Novel Thermosensitive Hydrogel Encapsulated Carvedilol for the Treatment of Rosacea.

BACKGROUND

Carvedilol can be used in the treatment of rosacea. However, their oral administration often results in a series of adverse effects.

PURPOSE: A novel thermosensitive hydrogel was developed to improve the administration of carvedilol in the treatment of rosacea and to evaluate its safety and efficacy.

METHODS

The thermosensitive hydrogel was formulated using varying ratios of poloxamer 407 (P407) and poloxamer 188 (P188), with carvedilol being encapsulated during the process. The gel temperature and time of the hydrogel were observed, its phase transition was assessed through the inverted tube test, its microstructure was examined using scanning electron microscopy (SEM), and its characteristic functional groups were identified with Fourier transform infrared spectrometry (FTIR). The hydrogel's therapeutic efficacy on a rosacea-like phenotype in mice was evaluated through in vitro experiments.

RESULTS

It is observed that the microstructure of the hydrogel possesses a porous structure, with pores uniformly arranged in a square lattice measuring 8-12 μm in diameter. Thermosensitive hydrogel encapsulated carvedilol (Car-P40724/P1881) had favorable drug release rate and swelling properties. Live/dead cell assays indicated minimal toxicity of the hydrogel to HaCaT cells, and the carvedilol encapsulated with hydrogel possessed a better therapeutic effect on the rosacea-like phenotype in mice.

CONCLUSION

Car-P40724/P1881 was not significantly cytotoxic and possessed good cellular biocompatibility. Furthermore, it exhibits a good therapeutic effect on rosacea-associated facial flushing and erythema. It possesses some anti-inflammatory properties and exhibits great potential for future use in rosacea treatment.