Abstract
Transmucosal drug delivery represents a promising noninvasive option when drugs are employed which have a low oral bioavailability like CBD. However, this concept can only be successful as long as the formulation provides sufficient buccal retention and mucosal penetration. In this study, mucoadhesive carrier systems were evaluated consisting of CBD-loaded silica (Aeroperl 300) carriers, mucoadhesive polymers (Hypromellose (HPMC), chitosan and carbomer) and propylene glycol as a penetration enhancer. Mucoadhesive effect, drug release and penetration ability were evaluated for each carrier system. The results show that the addition of HPMC and carbomer substantially improve mucoadhesion compared to pure CBD, with an increase of 16-fold and 20-fold, respectively. However, due to their strong swelling, HPMC and carbomer hinder the penetration of CBD and rely on co-administration of propylene glycol as an enhancer to achieve sufficient mucosal absorption. Chitosan, on the other hand, achieves an 8-fold increase in mucoadhesion and enhances the amount of CBD absorbed by three times compared to pure CBD. Thus, chitosan represents a promising polymer to combine both effects. Considering the results, the development of silica-based buccal drug delivery systems is a promising approach for the effective delivery of CBD.
Highlights
Cannabidiol (CBD) is a non-psychoactive cannabinoid isolated from the Cannabis sativa plant [1] or derived by chemical synthesis [2]
No melting peak of crystalline CBD was obtained in the DSC measurement of the CBD-loaded mesoporous silica (Figure 2), indicating that CBD was fully incorporated the CBD-loaded mesoporous silica (Figure 2), indicating that CBD was fully incorporated into the silica carrier
Mucoadhesive carrier systems were prepared with 5% propylene glycol to assess whether the addition of propylene glycol has a penetration enhancing effect in the carrier systems containing a mucoadhesive polymer
Summary
Cannabidiol (CBD) is a non-psychoactive cannabinoid isolated from the Cannabis sativa plant [1] or derived by chemical synthesis [2]. Chitosan, as a biocompatible and non-toxic polymer, together with its penetration enhancing properties, is a desirable option for penetration enhancement in the oral cavity [12] Another promising option in the search for a substance classified as safe with penetration-enhancing properties is propylene glycol; which is already widely used in dermal formulations as a co-solvent and/or to enhance drug penetration [13]. Buccal drug delivery systems must maintain intimate contact with the mucosa long enough to allow drug release and absorption [8] and prevent drug loss by saliva flow in the oral cavity [14]. To counteract and prevent insufficient residence time of the drug on the mucosa, mucoadhesive polymers are incorporated in buccal delivery systems.
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