Key Transdermal Patch Using Cannabidiol-Loaded Nanocarriers with Better Pharmacokinetics in vivo

Int J Nanomedicine. 2024 May 16:19:4321-4337. doi: 10.2147/IJN.S455032. eCollection 2024.

Abstract

Purpose: Cannabidiol (CBD) is a promising therapeutic drug with low addictive potential and a favorable safety profile. However, CBD did face certain challenges, including poor solubility in water and low oral bioavailability. To harness the potential of CBD by combining it with a transdermal drug delivery system (TDDS). This innovative approach sought to develop a transdermal patch dosage form with micellar vesicular nanocarriers to enhance the bioavailability of CBD, leading to improved therapeutic outcomes.

Methods: A skin-penetrating micellar vesicular nanocarriers, prepared using nano emulsion method, cannabidiol loaded transdermal nanocarriers-12 (CTD-12) was presented with a small particle size, high encapsulation efficiency, and a drug-loaded ratio for CBD. The skin permeation ability used Strat-M™ membrane with a transdermal diffusion system to evaluate the CTD and patch of CTD-12 (PCTD-12) within 24 hrs. PCTD-12 was used in a preliminary pharmacokinetic study in rats to demonstrate the potential of the developed transdermal nanocarrier drug patch for future applications.

Results: In the transdermal application of CTD-12, the relative bioavailability of the formulation was 3.68 ± 0.17-fold greater than in the free CBD application. Moreover, PCTD-12 indicated 2.46 ± 0.18-fold higher relative bioavailability comparing with free CBD patch in the ex vivo evaluation. Most importantly, in the pharmacokinetics of PCTD-12, the relative bioavailability of PCTD-12 was 9.47 ± 0.88-fold higher than in the oral application.

Conclusion: CTD-12, a transdermal nanocarrier, represents a promising approach for CBD delivery, suggesting its potential as an effective transdermal dosage form.

Keywords: cannabidiol; drug patch; nano emulsion; nanocarrier; pharmacokinetics; transdermal.

MeSH terms

  • Administration, Cutaneous*
  • Animals
  • Biological Availability*
  • Cannabidiol* / administration & dosage
  • Cannabidiol* / chemistry
  • Cannabidiol* / pharmacokinetics
  • Drug Carriers* / chemistry
  • Drug Carriers* / pharmacokinetics
  • Male
  • Micelles
  • Nanoparticles* / chemistry
  • Particle Size
  • Rats
  • Rats, Sprague-Dawley
  • Skin / drug effects
  • Skin / metabolism
  • Skin Absorption* / drug effects
  • Transdermal Patch*

Grants and funding

This research was funded by the Powin Biomedical Co., Ltd.