The present work aimed to evaluate the behavior of dexamethasone-loaded cationic polymericnanocapsules in hydrogels, regarding their in vitro drug release and skin drug retention and per- meation. Cationic polymeric nanocapsules prepared with Eudragit RS 100 as the polymeric wall had mean particle size of 139 +/- 3.6 nm, positive zeta potential (+11.38 +/- 1.7 mV), and high encapsulation efficiency (81 +/- 2%). After preparation, they were formulated as hydrogels, which showed non-Newtonian, plastic behavior, and acidic pH. Photon correlation spectroscopy analysis of these hydrogels demonstrated the presence of particles with mean particle size close to that of the original colloidal suspensions. The presence of dexamethasone-loaded nanocapsules in hydrogels promoted controlled drug release and an increase in the amount of drug delivered into viable epidermis, the main target tissue to topical glucocorticoid action. Moreover, the formulation did not increase the risk of drug penetration to dermis and permeation to the receptor compartment.
Topical glucocorticoids (TG) such as dexamethasone (DEX) have been used for decades for the treatment of skin diseases. However, TG present welldocumented side effects and their delivery to the skin is often insufficient.Therefore, many efforts have been undergone to improve the amount of drug delivered to the skin and to reduce side effects at the same time. In this work, the feasibility of DEX-submicron polymeric particles (SP) prepared by vibrational spray-drying as an approach to overcome the challenges associated with the topical administration of this drug class was evaluated. DEX was homogeneously dispersed in the SP matrix, according to confocal Raman microscopy analysis. Drug-loaded SP were incorporated into the oil phase of oil-in-water emulsions (creams). The formulation containing polymeric submicron particles (C-SP) showed controlled drug release kinetics and a significant drug accumulation in skin compared to formulations containing nonpolymeric particles or free drug. DEX accumulation in the stratum corneum was evaluated by tape stripping and a depot effect over time was observed for C-SP, while the formulation containing the free drug showed a decrease over time.Similarly, C-SP presented higher drug retention in epidermis and dermis in skin penetration studies performed on pig skin in Franz diffusion cells, while drug permeation into the receptor compartment was negligible. It was demonstrated, for the first time, the advantageous application of submicron polymeric particles obtained by vibrational spray-drying in semisolid formulations for cutaneous administration to overcome challenges related to the therapy with TG such as DEX.
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