University of Oulu

Remi Kamakura, Miia Kovalainen, Joakim Riikonen, Tuomo Nissinen, Ghulam Shere Raza, Jaroslaw Walkowiak, Vesa-Pekka Lehto, Karl-Heinz Herzig, Inorganic mesoporous particles for controlled α-linolenic acid delivery to stimulate GLP-1 secretion in vitro, European Journal of Pharmaceutics and Biopharmaceutics, Volume 144, 2019, Pages 132-138, ISSN 0939-6411,

Inorganic mesoporous particles for controlled α-linolenic acid delivery to stimulate GLP-1 secretion in vitro

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Author: Kamakura, Remi1; Kovalainen, Miia1; Riikonen, Joakim2;
Organizations: 1Research Unit of Biomedicine, Biocenter of Oulu, Medical Research Center, Faculty of Medicine, University of Oulu, and Oulu University Hospital, Oulu, Finland
2Department of Applied Physics, Faculty of Science and Forestry, University of Eastern Finland, Kuopio, Finland
3Department of Gastroenterology and Metabolism, Poznan University of Medical Sciences, Poznan, Poland
Format: article
Version: accepted version
Access: open
Online Access: PDF Full Text (PDF, 1.4 MB)
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Language: English
Published: Elsevier, 2019
Publish Date: 2019-11-15


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.

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Series: European journal of pharmaceutics and biopharmaceutics
ISSN: 0939-6411
ISSN-E: 1873-3441
ISSN-L: 0939-6411
Volume: 144
Pages: 132 - 138
DOI: 10.1016/j.ejpb.2019.09.009
Type of Publication: A1 Journal article – refereed
Field of Science: 3111 Biomedicine
Funding: The financial support from Biocenter of Oulu (RK), and Academy of Finland (#287625) (MK) are acknowledged.
Academy of Finland Grant Number: 287625
Detailed Information: 287625 (Academy of Finland Funding decision)
Copyright information: © 2019 Elsevier B.V. All rights reserved. This manuscript version is made available under the CC-BY-NC-ND 4.0 license