Abstract
Cannabidiol (CBD) has attracted increasing interest due to its therapeutic potential for treating numerous diseases. However, CBD is very lipophilic and has very unfavorable pharmacokinetics and low bioavailability. Efforts are focused on developing drug delivery systems for enhanced solubilization and therapeutic activity of CBD. Here, we report the preparation of original super-macroporous cryogels from 2-hydroxyethyl cellulose (HEC) and β-cyclodextrin (β-CD) designed for the topical delivery of CBD. The cryogels were synthesized by photochemical crosslinking in a frozen aqueous system, purified, and then loaded with CBD. The effect of HEC/β-CD mass ratio (100:0; 50:50; 40:60 and 20:80) in the reaction mixture on the reaction efficiency, physico-mechanical properties of cryogels, drug release profile, and antineoplastic potential were evaluated in detail. The cryogels showed a bi-phasic release behavior: initial burst release in the first 3 hours followed by slower drug release which can be beneficial in the treatment of cutaneous neoplastic diseases.
Highlights
The natural terpenophenolic compound cannabidiol from Cannabis sativa is endowed with a plethora of pharmacological activities, including analgesic, antidepressant, antiepileptic, anti-inflammatory, antioxidant, cytotoxic, and antineoplastic, among others [1,2,3,4,5,6,7,8,9]
We have reported on a nanocomposite system based on CBD-loaded polymeric micelles, embedded in a hydroxyethyl cellulose cryogel matrix [15]
Cryogels of different compositions were synthesized by photochemical crosslinking of the biocompatible and biodegradable polysaccharide hydroxyethyl cellulose (HEC) and modified oligosaccharide utics 2021, 13, x
Summary
The natural terpenophenolic compound cannabidiol from Cannabis sativa is endowed with a plethora of pharmacological activities, including analgesic, antidepressant, antiepileptic, anti-inflammatory, antioxidant, cytotoxic, and antineoplastic, among others [1,2,3,4,5,6,7,8,9] It has been the subject of numerous experimental and clinical studies and has been granted orphan drug designation for the treatment of rare pediatric forms of epilepsy [1,6,7,8]. Systems with bi-phasic release behavior (combination of burst and sustained release) might offer new perspectives for efficient therapy, providing prompt exposure of malignant cells to the initially released CBD and sustained inhibitory activity, afforded by the second drug release phase In this vein, the present contribution describes a novel drug delivery platform for the topical delivery of cannabidiol, based on CBD/β-cyclodextrin inclusion complexes within biocompatible cryogels. The effect of the HEC/β-CD mass ratio on the swelling behavior and mechanical properties of cryogels, drug loading and release profile, and antineoplastic potential was evaluated
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