Mahajan Hitendra Shaligram, Gattani Surendra Ganeshlal
Department of Pharmaceutics, R. C. Patel Institute of Pharmaceutical Education and Research, Maharashtra, India.
Chem Pharm Bull (Tokyo). 2009 Apr;57(4):388-92. doi: 10.1248/cpb.57.388.
The purpose of this study was to develop nasal microparticles of metoclopromide employing gellan gum as a polymer by spray drying method. This method of microencapsulation is particularly less dependent on the solubility characteristics of the drug and polymer and is simple, reproducible, and easy to scale up. The microparticles were evaluated for characteristics like particle size, incorporation efficiency, swelling ability, zeta potential, mucoadhesion, thermal analysis, X-ray diffraction (XRD) study and in vitro drug release. The microparticles so prepared had irregular shape and smooth but distorted surface morphology. They were negatively charged. The particle size ranged from 9.38 to 10.67 microm. Differential scanning calorimetry (DSC) studies revealed that metoclopromide was molecularly dispersed inside the microparticles. The swelling was increased with increase in amount of polymer. The release of drug from microparticles was moderately sustained without lag time and attributed to formation of hydrogel; ionically cross linked hydrogel was hypothesized. The formulation was found to be non toxic to nasal tissue. These in vitro preliminary results show that spray dried microparticles based on gellan gum could be suitable nasal delivery system for the administration of metoclopromide.
本研究的目的是通过喷雾干燥法,以结冷胶作为聚合物制备甲氧氯普胺鼻用微粒。这种微囊化方法尤其不太依赖药物和聚合物的溶解性特征,且简单、可重复且易于放大。对微粒进行了粒径、包封效率、溶胀能力、ζ电位、粘膜粘附性、热分析、X射线衍射(XRD)研究以及体外药物释放等特性评估。如此制备的微粒形状不规则,表面形态光滑但有扭曲,带负电荷。粒径范围为9.38至10.67微米。差示扫描量热法(DSC)研究表明甲氧氯普胺在微粒内部呈分子分散状态。溶胀随着聚合物用量的增加而增大。药物从微粒中的释放呈适度持续且无滞后时间,这归因于水凝胶的形成;推测为离子交联水凝胶。该制剂被发现对鼻组织无毒。这些体外初步结果表明,基于结冷胶的喷雾干燥微粒可能是用于甲氧氯普胺给药的合适鼻用递送系统。