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

Abstract

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.