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自发乳化法制备亲脂性纳米胶束。

Production of lipophilic nanogels by spontaneous emulsification.

机构信息

Université de Strasbourg, CNRS, Institut Charles Sadron UPR 22, F-67000 Strasbourg, France; Shaanxi University of Science & Technology, Institute of Atomic and Molecular Science, CN-710021 Xi'an, Shaanxi, China.

Université de Strasbourg, CNRS, Institut Charles Sadron UPR 22, F-67000 Strasbourg, France; Université de Strasbourg, CNRS, CAMB UMR 7199, F-67000 Strasbourg, France; Faculty of Pharmacy, University of Sindh, Jamshoro, Sindh, Pakistan.

出版信息

Int J Pharm. 2020 Jul 30;585:119481. doi: 10.1016/j.ijpharm.2020.119481. Epub 2020 May 27.

Abstract

Nanosized gel particles, so-called nanogels, have attracted substantial interest in different application fields, thanks to their controllable and three-dimensional physical structure, good mechanical properties and potential biocompatibility. Literature reports many technologies for their preparation and design, however a recurrent limitation remains in their broad size distributions as well as in the poor size control. Therefore, the monodisperse and size-controlled nanogels preparation by simple process -like emulsification- is a real challenge still in abeyance to date. In this study we propose an original low energy emulsification approach for the production of monodisperse nanogels, for which the size can be finely controlled in the range 30 to 200 nm. The principle lies in the fabrication of a direct nano-emulsion containing both oil (medium chain triglycerides) and a bi-functional acrylate monomer. The nanogels are thus formed in situ upon UV irradiation of the droplet suspension. Advantage of such modification of the oil nano-carriers are the potential modulation of the release of encapsulated drugs, as a function of the density and/or properties of the polymer chain network entrapped in the oil nano-droplets. This hypothesis was confirmed using a model of hydrophobic drug -ketoprofen- entrapped into the nanogels particles, along with the study of the release profile, carried out in function of the nature of the monomers, density of polymer chains, and different formulation parameters.

摘要

纳米凝胶颗粒,又称纳米胶,由于其可控的三维物理结构、良好的机械性能和潜在的生物相容性,在不同的应用领域引起了极大的兴趣。文献报道了许多制备和设计纳米凝胶的技术,但它们的宽粒径分布和较差的粒径控制仍然是一个反复出现的限制。因此,通过简单的工艺(如乳化)制备单分散且粒径可控的纳米凝胶仍然是一个尚未解决的挑战。在这项研究中,我们提出了一种原始的低能量乳化方法来制备单分散纳米凝胶,其粒径可以在 30 至 200nm 的范围内精细控制。其原理在于制备直接纳米乳液,其中包含油(中链甘油三酯)和双官能丙烯酸酯单体。纳米凝胶是在液滴悬浮液的紫外线照射下原位形成的。这种油纳米载体的改性的优点是可以潜在地调节包封药物的释放,这取决于聚合物链网络在油纳米液滴中的密度和/或性质。通过将疏水性药物酮洛芬包封在纳米凝胶颗粒中,并研究其释放曲线,验证了这一假设,该释放曲线与单体的性质、聚合物链密度以及不同的配方参数有关。

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