Beclomethasone Dipropionate

Beclomethasone dipropionate increases maximum isometric force production in isolated mouse slow-twitch skeletal muscle fibres without affecting fast-twitch fibres. This effect occurs within ten minutes of drug exposure and is insensitive to the transcriptional inhibitor actinomycin D, indicating a non-genomic mechanism independent of gene transcription. The force enhancement is maximal at approximately 250 nM and is blocked by the glucocorticoid receptor inhibitor mifepristone as well as by a monoclonal antibody against the glucocorticoid receptor. Immunohistochemical analysis reveals that a membrane-associated glucocorticoid receptor is present only in slow-twitch fibres, localised predominantly at the fibre periphery where it co-localises with laminin in the extracellular matrix. Fast-twitch fibres express only the cytoplasmic glucocorticoid receptor and lack the membrane-associated form.

Fig. 1 Possible pathways mediating the genomic and non-genomic effects of glucocorticoids. (Pérez M H A.; et al. 2013)

Beclomethasone dipropionate loaded mixed micelles were prepared using the thin-film hydration technique with pluronic L121 combined with either poloxamer P84 or pluronic F127. The optimized formulation was incorporated into a hydroxypropyl methylcellulose hydrogel for dermal delivery. Ex vivo skin deposition studies demonstrated superior dermal accumulation compared to the commercial cream Beclozone. In vivo histopathological evaluation in a sub-chronic dermatitis animal model showed that the micelle-loaded hydrogel successfully treated dermatitis within a shorter period, achieving better patient compliance and fewer side effects than the commercial product.

Fig. 2 Predicted and observed responses of the Chosen BDP-Loaded MX formulae. (Assem M.; et al. 2019)