期刊
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 105, 期 -, 页码 19-32出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejps.2017.04.017
关键词
Nanocapsules; PLA-PEG; Chitosan; Polymer dose; Phthalocyanine; Field flow fractionation
资金
- Brazilian agency Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq) [312893/2009-4, 481195/2011-4]
- Brazilian agency Fundacao de Amparo a Pesquisa do Estado de Minas Gerais (FAPEMIG) [PPM-00452-11, 00432-13, BPD-00612-14]
- Brazilian agency Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES)
- Brazilian agency NANOBIOMG Network [RED-00007-14]
The effect of polymeric nanocapsule dose on plasmatic and liver concentrations 20 min after intravenous administration in mice was evaluated. Nanocapsules were prepared with different polymers, namely, poly(D,L-lactide) (PLA), polyethylene glycol-block-poly(D,L-lactide) (PLA-PEG), and PLA with chitosan (PLA-Cs) and compared with a nanoemulsion. These formulations were labelled with a phthalocyanine dye for fluorescent detection. The nanostructures had narrow size distributions upon separation by asymmetric flow field flow fractionation with static and dynamic light scattering detection, with average hydrodynamic diameters in the 130-300 nm range, negative zeta potentials, except PLA-Cs nanocapsules, which had a positive zeta potential. Flow cytometry revealed uptake mostly by monocytes and neutrophils in mice and human blood. PLA nanocapsules and the nanoemulsion showed dose-dependent plasma concentrations, where the percentage of plasmatic fluorescence increased with increasing administered dose. In contrast, PLA-PEG nanocapsules led to a dose-independent plasmatic profile. PLA-Cs nanocapsules showed the lowest plasmatic and liver levels of fluorescence at all administered doses and significant intravenous toxicity in mice. This work demonstrates the importance of considering the nanocarrier dose when evaluating pharmacokinetic and biodistribution data and emphasizes the role of surface features in determining the plasmatic and liver concentrations of a poorly soluble lipophilic encapsulated compound.
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