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This study aimed to develop topical granules of finasteride (FIN) with a follicular targeting potential to treat androgenic alopecia. In this sense, FIN inclusion complexes with cyclodextrin produced by two different methods (nanospray-drying and rotary evaporation) were inserted into polymeric matrices by hot-melt extrusion (HME) and evaluated regarding their physicochemical properties, skin permeation, and follicular targeting capacities. While rotary evaporation produces complexes with low interaction between the components and a crystalline profile, nanospray-drying can generate almost completely amorphous systems with high drug-cyclodextrin interactions. Both provided slow drug release and limited drug skin permeation. A desirable follicular targeting was achieved (40%) by combining such amorphous cyclodextrin complex with the polymeric matrix by HME. In conclusion, the FIN inclusion complexes produced by HME represent promising topical formulations for the optimized alopecia treatment, targeting the drug directly at the action site. Furthermore, the developed formulation can be easily produced by a scalable industrial process. [Display omitted] • Nanospray-drying produced amorphous powder with high drug-cyclodextrin interaction. • Complexed powders produced by extrusion increased drug accumulation in the skin. • Granules with high-level drug complexation reached follicular targeting. [ABSTRACT FROM AUTHOR]

In the present study, iron oxide nanoparticles, in the form of maghemite core coated with lauric acid (ION), were synthesized and loaded with finasteride (FIN) or dutasteride (DUT) as a novel drug delivery system for the topical treatment of alopecia. Additionally, developed formulations (FIN-ION and DUT-ION) were completely elaborated with components involved in the follicle metabolism, i.e., lauric acid, which acts as a 5α-reductase inhibitor, and iron which deficiency has been related to hair loss aggravation. Stability assessment conducted over the course of 90 days showed they are highly stable, with pH 7.4, constant EE% (>99%), and practically unchanged particle size and zeta potential. Besides drug distribution, the actual number of iron oxide nanoparticles, through a newly developed method using ferromagnetic resonance, was determined in each skin layer following permeation experiments. Despite the same donor concentration of colloids, nanoparticle distribution in the skin varied according to the loaded molecule. While DUT did not interfere with the nanoparticle natural tendency to accumulate within the hair follicle shafts, FIN presence hampered nanosystem interaction with the skin. Still, both formulations provided a higher skin drug penetration, compared to each respective control solution. Additionally, iron nanocarriers present a desirable visual characteristic, as the dark color aspect might instantly help disguise scarce hair follicle areas. These findings suggest the nanoformulations are highly promising for alopecia therapies. [ABSTRACT FROM AUTHOR]