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利用电喷雾快速制备载药量高的 pH 敏感型聚合物纳米粒子用于口服给药。

Rapid preparation of pH-sensitive polymeric nanoparticle with high loading capacity using electrospray for oral drug delivery.

机构信息

Key Laboratory of Biorheological Science and Technology, Ministry of Education, College of Bioengineering, Chongqing University, Chongqing 400030, China.

出版信息

Mater Sci Eng C Mater Biol Appl. 2013 Dec 1;33(8):4562-7. doi: 10.1016/j.msec.2013.07.009. Epub 2013 Jul 18.

Abstract

Drug loading capacity is an important property for an ideal drug delivery system. However, the drug loading capacity of prepared pH-sensitive polymeric nanoparticles is usually low. To overcome this drawback, the electrospray method was used to prepare Eudragit L 100-55 nanoparticles with high drug loading capacity in one step. Omeprazole was selected as the model drug. The maximum loading capacity of nanoparticles was 43.21% by changing the mass ratio of drug to polymer, and the entrapment efficiency was nearly 100%. The prepared nanoparticle showed spherical or ellipsoidal morphology and the average diameter was about 300 nm. The pH-sensitive nanoparticle displayed pH-dependent release in vitro. In addition, a slight cytotoxicity was detected in the cytotoxicity study. The results indicated that electrospray is an easy, rapid and efficient technique for the preparation of high-loading pH-sensitive polymeric nanoparticles, and the pH-sensitive nanoparticle is a promising carrier for oral drug delivery.

摘要

载药量是理想药物输送系统的一个重要性质。然而,所制备的 pH 敏感聚合物纳米粒的载药量通常较低。为了克服这一缺点,采用静电喷雾法一步法制备载药量高的 Eudragit L 100-55 纳米粒。以奥美拉唑为模型药物。通过改变药物与聚合物的质量比,纳米粒的最大载药量可达 43.21%,包封率接近 100%。所制备的纳米粒呈球形或椭圆形,平均直径约为 300nm。该 pH 敏感纳米粒在体外表现出 pH 依赖性释放。此外,在细胞毒性研究中检测到轻微的细胞毒性。结果表明,静电喷雾是一种用于制备高载药量 pH 敏感聚合物纳米粒的简便、快速、高效的技术,pH 敏感纳米粒是口服药物输送的一种有前途的载体。

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