Department of Applied Physics, University of Granada, Granada, Spain; Department of Biopharmaceutics and Pharmaceutical Technology, Saarland University, Saarbrücken, Germany.
J Control Release. 2010 Jan 4;141(1):85-92. doi: 10.1016/j.jconrel.2009.08.012. Epub 2009 Aug 21.
The goal of this paper was aimed to the formulation of nanoparticles by using two different propyl-starch derivatives - referred to as PS-1 and PS-1.45 - with high degrees of substitution: 1.05 and 1.45 respectively. A simple o/w emulsion diffusion technique, avoiding the use of hazardous solvents such as dichloromethane or dimethyl sulfoxide, was chosen to formulate nanoparticles with both polymers, producing the PS-1 and PS-1.45 nanoparticles. Once the nanoparticles were prepared, a deep physicochemical characterization was carried out, including the evaluation of nanoparticles stability and applicability for lyophilization. Depending on this information, rules on the formation of PS-1 and PS-1.45 nanoparticles could be developed. Encapsulation and release properties of these nanoparticles were studied, showing high encapsulation efficiency for three tested drugs (flufenamic acid, testosterone and caffeine); in addition a close to linear release profile was observed for hydrophobic drugs with a null initial burst effect. Finally, the potential use of these nanoparticles as transdermal drug delivery systems was also tested, displaying a clear enhancer effect for flufenamic acid.
本文的目的旨在通过使用两种不同的高取代度(分别为 1.05 和 1.45)的丙基淀粉衍生物 - PS-1 和 PS-1.45 - 来制备纳米粒子。选择了一种简单的 o/w 乳液扩散技术,避免使用二氯甲烷或二甲基亚砜等危险溶剂,来用两种聚合物制备纳米粒子,得到 PS-1 和 PS-1.45 纳米粒子。一旦制备好纳米粒子,就进行了深入的物理化学特性分析,包括纳米粒子稳定性和冻干适用性的评估。根据这些信息,可以制定出 PS-1 和 PS-1.45 纳米粒子形成的规则。研究了这些纳米粒子的包封和释放性能,发现三种测试药物(氟芬那酸、睾酮和咖啡因)的包封效率很高;此外,对于疏水性药物,观察到接近线性的释放曲线,且没有初始突释效应。最后,还测试了这些纳米粒子作为透皮药物传递系统的潜在用途,结果显示对氟芬那酸有明显的增强作用。