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When a drug is taken orally, it undergoes a journey starting from the gastrointestinal (GI) tract, passing through the portal vein, reaching the liver, and finally entering the systemic circulation. This process involves the absorption of the drug across the GI tract. The liver is the primary site for metabolizing the drug, with some metabolism also occurring in the gut wall. This journey significantly reduces the quantity of the drug that reaches the systemic circulation, a phenomenon known as...
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The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
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The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
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The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
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Strategies to Improve Cannabidiol Bioavailability and Drug Delivery.

Saoirse Elizabeth O'Sullivan1, Sanne Skov Jensen2, Aditya Reddy Kolli3

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Novel oral cannabidiol (CBD) delivery strategies, like lipid-based formulations, enhance CBD pharmacokinetics (PK). Different administration routes offer varied delivery speeds, but clinical efficacy requires further research.

Keywords:
cannabidiolclinicaldiseasepharmacodynamicspharmacokineticsroute of administrationtissue distribution

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Area of Science:

  • Pharmacology
  • Drug Delivery Systems
  • Cannabinoid Research

Background:

  • Cannabidiol (CBD) exhibits poor physicochemical properties, hindering its clinical application.
  • Developing effective delivery methods is crucial for optimizing CBD's therapeutic potential.

Purpose of the Study:

  • To review novel oral products and delivery strategies for CBD.
  • To assess the clinical implications and translatability of these CBD delivery methods.

Main Methods:

  • Literature evaluation of published studies on oral CBD delivery.
  • Analysis of various formulation types, including lipid-based and emulsion solutions.
  • Review of alternative administration routes beyond oral delivery.

Main Results:

  • Lipid-based and emulsion formulations significantly improve CBD pharmacokinetics (PK).
  • Some oral CBD emulsions provide faster systemic delivery.
  • Diverse administration routes (intranasal, inhalation, transdermal, transmucosal, intramuscular, subcutaneous) show potential for specific applications.
  • CBD distribution to brain regions can be enhanced by certain products.

Conclusions:

  • Novel oral and alternative CBD delivery strategies show promise for improving PK and tissue distribution.
  • Further research is needed to correlate altered PK profiles and tissue distribution with enhanced therapeutic efficacy.
  • Identifying specific CBD products suitable for particular indications remains an area for investigation.