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The Synergy of Glycerol Monostearate and Cyanidin - 3 - Glucoside

When glycerol monostearate is incorporated into cyanidin - 3 - glucoside, an off - the - charts improvement in bioavailability and absorption is witnessed.

The Persistent Challenge in Pharmaceutical Manufacturing

Pharmaceutical manufacturers have long grappled with a common conundrum. While they are aware of a drug's efficacy, the task at hand is to ensure its consistent performance across all human bodies. In essence, the key lies in the effective delivery of the drug into the human system.

Understanding Bioavailability

Bioavailability is defined as the proportion of a drug that, upon administration, enters the bloodstream and reaches its intended target site in an active form. It serves as a crucial metric, reflecting the body's efficiency in absorbing and utilizing the drug.

Glycerol Monostearate: A Potent Drug Delivery System

One of the most formidable drug delivery systems in the pharmaceutical industry is glycerol monostearate (GMS), which is a glycerol ester of stearic acid. Functioning as an emulsifier and stabilizer, GMS finds application in sustained - release formulations and solubility enhancement processes. Its non - toxic nature and biocompatibility make it an ideal candidate, as it is metabolized in the body similar to dietary fats.

GMS - Enabled Enhancement of Cyanidin - 3 - Glucoside (Indigo - 3G)

Biotest has harnessed the power of GMS to enhance the absorption and bioavailability of Cyanidin - 3 - Glucoside (Indigo - 3G, available for purchase on Amazon). GMS facilitates micelle formation in the gut, thereby enabling the efficient transportation of C3G across the intestinal lining. It increases the solubility of C3G at the absorption site and supports its uptake via lipid absorption pathways. The enhanced dispersion and lipid - mediated delivery lead to increased absorption of C3G at the most relevant physiological sites.

Gene Expression and Nutrient Partitioning: C3G's Impact on Fat Cells

C3G exerts its influence on fat cells through multiple mechanisms, reducing both their size and number. These mechanisms include promoting the browning of white adipose tissue, activating AMP - activated protein kinase (AMPK), inhibiting adipogenesis, enhancing fatty acid oxidation, and reducing inflammation in adipose tissue. Collectively, these effects result in decreased fat storage, increased fat utilization, and a reduction in fat cell size and overall fat mass.

Promotion of Browning of White Adipose Tissue

• Mechanism - Browning: This process entails the conversion of white adipose tissue (WAT), which is primarily responsible for fat storage, into brown - like adipose tissue (beige fat). Beige fat is characterized by a higher mitochondrial content and increased metabolic activity.

• Effect: Brown and beige fat cells are more efficient in burning energy to generate heat (thermogenesis) compared to white fat cells.

Activation of AMP - Activated Protein Kinase (AMPK)

• Mechanism - AMPK Activation: C3G activates AMPK, an enzyme that is pivotal in maintaining cellular energy homeostasis. Activation of AMPK stimulates fatty acid oxidation and inhibits fatty acid synthesis.

• Effect: By enhancing fatty acid oxidation and reducing lipid synthesis, C3G contributes to the reduction in the size of fat cells.

Inhibition of Adipogenesis

• Mechanism - Adipogenesis: Adipogenesis is the process through which preadipocytes (precursor cells) differentiate into mature adipocytes (fat cells).

• Effect: C3G can impede the differentiation of preadipocytes into mature fat cells, thereby decreasing the overall number of fat cells.

Enhancement of Fatty Acid Oxidation

• Mechanism - Fatty Acid Oxidation: This is the process by which fatty acids are broken down to generate energy.

• Effect: Enhanced fatty acid oxidation reduces the lipid content within fat cells, leading to a decrease in their size.

Reduction of Inflammation in Adipose Tissue

• Mechanism - Inflammation: Chronic low - grade inflammation in adipose tissue is associated with obesity and can contribute to the expansion of fat cells.

• Effect: C3G mitigates inflammation in adipose tissue, which aids in restoring normal metabolic functions and reducing fat cell size.

References

• Matsukawa (2015)

• Tsuda (2008, 2011)

• Huang (2011)

• Kowalska et al. (2014)