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半乳糖化牛血清白蛋白纳米粒的制备及表征及其用于冬凌草甲素肝靶向给药系统的研究

Preparation and characterization of galactosylated bovine serum albumin nanoparticles for liver-targeted delivery of oridonin.

机构信息

College of Pharmacy, Shandong University, Jinan 250012, China.

出版信息

Int J Pharm. 2013 May 1;448(1):79-86. doi: 10.1016/j.ijpharm.2013.03.019. Epub 2013 Mar 19.

Abstract

In this study, galactosylated bovine serum albumin (GB), which could be developed for a liver targeting carrier was synthetized and it was identified by Fourier transform infrared (FT-IR) spectrometer. Oridonin loaded bovine serum albumin nanoparticle (ORI-BSA-NP) and oridonin loaded GB nanoparticle (ORI-GB-NP) were prepared and optimized by the desolvation technique. During the preparation of ORI-GB-NP, galactosamine was introduced to end-cap the free aldehyde groups on nanoparticles. The characteristics of ORI-GB-NP such as particle size, zeta potential, particle morphologie, entrapment efficiency and drug loading were evaluated. The nearly spherical nanoparticles, with a narrow size distribution below 200 nm, were negatively charged with zeta potential of about -30 mV. Meanwhile, differential scanning calorimetry (DSC) and X-ray diffraction confirmed the amorphous state of ORI in ORI-GB-NP. The in vitro drug release of ORI from ORI-GB-NP presented a biphasic pattern with an initial burst effect and consequently sustained release. These results implied that the nanoparticles possessed fine physicochemical characteristics and seemed to be a stable delivery system for poorly soluble oridonin.

摘要

在这项研究中,合成了半乳糖化牛血清白蛋白(GB),可将其开发为肝脏靶向载体,并通过傅里叶变换红外(FT-IR)光谱仪进行了鉴定。采用去溶剂化技术制备并优化了负载奥里吉宁的牛血清白蛋白纳米粒(ORI-BSA-NP)和负载奥里吉宁的 GB 纳米粒(ORI-GB-NP)。在制备 ORI-GB-NP 的过程中,向纳米粒上的游离醛基末端引入半乳糖胺。对 ORI-GB-NP 的粒径、Zeta 电位、形态、包封率和载药量等特性进行了评价。近球形纳米粒,粒径分布在 200nm 以下,带负电荷,Zeta 电位约为-30mV。同时,差示扫描量热法(DSC)和 X 射线衍射证实了 ORI 在 ORI-GB-NP 中的无定形状态。ORI-GB-NP 中 ORI 的体外释放呈双相模式,具有初始突释效应,随后持续释放。这些结果表明,纳米粒具有良好的物理化学特性,似乎是一种用于难溶性奥里吉宁的稳定递送系统。

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