Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Monazzamet El Wehda El Afrikeya Street, Abbasseya, Cairo, Egypt.
Carbohydr Polym. 2013 Apr 15;94(1):669-76. doi: 10.1016/j.carbpol.2013.01.072. Epub 2013 Feb 8.
Engineering polymer surfaces reduces nanoparticles (NPs) aggregation and phagocytosis due to effective shielding, hindering recognition by the reticuloendothelial system (RES). The shielding of NPs is complex and affected by the type of groups used in terms of charge and hydrophilicity. This will, in turn, affect NPs biodistribution which will determine the length of activity of the drug. Polysaccharides are nowadays recognized for decreasing the uptake of particulate carriers by the mononuclear phagocytic system (MPS). Chitosan is considered as an attractive candidate due to its biocompatibility, biodegradability, non-toxicity and low cost. In this study clozapine (CZP)-loaded NPs were coated with chitosan, pluronic F-68, polyethylene glycol (PEG) 4000 and polysorbate 80. The factors affecting drug encapsulation efficiency, particle size, surface charge, surface hydrophilicity, pharmacokinetics and biodistribution were studied. The results proved that although a similarity in surface hydrophilicity, chitosan-stealth NPs showed different pharmacokinetic profile and biodistribution behavior compared to polysorbate-stealth NPs.
工程聚合物表面由于有效的屏蔽作用，减少了纳米粒子（NPs）的聚集和吞噬作用，从而阻碍了网状内皮系统（RES）的识别。NPs 的屏蔽作用很复杂，受到所使用的基团的类型的影响，包括电荷和亲水性。这反过来又会影响 NPs 的生物分布，从而决定药物的作用时间。多糖类物质现在被认为可以减少单核吞噬细胞系统（MPS）对颗粒载体的摄取。壳聚糖由于其生物相容性、生物降解性、无毒性和低成本而被认为是一种有吸引力的候选物。在这项研究中，氯氮平（CZP）负载的 NPs 用壳聚糖、泊洛沙姆 F-68、聚乙二醇（PEG）4000 和聚山梨酯 80 进行了包覆。研究了影响药物包封效率、粒径、表面电荷、表面亲水性、药代动力学和生物分布的因素。结果证明，尽管表面亲水性相似，但与聚山梨酯 80-隐形 NPs 相比，壳聚糖-隐形 NPs 表现出不同的药代动力学特征和生物分布行为。
