Desenvolvimento, caracterização e avaliação clínica de formulações carregadas com itraconazol para o tratamento tópico da esporotricose felina.

Abstract

Sporotrichosis is a fungal disease endemic in Brazil that can affect animals and humans, presenting a risk of death in immunocompromised individuals, in addition to social withdrawal due to apparent injuries. The high number of cases has been associated with zoonotic transmission due to contact with infected cats. For an effective control of the disease it is important to treat the feline population properly. Currently, oral administration of itraconazole (ITZ) capsules is the first choice for the treatment of sporotrichosis, both in animals and in humans. However, it is an expensive and time-consuming treatment. As most animals present skin lesions with a high fungal load, a topical formulation loaded with ITZ can be an effective alternative to improve the treatment of sporotrichosis lesions. However, there is no topical formulation loaded with ITZ in the national market. Thus, the present study aimed to develop, characterize and evaluate the clinical efficacy of the developed topical formulations loaded with ITZ in the treatment of feline sporotrichosis. It was developed oily and polymeric formulations with 1% w/w ITZ. For the experimental design, was proposed a literature review and minimal solubility assay of ITZ in different excipients. Formulations were characterized by the sensorial, macro and microscopic aspects, rheological and spreadability profiles, and content of ITZ by high performance liquid chromatography (HPLC). The excipient X1 was established as the most critical for the maintenance of ITZ solubilized. For the polymeric formulation, the polymer X26 allowed the formation of a network that coexisted with polymeric micelles that keep the ITZ solubilized for more than 30 days. Both formulations presented appropriates viscosity and spreadability for the treatment of feline sporothrichosis. The clinical evaluation of the formulations was initially conducted in a pilot case of a cat with an extensive lesion, where the application of one drop per day of the topical oily formulation associated with oral ITZ provided the animal's cure; and later in a clinical study in felines, where the association of the polymeric topical formulation, with the same dosage as the oil, proved to be effective, with a faster cure and less side effects in animals.