Tag Archives: anti-inflammatory

Curcumin nanoemulsion for treatment of intestinal inflammation

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Most of my posts about research into curcumin (which is derived from turmeric) treatments has been based in India but this work according to a March 7, 2024 news item on phys.org comes from Brazil, Note: If you’re interested in more about turmeric/curcumin, I have a link to more information at the end of this posting,

A nanoemulsion containing particles of curcumin, which is known to have anti-inflammatory and antioxidant properties, has been found capable of modulating the gut microbiota of mice with intestinal inflammation in experiments conducted by researchers at the University of Western São Paulo (UNOESTE) and São Paulo State University (UNESP) in Brazil.

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The image being used to illustrate an aspect of this research is a bit of a mystery. Is curcumin bright orange? And, it seems like a lot for a mouse,

Caption: The nanoemulsion enhanced the bioavailability of the curcumin and resulted in increased abundance of beneficial bacteria in the murine gut microbiota. Credit: UNOESTE

A March 6, 2024 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) press release (also on EurekAlert but published March 7, 2024) by Thais Szegö, which originated the news item, Note: Links have been removed,

Curcumin, a natural substance belonging to the group of bioactive compounds called curcuminoids, is a yellow polyphenolic pigment found in the turmeric plant (Curcuma longa). It has gained prominence in treatments to combat inflammatory intestinal disorders, but its bioavailability is low when it is administered orally. This problem is exacerbated in patients with Crohn’s disease, ulcerative colitis and other conditions associated with inflammation of the digestive tract and gut microbiota alterations. 

To enhance the efficacy of curcumin in such cases, the scientists developed an emulsion containing nanometric particles of the compound (invisible to the naked eye). “The research comprised two stages. The first entailed producing a nanoemulsion to deliver the curcumin. In the second, we evaluated its stability, morphology and physicochemical properties,” said Lizziane Kretli Winkelströter Eller, last author of the article and a professor at UNOESTE. 

Next, to test the action of the nanoemulsion in mice, the researchers induced intestinal inflammation using a drug called indomethacin and administered the nanoemulsion orally for 14 days. At the end of this period, they evaluated the intestinal inflammation by macroscopic, histopathological and metagenomic analysis.

The results showed that the nanoemulsion effectively improved the bioavailability of curcumin and modulated the gut microbiota of the mice after the damage was caused by the drug, increasing the presence there of beneficial bacteria. “The nanoemulsion didn’t lead to a significant improvement in the intestinal inflammation, but the relative abundance of Lactobacillus bacteria was about 25% higher in the mice treated with curcumin nanoemulsion than in the control group,” Eller said.

The authors of the study, the first to measure the effects of curcumin nanoemulsion in this way, stressed the importance of developing novel formulations that enhance the efficacy of curcumin in preventing and treating inflammatory bowel disease, since it has proved to be a valid alternative to existing treatments, which are expensive and have significant side effects. 

The group continues to conduct research on the potential of nanoformulations to deliver nutraceuticals (food elements of plant or animal origin with significant health benefits). “Specifically with regard to the curcumin nanoemulsion, we’re adjusting the formulation to increase the bioavailability of the active ingredient and will soon apply it in other protocols for the prevention and treatment of intestinal damage,” Eller said. 

About São Paulo Research Foundation (FAPESP)

The São Paulo Research Foundation (FAPESP) is a public institution with the mission of supporting scientific research in all fields of knowledge by awarding scholarships, fellowships and grants to investigators linked with higher education and research institutions in the State of São Paulo, Brazil. FAPESP is aware that the very best research can only be done by working with the best researchers internationally. Therefore, it has established partnerships with funding agencies, higher education, private companies, and research organizations in other countries known for the quality of their research and has been encouraging scientists funded by its grants to further develop their international collaboration. You can learn more about FAPESP at www.fapesp.br/en and visit FAPESP news agency at www.agencia.fapesp.br/en to keep updated with the latest scientific breakthroughs FAPESP helps achieve through its many programs, awards and research centers. You may also subscribe to FAPESP news agency at http://agencia.fapesp.br/subscribe.

Here’s a link to and a citation for the paper,

Evaluation of curcumin nanoemulsion effect to prevent intestinal damage by Maria Vitória Minzoni de Souza Iacia, Maria Eduarda Ferraz Mendes, Karolinny Cristiny de Oliveira Vieira, Gilia Cristine Marques Ruiz, Carlos José Leopoldo Constantino, Cibely da Silva Martin, Aldo Eloizo Job, Gisele Alborghetti Nai, and Lizziane Kretli Winkelstroter Eller. International Journal of Pharmaceutics Volume 650, 25 January 2024, 123683 DOI: https://doi.org/10.1016/j.ijpharm.2023.123683

This paper is behind a paywall.

For the curious, Johns Hopkins Medical School has a posting by Mary-Eve Brown about turmeric, its benefits, and its use in Ayurvedic medicine.

Quebecol, a maple syrup-based molecule, could be used as an anti-inflammatory

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I think this is the first time I’ve had any research from Université Laval (Québec; Laval University) and it seems fitting that it would involve maple syrup. From a Dec. 22, 2015 Université Laval news release on EurekAlert,

Arthritis and other inflammatory diseases could someday be treated with medication containing a molecule from maple syrup. Université Laval researchers demonstrated in a recent study that quebecol, a molecule found in maple syrup, has interesting properties for fighting the body’s inflammatory response.

Discovered in 2011, quebecol is the result of chemical reactions during the syrup-making process that transform the naturally occurring polyphenols in maple sap. After successfully synthesizing quebecol and its derivatives, Université Laval researchers under the supervision of Normand Voyer, a chemist with the Faculty of Science and Engineering, evaluated its anti-inflammatory properties. They called on colleague Daniel Grenier of the Faculty of Dentistry, who developed an in vitro model for determining the anti-inflammatory potential of natural molecules. “We take blood cells called macrophages and put them with bacterial toxins,” explained Professor Grenier. “Macrophages usually react by triggering an inflammatory response. But if the culture medium contains an anti-inflammatory molecule, this response is blocked.”

The researchers carried out tests that showed quebecol curbs the inflammatory response of macrophages, and some derivatives are even more effective than the original molecule. “The most powerful derivative has a simpler structure and is easier to synthesize than quebecol,” said Normand Voyer. “This paves the way for a whole new class of anti-inflammatory agents, inspired by quebecol, that could compensate for the low efficacy of certain treatments while reducing the risk of side effects.”

Here’s a link to and a citation for the paper,

Anti-inflammatory properties of quebecol and its derivatives by Sébastien Cardinal, Jabrane Azelmat, Daniel Grenier, Normand Voyer. Bioorganic & Medicinal Chemistry Letters         doi:10.1016/j.bmcl.2015.11.096 Available online 27 November 2015

This paper is behind a paywall.

Self-assembling nanofibres could help mitigate side effects from pain killers

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The research itself is pretty exciting but even more so is the fact that it was conducted by an undergraduate student. From an April 3, 2015 news item on Azonano,

A Chemistry undergraduate at the University of York [UK] has helped to develop a new drug release gel, which may help avoid some of the side effects of painkillers such as ibuprofen and naproxen.

In a final year project, MChem undergraduate student Edward Howe, working in Professor David Smith’s research team in the Department of Chemistry at York looked for a way of eliminating the adverse side-effects associated pain-killing drugs, particularly in the stomach, and the problems, such as ulceration, this could cause patients.

A March 31, 2015 University of York press release, which originated the news item, describes the research in more detail,

Supervised by PhD student Babatunde Okesola, whose research is supported by The Wild Chemistry Scholars Fund, Edward hoped to create gels which could interact with drugs such as Naproxen, and release them at the slightly alkaline pH values found in the intestine rather than the acidic conditions in the stomach.  His aim was to both protect the pain-killing drugs and help limit some of the side effects they can cause.

The researchers created a new gel, based on small molecules which self-assemble into nanofibers which could interact with a variety of anti-inflammatory, painkiller drugs, including iburofen and naproxen. The research is published in Chemical Communications.

Specific interactions between the gel nanofibres and the drugs meant that high loadings could be achieved, and more importantly, the release of the drug could be precisely controlled.  The gels were able to release naproxen at pH 8 – the value found in the intestine, but not at lower pH values found elsewhere in the body.

Professor Smith said: “Although researchers have used gels before to try and improve the formulation of naproxen, this is the first time that a self-assembling system has been used for the job, with the advantages of directed interactions between the nanoscale delivery scaffold and the drug.  As such, this is the first time that such precise control has been achieved.”

Edward Howe said: “The research really fascinated me. The prospect of being involved in developing a method to reduce the pain of others filled me with great pride. Understanding the interactions between the gel and the painkillers was very interesting and improved my knowledge of supramolecular chemistry.”

The next step for Professor Smith’s team will involve stabilising the gel drug delivery systems in the very acidic, low pH conditions found in the stomach so that they can transit safely to the intestine before delivering naproxen just where it is needed.

Professor Smith added: “Perhaps this is something that one of next year’s undergraduate project students might solve. As a research-intensive institution, York is committed to its undergraduates carrying out cutting-edge research such as this.”

Here’s a link to and a citation for the paper,

Self-assembled sorbitol-derived supramolecular hydrogels for the controlled encapsulation and release of active pharmaceutical ingredients by Edward J. Howe, Babatunde O. Okesola, and David K. Smith. Chem. Commun., 2015, Advance Article DOI: 10.1039/C5CC01868D First published online 31 Mar 2015

This paper is behind a paywall.