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两亲性聚乳酸-超支化聚甘油纳米粒作为难溶性药物的控制释放系统:理化性质研究。

Amphiphilic polylactic acid-hyperbranched polyglycerol nanoparticles as a controlled release system for poorly water-soluble drugs: physicochemical characterization.

机构信息

Key Laboratory of Functional Polymer Materials of Ministry Education, Institute of Polymer Chemistry, Nankai University, Tianjin, China.

出版信息

J Pharm Pharmacol. 2011 Jun;63(6):757-64. doi: 10.1111/j.2042-7158.2011.01260.x. Epub 2011 Apr 28.

Abstract

OBJECTIVES

Quercetin was applied as a model drug to evaluate the potential application of amphiphilic polylactic acid-hyperbranched polyglycerol (HPG-PLA) nanoparticles as carriers for poorly water-soluble drugs.

METHODS

The drug delivery systems were characterized by dynamic light scattering, powder X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR) and so forth.

KEY FINDINGS

The results showed the particle sizes ranged from 205.3 to 433.3 nm with low polydispersity index. XRD and FTIR demonstrated that the crystal of the drug was converted to an amorphous state in the matrices and formed intermolecular interaction with carriers. The drug encapsulation efficiency and drug loading could reach 91.8% and 21.0%, respectively. Cell viability assay suggested the nanoparticles had good cytocompatibility. The in-vitro drug release profiles showed a sustained quercetin release up to 192 h, indicating the suitability of nanoparticles in sustained drug release. Furthermore, the influence of many factors on release profiles could also be evaluated for the potential of using nanoparticles as controlled release systems.

CONCLUSIONS

This system may be of clinical importance in both stabilizing and delivering hydrophobic drugs for the treatment of many diseases.

摘要

目的

以槲皮素为模型药物,评价两亲性聚乳酸-超支化聚甘油(HPG-PLA)纳米粒作为难溶性药物载体的应用潜力。

方法

采用动态光散射、粉末 X 射线衍射(XRD)和傅里叶变换红外光谱(FTIR)等方法对载药系统进行了表征。

主要发现

结果表明,粒径范围为 205.3-433.3nm,多分散指数低。XRD 和 FTIR 表明,药物晶体在基质中转化为无定形状态,并与载体形成分子间相互作用。药物包封率和载药量分别可达 91.8%和 21.0%。细胞活力测定表明,纳米粒具有良好的细胞相容性。体外药物释放曲线表明,槲皮素可持续释放 192h,表明纳米粒适用于缓控释。此外,还可以评估多种因素对释放曲线的影响,以评估纳米粒作为控释系统的潜力。

结论

该系统在稳定和递疏水药物治疗多种疾病方面具有重要的临床意义。

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