Abstract
Ocular drug delivery is challenging due to the very short drug residence time and low permeability. In this work, we produce and characterize mucoadhesive mixed polymeric micelles (PMs) made of chitosan (CS) and poly(vinyl alcohol) backbones graft-hydrophobized with short poly(methyl methacrylate) blocks and use them to encapsulate cannabidiol (CBD), an anti-inflammatory cannabinoid. CBD-loaded mixed PMs are physically stabilized by ionotropic crosslinking of the CS domains with sodium tripolyphoshate and spray-drying. These mixed PMs display CBD loading capacity of 20% w/w and sizes of 100–200 nm, and spherical morphology (cryogenic-transmission electron microscopy). The good compatibility of the unloaded and CBD-loaded PMs is assessed in a human corneal epithelial cell line. Then, we confirm the permeability of CBD-free PMs and nanoencapsulated CBD in human corneal epithelial cell monolayers under liquid–liquid and air–liquid conditions. Overall, our results highlight the potential of these polymeric nanocarriers for ocular drug delivery.
Highlights
Cannabis sativa has emerged as a promising therapeutic agent to treat a broad spectrum of local and systemic diseases [1,2], and the global market is expected to grow at a compound annual growth rate of ~20% and reach USD 82.2 billion in 2027 [3]
CS favors the absorption of nanoparticles by the paracellular route by transiently opening tight junctions in different epithelia [54], including the corneal epithelium [55]
This work reports on the synthesis and characterization of mucoadhesive mixed CSPMMA30:poly(vinyl alcohol) (PVA)-PMMA16 polymeric micelles (PMs) (1:1 weight ratio) for the loading of CBD and trans-corneal delivery of CBD for potential application in inflammatory eye conditions
Summary
Cannabis sativa has emerged as a promising therapeutic agent to treat a broad spectrum of local and systemic diseases [1,2], and the global market is expected to grow at a compound annual growth rate of ~20% and reach USD 82.2 billion in 2027 [3]. Cannabidiol (CBD, Figure S1, see Supplementary Materials), one of the more than 120 phytocannabinoids produced by it [4], has neuroprotective, antiemetic, antioxidant, anti-cancer, and anti-inflammatory properties and it is not psychotropic [5]. In this context, it has been proposed in the therapy of cancer, epilepsy, pain, inflammation, and autism spectrum disorder with promising clinical results [1,2,6,7]. Oral CBD is often administered in oil or alcoholic formulations [11], and undergoes limited intestinal absorption and substantial hepatic first-pass, which results in a very low oral bioavailability (
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
