactants.
The results of this study indicate that the self-nanoemulsifying drug delivery system of GBD, owing to nanosize, has potential to enhance its absorption and without interaction or incompatibility between the ingredients.
开发并表征难溶性药物格列本脲（GBD）的自微乳给药系统（SNEDDS）。
测定 GBD 在各种载体中的溶解度。在水相环境中使用油、表面活性剂和助表面活性剂构建相图以确定有效的自乳化区域。评估制剂的药物含量、光谱清晰度、乳化时间、接触角、Zeta 电位、粒径和溶解研究。根据粒径分布的相似性和相异性，进一步使用主成分分析和凝聚层次聚类分析对制剂进行特征描述。
在所制备和评估的制剂中，优化制剂在各种介质中稀释 24 小时后显示出 15.65 至 32.70nm 之间的平均粒径。稀释体积对粒径没有显著影响。这些制剂的透射电子显微镜证实了液滴呈球形，没有液滴聚结和药物沉淀的迹象。通过双向方差分析评估 t（50%）和溶解效率百分比差异的相关性。红外光谱、差示扫描量热法和 X 射线衍射研究表明药物、油和表面活性剂之间具有相容性。
本研究结果表明，GBD 的自微乳给药系统由于纳米尺寸，具有增强其吸收的潜力，且成分之间没有相互作用或不兼容。
