Abulateefeh Samer R, Taha Mutasem O
Department of Pharmaceutics and Pharmaceutical Technology and.
J Microencapsul. 2015;32(1):96-105. doi: 10.3109/02652048.2014.985343. Epub 2014 Nov 21.
Calcium alginate nanoparticles (NPs) suffer from sub-optimal stability in bio-relevant media leading to low drug encapsulation efficiency and uncontrolled release profiles. To sort out these drawbacks, a novel approach is proposed herein based on introducing tannic acid into these NPs to act as a bridging cross-linking aid agent. Calcium-alginate NPs were prepared by the ionotropic gelation method and loaded with diltiazem hydrochloride as a model drug. These NPs were characterized in terms of particle size, zeta potential, and morphology, and results were explained in accordance with Fourier-transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC). The incorporation of tannic acid led to more than four folds increase in drug encapsulation efficiency (i.e. from 15.3% to 69.5%) and reduced burst drug release from 44% to around 10% within the first 30 min. These findings suggest the possibility of improving the properties of Ca-alginate NPs by incorporating cross-linking aid agents under mild conditions.
海藻酸钙纳米颗粒(NPs)在生物相关介质中的稳定性欠佳,导致药物包封效率较低且释放曲线不可控。为解决这些缺点,本文提出一种基于将单宁酸引入这些纳米颗粒以充当桥连交联助剂的新方法。通过离子凝胶法制备海藻酸钙纳米颗粒,并负载盐酸地尔硫䓬作为模型药物。对这些纳米颗粒进行了粒径、zeta电位和形态表征,并根据傅里叶变换红外(FTIR)光谱和差示扫描量热法(DSC)对结果进行了解释。单宁酸的加入使药物包封效率提高了四倍多(即从15.3%提高到69.5%),并将前30分钟内的药物突释从44%降低到约10%。这些发现表明在温和条件下通过加入交联助剂改善海藻酸钙纳米颗粒性能的可能性。