The incorporation of Pterodon pubescens fruit oil into optimized nanostructured lipid carriers improves its effectiveness in colorectal cancer

The incorporation of Pterodon pubescens fruit oil into optimized nanostructured lipid carriers improves its effectiveness in colorectal cancer

•The 23 factorial design was used to optimize the PpO-loaded NLCs development.•Optimized PpO-loaded NLCs showed excellent physicochemical characteristics.•Solid lipids may be partially recrystallized and less ordered in PpO-loaded NLCs.•An interaction may exist between PpO and lipid matrix in PpO-lo...

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Bibliographic Details
Published in:Industrial crops and products Vol. 123; pp. 719 - 730
Main Authors: Outuki, P.M., Kleinubing, S.A., Hoscheid, J., Montanha, M.C., da Silva, E.A., do Couto, R.O., Kimura, E., Cardoso, M.L.C.
Format: Journal Article
Language:English
Published: Elsevier B.V 01-11-2018
Subjects:
Cytotoxicity
Design of experiments
HT-29
Melt-emulsification
Pterodon pubescens Benth
NLC
TAS
Cytotoxicity
DLS
XRD
Pterodon pubescens Benth
DSC
ANOVA
SLNs
D50
PEG-40H
R2
EE
GC–MS
CC50
P80H
NLCs
TSL
RSM
PpO
TC
PC
FT-Raman
HT-29
SIM
ZP
PI
DoE
TEM
Design of experiments
Melt-emulsification
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Summary:•The 23 factorial design was used to optimize the PpO-loaded NLCs development.•Optimized PpO-loaded NLCs showed excellent physicochemical characteristics.•Solid lipids may be partially recrystallized and less ordered in PpO-loaded NLCs.•An interaction may exist between PpO and lipid matrix in PpO-loaded NLCs.•NLCs loaded with PpO showed higher anticancer activity than the pure PpO. The 23 full factorial design was used to optimize the development of nanostructured lipid carriers (NLCs) containing P. pubescens fruit oil by the melt-emulsification method. The effects of the type of solid lipid, concentration of Phospholipon® 80H and type of aqueous surfactant in parameters such as particle size, polydispersity index (PI), zeta potential (ZP), total content (TC), and encapsulation efficiency (EE) of vouacapans were evaluated. The preparation method of the NLCs was appropriate as the chemical profile of the oil remained unchanged before and after the development process. The studied factors proved to affect the NLCs quality factors at different significant levels. The NLC that presented the best results was the formulation F4, which was produced with Precirol® ATO 5, 0.5% Phospholipon® 80H, and PEG-40 hydrogenated castor oil/sorbitan oleate. The optimized formulation showed small and spherical particles of 94.47 ± 2.05 nm, a PI of 0.197 ± 0.003, ZP less than –30 mV, and excellent physical stability after dispersion analysis. In addition, high values (>98%) of the TC and EE of vouacapans were obtained. X-ray diffraction, Fourier transform Raman spectroscopy and differential scanning calorimetry analysis were also performed. The results suggested that lipids may be partially recrystallized and less ordered in NLCs and that between the P. pubescens oil and lipid matrix an interaction may exist. The P. pubescens fruit oil presented in vitro cytotoxicity to HT-29 cells, with CC50 of 273.47 μg/mL, and was more cytotoxic when incorporated into NLCs (CC50 of 154.19 μg/mL), which justifies the use of such technology in the development of novel phytopharmaceutical products.
ISSN:0926-6690
1872-633X
DOI:10.1016/j.indcrop.2018.07.044