多孔碳酸钙微粒吸附与聚电解质多层膜包封相结合用于药物持续递送
Combination of adsorption by porous CaCO3 microparticles and encapsulation by polyelectrolyte multilayer films for sustained drug delivery.
作者信息
Wang Chaoyang, He Chengyi, Tong Zhen, Liu Xinxing, Ren Biye, Zeng Fang
机构信息
Research Institute of Materials Science, South China University of Technology, Guangzhou 510640, China.
出版信息
Int J Pharm. 2006 Feb 3;308(1-2):160-7. doi: 10.1016/j.ijpharm.2005.11.004. Epub 2005 Dec 15.
Combination of adsorption by porous CaCO(3) microparticles and encapsulation by polyelectrolyte multilayers via the layer-by-layer (LbL) self-assembly was proposed for sustained drug release. Firstly, porous calcium carbonate microparticles with an average diameter of 5 microm were prepared for loading a model drug, ibuprofen (IBU). Adsorption of IBU into the pores was characterized by ultraviolet (UV), infrared (IR), thermogravimetric analysis (TGA), Brunauer-Emmett-Teller (BET) experiment and X-ray diffraction (XRD). The adsorbed IBU amount Gamma was 45.1mg/g for one-time adsorption and increased with increasing adsorption times. Finally, multilayer films of protamine sulfate (PRO) and sodium poly(styrene sulfonate) (PSS) were formed on the IBU-loaded CaCO(3) microparticles by the layer-by-layer self-assembly. Amorphous IBU loaded in the pores of the CaCO(3) microparticles had a rapider release in the gastric fluid and a slower release in the intestinal fluid, compared with the bare IBU crystals. Polyelectrolyte multilayers assembled on the drug-loaded particles by the LbL reduced the release rate in both fluids. In this work, polymer/inorganic hybrid core-shell microcapsules were fabricated for controlled release of poorly water-soluble drugs. The porous inorganic particles are useful to load drugs in amorphous state and the polyelectrolyte multilayer films coated on the particle assuage the initial burst release.
提出了通过多孔碳酸钙微粒吸附和聚电解质多层膜逐层(LbL)自组装包封相结合的方法来实现药物的持续释放。首先,制备了平均直径为5微米的多孔碳酸钙微粒,用于负载模型药物布洛芬(IBU)。通过紫外(UV)、红外(IR)、热重分析(TGA)、布鲁诺尔-埃米特-泰勒(BET)实验和X射线衍射(XRD)对IBU在孔中的吸附进行了表征。一次吸附时,IBU的吸附量Γ为45.1mg/g,且随吸附次数增加而增加。最后,通过逐层自组装在负载IBU的碳酸钙微粒上形成了硫酸鱼精蛋白(PRO)和聚苯乙烯磺酸钠(PSS)的多层膜。与裸露的IBU晶体相比,负载在碳酸钙微粒孔中的无定形IBU在胃液中释放较快,在肠液中释放较慢。通过LbL在载药颗粒上组装的聚电解质多层膜降低了两种流体中的释放速率。在这项工作中,制备了聚合物/无机杂化核壳微胶囊用于难溶性药物的控释。多孔无机颗粒可用于负载无定形态的药物,包覆在颗粒上的聚电解质多层膜可缓解初始突释。