Innovations in Pharmacology: Enhancing Bioavailability and Efficacy through Novel Compositions

Abstract

This Patent Highlight explores ground-breaking advancements in pharmaceutical compositions, revealing the integration of serotonergic tryptamine compounds and microbial-produced biosurfactants. These innovations aim to enhance the bioavailability and efficacy of health-promoting substances significantly. The article examines the existing challenges in pharmacological treatments and the inventive solutions proposed by recent developments. It discusses compositions that reduce inflammation and improve mental and physical health, the use of serotonergic tryptamine compounds in mood and neurological disorders, and novel methods for boosting bioavailability with biosurfactants. The article provides an overview of these strategies and their potential to influence future pharmacological approaches.

Important Compound Classes

Titles

Compositions for Reducing Inflammation to Improve or Maintain Mental or Physical Health; Compositions Comprising a Serotonergic Tryptamine Compound; and Compositions for Enhancing Bioavailability of Pharmaceuticals, Supplements and Ingested Substances

Patent Publication Numbers

US 2023/0405028 A1 (URL: https://patents.google.com/patent/US20230405028A1/en?oq=US+2023%2f0405028+A1)

US 2023/0404975 A1 (URL: https://patents.google.com/patent/US20230404975A1/en?oq=US+2023%2f0404975+A1)

US 2023/0405127 A1 (URL: https://patents.google.com/patent/US20230405127A1/en?oq=US+2023%2f0405127+A1)

Publication Date

December 21, 2023

Priority Applications

US 18/248,626; US 18/462,087; US 18/460,763

Priority Dates

October 12, 2021; September 6, 2023; September 5, 2023

Inventors

Hudson, D. D.; Selkirk, I, V. (US 2023/0405028 A1); Chaddeayne, A. R. (US 2023/0404975 A1); Lefkowitz, A. R.; Farmer, S.; Alibek, K. (US 2023/0405127 A1)

Assignee Companies

Goodcap Pharmaceuticals, Ltd., Toronto, Canada (US 2023/0405028 A1); CAAMTECH, Inc., Issaquah, WA, USA (US 2023/0404975 A1); and Locus Solutions IPCo, LLC, Solon, OH, USA (US 2023/0405127 A1)

Disease Area

Neuropsychiatric disorders

Biological Target

5-HT2A and TRP receptor

Summary

The pharmaceutical field is rapidly advancing with new patents enhancing drug efficacy and bioavailability, notably by integrating serotonergic tryptamine compounds and microbial-produced biosurfactants. These innovations tackle challenges like drug solubility and targeted efficacy, employing nanotechnology to improve drug delivery across the blood–brain barrier. This is particularly significant in treating neurodegenerative diseases like Alzheimer’s disease. The modulation of 5-HT2A serotonin receptors and transient receptor potential (TRP) receptors is pivotal in addressing pain, mood disorders, and inflammation. Combining 5-HT2A agonists with TRP receptor modulators promises enhanced treatment efficacy for neurological and psychological disorders.

Patent application US 20230405028 A1 introduces an innovative approach in medicinal therapy, centering on compositions that aim to reduce inflammation and enhance mental and physical health. It highlights the use of serotonergic tryptamine compounds, specifically targeting the 5-HT2A serotonin receptor, along with TRP receptor agonists, to modulate mood, pain perception, and inflammation.

This patent reflects a shift from traditional pharmaceutical methods to a multimodal therapeutic strategy that addresses multiple metabolic pathways. It underscores the connection between metabolism, inflammation, and mental health, emphasizing the roles of energy, sugar metabolism, and gut–brain interactions. A key aspect is the determination of minimum effective doses for various compounds, including natural 5-HT2A agonists from sources like morning glory and Hawaiian baby woodrose seeds.

A critical finding is the synergistic effect of combining 5-HT2A agonists, such as psilocybin, with different TRP agonists, leading to a significant reduction in inflammatory markers in human cells. This patent explores a wide range of these compounds, demonstrating diverse effects on inflammation and mood-related markers. Additionally, it examines the impact on neurological markers like GABA and BDNF, indicating potential benefits for mental health. This patent sets a new direction in pharmaceutical therapies, offering more effective and holistic treatments for mental and physical health conditions.

Patent application US 20230404975 A1 delves into compositions comprising serotonergic tryptamine compounds for treating neurological and mood disorders. This patent highlights the potential of psilocybin derivatives in psychiatric and neurological therapeutics. It proposes novel formulations that combine different purified psilocybin derivatives with other compounds like terpenes and serotonergic drugs, including LSD and MDMA. The focus is on developing tailored treatments that leverage the mood-altering properties of these compounds with reduced side effects and improved efficacy.

Patent application US 20230405127 A1 presents a method to enhance the bioavailability of health-promoting substances, including pharmaceuticals and nutritional supplements, using microbial-produced biosurfactants. This innovation may address the challenge of low bioavailability in many drugs due to poor solubility and efflux by cellular mechanisms like P-glycoprotein (P-gp). By incorporating biosurfactants, this innovation seeks to improve the absorption and effectiveness of various health-promoting substances. This approach can reduce required dosages, minimize side effects, and enhance therapeutic efficacy.

Integrating these novel approaches could revolutionize the pharmacological landscape. Combining serotonergic tryptamine compounds and biosurfactants opens new drug formulation and delivery avenues. These patents collectively address the need for more effective, targeted, and patient-friendly pharmacological interventions.

One of the key aspects of these patents is their focus on natural and biological sources. Using compounds derived from psilocybin-containing mushrooms and biosurfactants produced by microorganisms reflects a growing trend in pharmacology to harness natural substances for therapeutic purposes. This approach promises enhanced efficacy and aligns with a more holistic view of health and treatment.

Conclusion and Future Directions: These patents may significantly influence pharmacological research and development. They offer promising solutions to long-standing drug delivery and efficacy challenges, particularly in treating mood and neurological disorders. As research continues to unfold, these innovative strategies are expected to pave the way for more effective and personalized treatment options, benefiting a wide range of patients across various therapeutic areas. Integrating natural compounds and novel formulation techniques highlighted in these patents may likely influence future drug development, marking a new era in pharmacology focused on efficacy, safety, and patient-centric treatments.

Biological Assay

Treatment of human small intestinal epithelial cells (HSIEC) and A-172 cells with compounds like eugenol, capsaicin, curcumin, psilocybin, and other related agonists. The cells were exposed to inflammatory conditions, typically induced by agents like TNF-α and IFN-γ, to simulate an inflammatory response.

Biological Data

In HSIEC cells, TRP and 5-HT2A agonists, especially psilocybin and eugenol, significantly reduced COX-2 and IL-6, indicating anti-inflammatory effects. In A-172 cells, these compounds also impacted neurological markers like GABA and BDNF, suggesting broader neurotherapeutic potential.

Recent Review Articles

See refs (1−6).

The author declares no competing financial interest.