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							| Functional Foods in Health and Disease - Online ISSN: 2160-3855; Print ISSN: 2378-7007



	

				
						
 
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																Functional Foods in Health and Disease - Online ISSN: 2160-3855; Print ISSN: 2378-7007
										

				


				
				
					
					
						
																					
				
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					Vol. 4 No. 6 (2014): June 2014
				
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									Research Articles
							
		



	
		  	 

		
	
		N-alkylamides: from plant to brain
	


	
	
		

							
					Authors

						
							
								Lieselotte Veryser
							
															
									Drug Quality and Registration (DruQuaR) group, Faculty of Pharmaceutical Sciences, Ghent University, Harelbekestraat 72, B-9000 Ghent
																	
																																		
	
							
								Evelien Wynendaele
							
															
									Drug Quality and Registration (DruQuaR) group, Faculty of Pharmaceutical Sciences, Ghent University, Harelbekestraat 72, B-9000 Ghent
																	
																																		
	
							
								Lien Taevernier
							
															
									Drug Quality and Registration (DruQuaR) group, Faculty of Pharmaceutical Sciences, Ghent University, Harelbekestraat 72, B-9000 Ghent
																	
																																		
	
							
								Frederick Verbeke
							
															
									Drug Quality and Registration (DruQuaR) group, Faculty of Pharmaceutical Sciences, Ghent University, Harelbekestraat 72, B-9000 Ghent
																	
																																		
	
							
								Tanmayee Joshib
							
															
									C.U. Shah College of Pharmacy, 
S.N.D.T. Women’s University, Santacruz (W), Mumbai-400 049
																	
																																		
	
							
								Pratima Tatke
							
															
									C.U. Shah College of Pharmacy, 
S.N.D.T. Women’s University, Santacruz (W), Mumbai-400 049
																	
																																		
	
							
								Bart De Spiegeleer
							
															
									Drug Quality and Registration (DruQuaR) group, Faculty of Pharmaceutical Sciences, Ghent 
University, Harelbekestraat 72, B-9000 Ghent
																	
																																		


				
			
																	
					
												DOI:
					

					
						
							https://doi.org/10.31989/ffhd.v4i6.6
						
					
				
			

						
										
					Abstract

					Background: Plant N-alkylamides (NAAs) are bio-active compounds with a broad functional spectrum. In order to reach their pharmacodynamic targets, they have to overcome several barriers of the body in the absorption phase. The permeability kinetics of spilanthol (a diene NAA) and pellitorine (a triene NAA) across these barriers (i.e. skin, oral/gut mucosa, blood-brain barrier) were investigated.
Methods: The skin and oral mucosa permeability were investigated using human skin and pig mucosa in an ex vivo in vitro Franz diffusion cell set-up. The gut absorption characteristics were examined using the in vitro Caco-2 cell monolayer test system. The initial blood-brain barrier transport kinetics were investigated in an in vivo mice model using multiple time regression and efflux experiments. Quantification of both NAAs was conducted using HPLC-UV and bio-analytical UPLC-MS methods.
Results: We demonstrated that spilanthol and pellitorine are able to penetrate the skin after topical administration. It is likely that spilanthol and pellitorine can pass the endothelial gut as they easily pass the Caco-2 cells in the monolayer model. It has been shown that spilanthol also crosses the oral mucosa as well as the blood-brain barrier. 
Conclusion: It was demonstrated that NAAs pass various physiological barriers i.e. the skin, oral and gut mucosa, and after having reached the systemic circulation, also the blood-brain barrier. As such, NAAs are cosmenutriceuticals which can be active in the brain.
Key words: Plant N-alkylamides, pharmacokinetics, mucosa/skin, blood-brain barrier (BBB), cosmenutriceuticals 

				
			
			

						
																																																													
						
		


		

						
										
					
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						Published
					

					
																			2014-07-25
																	

				
							

			
						
										

											
							
								Issue
							

							
								
									Vol. 4 No. 6 (2014): June 2014
								
							

						
					
											
							
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								Research Articles
							

						
					
									

			
						
										
					
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