NMR cryoporometry characterisation studies of the relation between drug release profile and pore structural evolution of polymeric nanoparticles.
NMR cryoporometry characterisation studies of the relation between drug release profile and pore structural evolution of polymeric nanoparticles.
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DOI：
10.1016/j.ijpharm.2014.04.018
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发表时间：
2014-07-20
影响因子：
5.8
通讯作者：
Rigby, Sean P.
中科院分区：
文献类型：
--
作者：
Gopinathan, Navin;Yang, Bin;Lowe, John P.;Edler, Karen J.;Rigby, Sean P.
用于对流输送的纳米颗粒。PLGA/PLA聚合物纳米颗粒可以通过在比其他可能的更长的时间内实现更持续的剂量来潜在地增强药物（例如卡铂）对流递送到大脑的有效性。然而，控制释放纳米颗粒合成路线与随后获得的药物释放曲线之间的联系尚未得到充分理解，这阻碍了合成路线的设计和合适纳米颗粒的可用性。特别地，尽管孔结构演变经常形成获得特定药物释放曲线的物理机制的过去理论的关键方面，但是这些理论尚未针对孔结构信息进行独立测试和验证。这种验证是智能合成设计所必需的，NMR低温孔隙度测定法可以提供必要的信息。与传统的孔表征技术，NMR cryoporometry允许在湿状态下的多孔颗粒的调查。因此，NMR cryoporometry使得能够详细研究药物释放过程中纳米颗粒的不断变化的纳米级结构，并因此以先前未对纳米颗粒进行的方式将孔结构与药物释放曲线相关联。比较了具有不同类型的卡铂药物释放曲线的纳米颗粒，包括突释和各种形式的延迟释放。这些纳米颗粒的ESEM和TEM图像也提供了支持数据，显示了一些纳米颗粒的快速初始演变。不同阶段，在一个复杂的，不同的药物释放曲线，被发现与特定类型的纳米结构的变化，可以区分由NMR。对于核-包衣纳米颗粒制剂，在无结构变化的延长诱导期后，较小纳米孔的形成与实质性药物释放的开始相关。该信息可用于独立验证特定合成方法的原理。因此，已经阐明了用于获得具有延迟释放的芯包衣纳米颗粒的合成途径的有效性的具体原因。
Nanoparticles for convective delivery. PLGA/PLA polymeric nanoparticles could potentially enhance the effectiveness of convective delivery of drugs, such as carboplatin, to the brain, by enabling a more sustained dosage over a longer time than otherwise possible. However, the link between the controlled release nanoparticle synthesis route, and the subsequent drug release profile obtained, is not well-understood, which hinders design of synthesis routes and availability of suitable nanoparticles. In particular, despite pore structure evolution often forming a key aspect of past theories of the physical mechanism by which a particular drug release profile is obtained, these theories have not been independently tested and validated against pore structural information. Such validation is required for intelligent synthesis design, and NMR cryoporometry can supply the requisite information. Unlike conventional pore characterisation techniques, NMR cryoporometry permits the investigation of porous particles in the wet state. NMR cryoporometry has thus enabled the detailed study of the evolving, nanoscale structure of nanoparticles during drug release, and thus related pore structure to drug release profile in a way not done previously for nanoparticles. Nanoparticles with different types of carboplatin drug release profiles were compared, including burst release, and various forms of delayed release. ESEM and TEM images of these nanoparticles also provided supporting data showing the rapid initial evolution of some nanoparticles. Different stages, within a complex, varying drug release profile, were found to be associated with particular types of changes in the nanostructure which could be distinguished by NMR. For a core-coat nanoparticle formulation, the development of smaller nanopores, following an extended induction period with no structural change, was associated with the onset of substantial drug release. This information could be used to independently validate the rationale for a particular synthesis method. Hence, the specific reasons for the effectiveness of the synthesis route, for obtaining core-coat nanoparticles with delayed release, have been elucidated.
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