Dopamine (DA) and Grape Seed Extract (GSE), thanks to their role as neurotransmitter and antioxidant mixture, respectively, can be usefully co-administered for Parkinson disease (PD) treatment. This combination is intended to prevent the oxidative stress that occurs in PD patients along with restore the levels of the missing neurotransmitter. Hence, the aim of the present study was focusing on the production and in vitro characterization of nanostructured lipid carriers (NLCs) based on Gelucire® 50/13 as solid lipid and Transcutol P® as liquid lipid co-administering DA and GSE. NLCs were obtained according to the method of melt emulsification. DA-GSE-NLCs showed a mean diameter of 186±14 nm as mean diameter and -9.6±0.4 mV as zeta potential value, whereas from Transmission Electron Microscopy visualization they showed spherical morphology. X-ray diffraction indicated a more ordered solid state for DA-NLCs instead of DA-GSE-NLCs, but both of NLCs released DA in low amount in Simulated Nasal Fluid (SNF) as release medium within 48h. Such low amounts of DA delivered from DA-GSE-NLCs and DA-NLCs in SNF were consistent with the structure of such lipid nanocarriers characterized by a higher concentration of solid lipid than liquid lipid. From a biological viewpoint, we conceived our investigations using simple and reliable cell line-based models prior to performing in vivo studies. Therefore, Saccharomices cerevisiae yeast cells were assayed for cell growth after exposure to the NLCs and evidenced that only DA-NLCs allowed an improvement in cell growth. Next, the three types of NLCs (i.e., DA-NLCs, GSE-NLCs and DA-GSE-NLCs) have been were evaluated in the presence of Human Brain Microvascular Endothelial Cells and we found that, by setting the DA concentration at 75 µM instead of 150 µM, all the tested NLCs were safer. Overall, the results obtained provide a robust foundation for future research on PD and may open new avenues concerning lipid nanoparticle-based therapeutics.
Nanostructured lipid carriers containing Dopamine and Grape Seed Extract: evaluation of cell line-based models with application to Parkinson disease studies
Nicoletta Guaragnella;Stefano Castellani;Rosanna Mallamaci;Angela Primavera;Nicola Cioffi;Ernesto Mesto;Emanuela Schingaro;Adriana Trapani;
2026-01-01
Abstract
Dopamine (DA) and Grape Seed Extract (GSE), thanks to their role as neurotransmitter and antioxidant mixture, respectively, can be usefully co-administered for Parkinson disease (PD) treatment. This combination is intended to prevent the oxidative stress that occurs in PD patients along with restore the levels of the missing neurotransmitter. Hence, the aim of the present study was focusing on the production and in vitro characterization of nanostructured lipid carriers (NLCs) based on Gelucire® 50/13 as solid lipid and Transcutol P® as liquid lipid co-administering DA and GSE. NLCs were obtained according to the method of melt emulsification. DA-GSE-NLCs showed a mean diameter of 186±14 nm as mean diameter and -9.6±0.4 mV as zeta potential value, whereas from Transmission Electron Microscopy visualization they showed spherical morphology. X-ray diffraction indicated a more ordered solid state for DA-NLCs instead of DA-GSE-NLCs, but both of NLCs released DA in low amount in Simulated Nasal Fluid (SNF) as release medium within 48h. Such low amounts of DA delivered from DA-GSE-NLCs and DA-NLCs in SNF were consistent with the structure of such lipid nanocarriers characterized by a higher concentration of solid lipid than liquid lipid. From a biological viewpoint, we conceived our investigations using simple and reliable cell line-based models prior to performing in vivo studies. Therefore, Saccharomices cerevisiae yeast cells were assayed for cell growth after exposure to the NLCs and evidenced that only DA-NLCs allowed an improvement in cell growth. Next, the three types of NLCs (i.e., DA-NLCs, GSE-NLCs and DA-GSE-NLCs) have been were evaluated in the presence of Human Brain Microvascular Endothelial Cells and we found that, by setting the DA concentration at 75 µM instead of 150 µM, all the tested NLCs were safer. Overall, the results obtained provide a robust foundation for future research on PD and may open new avenues concerning lipid nanoparticle-based therapeutics.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
