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

• Published in: International journal of nanomedicine Vol. 19; pp. 4321 - 4337
• Main Authors: Chu, Po-Cheng, Liao, Man-Hua, Liu, Mao-Gu, Li, Cun-Zhao, Lai, Ping-Shan
• Format: Journal Article
• Language: English
• Published: New Zealand Dove Medical Press Limited 01.01.2024; Dove; Dove Medical Press
• Subjects: Administration, Cutaneous; Animals; Biological Availability; cannabidiol; Cannabidiol - administration & dosage; Cannabidiol - chemistry; Cannabidiol - pharmacokinetics; Drug Carriers - chemistry; Drug Carriers - pharmacokinetics; Drug delivery systems; drug patch; Drugs; Health aspects; Male; Micelles; nano emulsion; nanocarrier; Nanoparticles - chemistry; Original Research; Particle Size; pharmacokinetics; Rats; Rats, Sprague-Dawley; Skin; Skin - drug effects; Skin - metabolism; Skin Absorption - drug effects; transdermal; Transdermal Patch; Vehicles; Taiwan; cannabidiol; drug patch; pharmacokinetics; nanocarrier; nano emulsion; transdermal
• ISSN: 1178-2013; 1176-9114; 1178-2013
• DOI: 10.2147/IJN.S455032

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