Hemp proteins conjugated with green tea polyphenol extract form de novo plant-sourced emulsifiers suitable for nanodelivery systems bearing lipophilic psychopharmaceuticals

OpenAlex  – February 27, 2025

Source: OpenAlex

Summary

A novel biocompatible emulsifier combining hemp protein with green tea polyphenols effectively enhances the stability and bioavailability of 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT). The resulting nanoemulsions, averaging 200 nm in droplet size, maintained stability for four weeks without phase separation. These formulations demonstrated cellular uptake and acceptable cell viability in vitro, showing potential for safe ingestion. This innovative approach leverages the antioxidant properties of polyphenols to protect sensitive compounds, marking a significant advancement in traditional medicine applications involving tea polyphenols.

Abstract

Nanoformulation is often used to improve the solubility and uptake of bioactives; however, it also protects sensitive bioactives from chemical decomposition. We report a class of biocompatible emulsifiers created by conjugating hemp protein with green tea polyphenols. A simple pH-assisted coupling protocol was employed to synthesize covalent and non-covalent conjugates, which were then used to produce 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) enriched hemp oil nanoemulsions in water with an average droplet sizes of ca. 200 nm and ζ potential values of ca. -40 mV. Our de novo emulsifiers protected the sensitive drug under conditions of simulated oxidative stress, an indication that the antioxidant properties of polyphenols are retained. These emulsions were resistant to a wide variety of emulsion-breaking stressors and demonstrated remarkable colloidal stability over a period of 4 weeks with no evidence of phase separation. Fluorescence and confocal imaging confirmed cellular uptake of the formulation, while in vitro cytotoxicity assays showed acceptable cell viability with drug-loaded nanoemulsions. This represents an ingestible 5-MeO-DMT formulation; the sensitivity of this molecule mandates some form of formulation for reasonable bioavailability and reproducible dosages.

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