Inorganic mesoporous particles for controlled [alpha]-linolenic acid delivery to stimulate GLP-1 secretion in vitro
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CitationKamakura, R. Kovalainen, M. Riikonen, J. Nissinen, T. Shere Raza, G. Walkowiak, J. Lehto, VP. Herzig, KH. (2019). Inorganic mesoporous particles for controlled [alpha]-linolenic acid delivery to stimulate GLP-1 secretion in vitro. European journal of pharmaceutics and biopharmaceutics, 144, 132-138. 10.1016/j.ejpb.2019.09.009.
Novel treatment methods for obesity are urgently needed due to the increasing global severity of the problem. Gastrointestinal hormones, such as GLP-1 and PYY, are secreted by the enteroendocrine cells, playing a critical role in regulating food intake. Digested nutrients trigger the secretion of these hormones, which have a very short half-life. α-Linolenic acid (αLA) has been shown to stimulate GLP-1 secretion, however, chemical instability and fast uptake in the small intestine hinder its use in body weight management. We developed a novel delivery system based on inorganic mesoporous particles for αLA to increase secretion of gastrointestinal peptides. αLA was loaded to thermally hydrocarbonized porous silicon particles (THCPSi). 47.9 ± 3.84% and 30.7 ± 2.86% of αLA was released during 6 h from 3.0% and 9.2% loading degree (w/w) samples in vitro, respectively. Native αLA (50 µM) significantly increased GLP-1 secretion from enteroendocrine STC-1 and GLUTag cell lines. αLA loaded THCPSi significantly and dose dependently stimulated GLP-1 secretion from STC-1 cells, whereas empty particles did not. We demonstrated in vitro that THCPSi particles have the potential to be used as a controlled delivery system for nutrients such as αLA, increasing GLP-1 secretion. Our results justify further in vivo investigations.