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Molecules
2019 Oct 28;2421:. doi: 10.3390/molecules24213881.
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Praziquantel-Solid Lipid Nanoparticles Produced by Supercritical Carbon Dioxide Extraction: Physicochemical Characterization, Release Profile, and Cytotoxicity.
Andrade LN
,
Oliveira DML
,
Chaud MV
,
Alves TFR
,
Nery M
,
da Silva CF
,
Gonsalves JKC
,
Nunes RS
,
Corrêa CB
,
Amaral RG
,
Sanchez-Lopez E
,
Souto EB
,
Severino P
.
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Solid lipid nanoparticles (SLNs) can be produced by various methods, but most of them are difficult to scale up. Supercritical fluid (SCF) is an important tool to produce micro/nanoparticles with a narrow size distribution and high encapsulation efficiency. The aim of this work was to produce cetyl palmitate SLNs using SCF to be loaded with praziquantel (PZQ) as an insoluble model drug. The mean particle size (nm), polydispersity index (PdI), zeta potential, and encapsulation efficiency (EE) were determined on the freshly prepared samples, which were also subject of Differential Scanning Calorimetry (DSC), Fourier-Transform Infrared Spectroscopy (FTIR), drug release profile, and in vitro cytotoxicity analyses. PZQ-SLN exhibited a mean size of ~25 nm, PdI ~ 0.5, zeta potential ~-28 mV, and EE 88.37%. The DSC analysis demonstrated that SCF reduced the crystallinity of cetyl palmitate and favored the loading of PZQ into the lipid matrices. No chemical interaction between the PZQ and cetyl palmitate was revealed by FTIR analysis, while the release or PZQ from SLN followed the Weibull model. PZQ-SLN showed low cytotoxicity against fibroblasts cell lines. This study demonstrates that SCF may be a suitable scale-up procedure for the production of SLN, which have shown to be an appropriate carrier for PZQ.
CNPq, #443238/2014-6, #470388/2014-5 Coordenação Aperfeiçoamento de Pessoal de Nivel Superior (CAPES), Fundação de Amparo à Pesquisa do Estado de Sergipe (FAPITEC), and Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), M-ERA-NET/0004/2015 Portuguese Science and Technology Foundation
Figure 3. In vitro drug release profile of free PZQ and PZQ-SLN.
Figure 4. Effect of praziquantel, SLNs, and PZQ-SLNs supercritical in the evaluation of the viability of human L929 fibroblasts determined by the MTT assay after 24 h of incubation. The negative control (C) was treated with the vehicle used to dilute the drug (DMSO 5%). The data correspond to the mean ± SEM of four independent experiments.
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