Comparative in vitro evaluation of several colloidal systems, nanoparticles, nanocapsules, and nanoemulsions, as ocular drug carriers
Comparative in vitro evaluation of several colloidal systems, nanoparticles, nanocapsules, and nanoemulsions, as ocular drug carriers
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DOI：
10.1021/js950474
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发表时间：
1996-05-01
影响因子：
3.8
通讯作者：
Alonso, MJ
中科院分区：
文献类型：
--
作者：
Calvo, P;VilaJato, JL;Alonso, MJ
设计了三种不同的胶体载体，即聚己内酯纳米粒和纳米胶囊以及亚微乳，并研究了它们增加药物角膜渗透的能力。这三种系统的内部结构和组成不同，但它们具有相似的尺寸（200-250 nm）和负表面电荷（-16 ~-42 mV）。吲哚美辛，这是用作模型药物，分散在胶体系统内的分子水平，没有检测到的聚合物和药物之间的化学相互作用。当在缓冲介质中高度稀释时，包封的吲哚美辛的释放非常迅速，并且与系统的组成无关。微囊化吲哚美辛滴眼液的体外角膜渗透性是市售滴眼液的3倍以上。这种增加的渗透性对于所研究的三种制剂是相似的，因此排除了胶体系统的内部结构或化学组成对吲哚美辛的角膜渗透性的影响。因此，可以说，负责吲哚美辛的有利角膜转运的主要因素是这些载体的胶体性质，而不是它们的内部结构或组成。
Three different colloidal carriers, namely, nanoparticles and nanocapsules made of poly-epsilon-caprolactone and submicron emulsions, were designed, and their capacity for increasing the corneal penetration of drugs was investigated, The three systems differed in their inner structure and composition, but they had a similar size (200-250 nm) and a negative superficial charge (-16 to -42 mV). Indomethacin, which was used as a model drug, was dispersed at a molecular level within the colloidal systems, no chemical interaction between the polymer and the drug being detected. Release of the encapsulated indomethacin occurred very rapidly upon high dilution in a buffered medium and was independent of the composition of the system. The in vitro corneal penetration of the encapsulated indomethacin was more than 3-fold that of the commercial eye drops. This increased penetration was similar for the three formulations investigated, which therefore excludes the influence of the inner structure or chemical composition of the colloidal systems on the corneal penetration of indomethacin. Thus, it could be stated that the main factor responsible for the favorable corneal transport of indomethacin is the colloidal nature of these carriers rather than their inner structure or composition.