Development and optimisation of biopharmaceutical properties of a new microemulgel of cannabidiol for locally-acting dermatological delivery

Abstract

Cannabidiol (CBD) is a pleiotropic phytocannabinoid, recently investigated to treat many skin diseases. This study aimed to develop a CBD-loaded O/A microemulsion (CBD-ME) formulated as microemulgel (CBD-MEgel), suitable for local administration. The developed CBD-ME consisted of Solutol HS 15 (20%, surfactant), Transcutol P (9%, cosolvent), isopropyl myristate (5%, oil phase), water (66%) and 1% w/w CBD. Globules had polydispersity index less than 0.23 ± 0.02 and size of 35 ± 2 nm; these values did not change after loading CBD and gelling the formulation with Sepigel 305 obtaining a clear and homogeneous formulation with a pH of 6.56 ± 0.20, suitable for cutaneous application. Viscosity properties were investigated by the rotational digital viscometer, at both 21 ± 2 °C and 35 ± 2 °C. Viscosities of CBD-MEgel were 439,000 ± 4,243 mPa·s and 391,000 ± 1,414 mPa·s respectively. The release studies displayed that 90 ± 24 μg/cm2 of CBD were released in 24 h. The CBD permeability, evaluated using Franz diffusion cells and rabbit ear skin, was 3 ± 1 μg/cm2. Skin-PAMPATM gave a CBD effective permeability of (1.67 ± 0.16) ·10−7 cm/s and an absorbed dose of 115.30 ± 16.99 µg/cm2 after 24 h. Lastly, physical and chemical stability of both CBD-ME and CBD-MEgel were evaluated over a period of 3 months, showing optimal shelf-life at the storage conditions.