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Scientific study suggests that mesoporous silica particles (MSPs) interact with the lipid digestion and absorption pathways to reduce calorific uptake

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Stockholm, March 21st, 2022: Sigrid Therapeutics today announced the publication of a multifaceted, scientific study in the peer-reviewed journal European Journal of Pharmaceutics and Biopharmaceutics suggesting that interactions between micron-sized mesoporous silica particles (MSPs), lipid digestion and absorption pathways are a likely mechanism for reducing calorific uptake. The results are compatible with previous findings that the mode of action for MSPs acting as “molecular sieves” block food enzyme activity.

Several previous studies, both in animals and in man, have shown promising results when it comes to applying mesoporous silica particles (MSPs) to prevent type 2-diabetes and treat obesity. In these studies, the MSPs were administered orally in solution and passed harmlessly from the body in stools. In the current study the interaction of MSPs with the lipid digestion process was investigated, specifically interactions with lipase enzymes and lipid digestion products as a key contributing factor to lipid absorption and calorific intake.

The study report comprising a combination of in vitro and in vivo data shows:

  1. Particles that inhibited lipase activity also tended to interact more extensively with lipid digestion products1
  2. The interaction of some MSPs with lipid digestion products occurred through changes in lipid self-assembly during digestion2
  3. The MSPs added to milk led to reduced lipid absorption in vivo compared to the control particles and MSP-free milk3

Professor Tore Bengtsson, Stockholm University and Sigrid Co-founder and CSO, who lead the research comments: “This study is the result of a successful collaboration with Ben J. Boyd’s research groups in Parkville in Australia. By applying their set of research tools to MSPs, we have been able to extend the characterization of how MSPs exert their effect on lipid metabolism and adsorption. The results fully support our original concept of using MSPs as “molecular sieves” to prevent type 2-diabetes and treat obesity.”

“The digestion of food and subsequent absorption of calorific components is a complex process. This research clearly indicates a link between material structure and the processing of fat under gastrointestinal conditions that can lead to reduced absorption when MSPs are present compared to in their absence”, says Ben J. Boyd, Professor in Drug Delivery Sciences, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.

Sigrid is now advancing its plans to conduct its pivotal clinical study SHINE with its proprietary MSPs targeting glycemic control and body weight in obese and overweight prediabetics and newly diagnosed type 2 diabetics. 

Experimental methods

1The impact of exposing lipase to MSPs on the enzyme activity was assessed directly using the tributyrin digestion test.

2The extent of interaction of digestion products with MSPs was studied using selectively radio labeled bile components and lipids

3The impact on in vivo absorption of lipids was studied by incorporation of radiolabelled lipid (triolein) into milk and administration with and without particles to Male Sprague Dawley rats

Title and link to the scientific publication:

Towards mesoporous silica as a pharmaceutical treatment for obesity - impact on lipid digestion and absorption, European Journal of Pharmaceutics and Biopharmaceutics, Volume 173, April 2022, Pages 1-11 https://www.sciencedirect.com/science/article/pii/S0939641122000224

For more information, please contact:

Tore Bengtsson, Professor at the Department of Molecular Biosciences, Stockholm University

Phone +46 70 5473994,

Email: Tore.Bengtsson@su.se

Ben J. Boyd, Professor and Head of Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia

Phone +61 99039112

Email: ben.boyd@monash.edu 

About Mesoporous silica particles (MSP)

Mesoporous silica particles (MSP) are a type of ingestible synthetic amorphous silica particles that can be produced with a large surface area and a range of pore sizes. Studies in mice, published in Nanomedicine1,2 have shown that MSP induced weight loss in obese mice and that food efficiency was reduced by 33% leading to a positive effect on metabolic profile with significant lower levels of adipose tissue formation and leptin, together with lower levels of circulating insulin. Weight gain was thus sufficiently attenuated. Further in vivo studies have shown that MSP led to reduced lipid adsorption in a post-prandial model3. Additional pre-clinical results published in Advanced Healthcare Materials4 confirm these findings and are compatible with a mode of action whereby a portion of the enzymes are trapped inside the MSPs resulting in an enzyme-blocking effect reducing the break down food and thus reduce the energy uptake into the body.

About Sigrid Therapeutics

Sigrid Therapeutics (Sigrid) is a clinical-stage technology startup pioneering a new class of naturally sourced, carefully engineered porous minerals to prevent and treat metabolic disease and disorders, including type 2 diabetes. The Company’s lead product candidate, SiPore21®, is an orally-administered medical device based on the Company’s proprietary platform technology, SiPore®. Designed to act locally in the gut, SiPore®, consists of precisely engineered micron-sized silica particles with tailored porosity. Clinical data confirms SiPore®’s beneficial effects on a range of metabolic parameters and its excellent safety profile4-7. Upon its approval, SiPore21® will be the first medical device available for reduction of blood sugar levels in people at risk of developing type 2 diabetes. https://www.sigridthx.com/.

  1. Large pore mesoporous silica induced weight loss in obese mice, Nanomedicine, 2014, https://www.futuremedicine.com/doi/10.2217/nnm.13.138
  2. Mesoporous Silica with Precisely Controlled Pores Reduces Food Efficiency and Suppresses Weight Gain in Mice, Nanomedicine, 2020, https://www.futuremedicine.com/doi/10.2217/nnm-2019-0262
  3. Towards mesoporous silica as a pharmaceutical treatment for obesity - impact on lipid digestion and absorption, European Journal of Pharmaceutics and Biopharmaceutics, 2022, https://doi.org/10.1016/j.ejpb.2022.02.001
  4. Entrapping Digestive Enzymes with Engineered Mesoporous Silica Particles Reduces Metabolic Risk Factors in Humans, Advanced Healthcare Materials, 2020, https://doi.org/10.1002/adhm.202000057
  5. Engineered Silica Particles Work as a Molecular Sieve and Reduce Metabolic Risk Factors in Obese Male Volunteers, presented at the ADA 2019 Scientific Session, available on: https://ada.scientificposters.com
  6. Oral intake of mesoporous silica is safe and well tolerated in male humans, PLoS ONE, 2020, DOI: 10.1002/adhm.202000057  
  7. Engineered mesoporous silica reduces long-term blood glucose, HbA1c, and improves metabolic parameters in prediabetics, Nanomedicine, 2021, https://doi.org/10.2217/nnm-2021-0235

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