RESUMEN
Cutaneous leishmaniasis (CL) is a vector-borne disease characterized by skin lesions that can evolve into high-magnitude ulcerated lesions. Thus, this study aimed to develop an innovative nanoemulsion (NE) with clove oil, Poloxamer® 407, and multiple drugs, such as amphotericin B (AmB) and paromomycin (PM), for use in the topical treatment of CL. METHODS: Droplet size, morphology, drug content, stability, in vitro release profile, in vitro cytotoxicity on RAW 264.7 macrophages, and antileishmanial activity using axenic amastigotes of Leishmania amazonensis were assessed for NEs. RESULTS: After optimizing the formulation parameters, such as the concentration of clove oil and drugs, using an experimental design, it was possible to obtain a NE with an average droplet size of 40 nm and a polydispersion index of 0.3, and these parameters were maintained throughout the 365 days. Furthermore, the NE showed stability of AmB and PM content for 180 days under refrigeration (4 °C), presented a pH compatible with the skin, and released modified AmB and PM. NE showed the same toxicity as free AmB and higher toxicity than free PM against RAW 264.7 macrophages. The same activity as free AmB, and higher activity than free PM against amastigotes L. amazonensis. CONCLUSION: It is possible to develop a NE for the treatment of CL; however, complementary studies regarding the antileishmanial activity of NE should be carried out.
Asunto(s)
Anfotericina B , Antiprotozoarios , Emulsiones , Leishmaniasis Cutánea , Paromomicina , Paromomicina/farmacología , Paromomicina/administración & dosificación , Anfotericina B/farmacología , Anfotericina B/administración & dosificación , Leishmaniasis Cutánea/tratamiento farmacológico , Leishmaniasis Cutánea/parasitología , Animales , Ratones , Antiprotozoarios/farmacología , Antiprotozoarios/administración & dosificación , Antiprotozoarios/química , Células RAW 264.7 , Macrófagos/efectos de los fármacos , Macrófagos/parasitología , Leishmania mexicana/efectos de los fármacos , Aceite de Clavo/farmacología , Aceite de Clavo/química , Poloxámero/química , Estabilidad de Medicamentos , Nanopartículas/químicaRESUMEN
Fruits such as bacaba (Oenocarpus bacaba Mart), pracaxi (Pentaclethra macroloba Kuntze) and uxi (Endopleura uchi (Huber) Cuatrec), from the Amazon rainforest, are potentially interesting for studies of natural products. The current article aims at mapping and characterizing studies on the bacaba, pracaxi and uxi species. This review reports the main bioactive compounds identified in these species and discusses their therapeutic potential. Searches were performed in MEDLINE (Via Pubmed) and Web of Science. Thirty-one studies that described or evaluated the development of formulations aimed at the therapeutic use of the species were included. The findings suggest that species have the potential for the development of pharmaceutical formulations due to their therapeutic properties. However, further studies are required to assess safety and efficacy of these products. Therefore, it is suggested that new research studies propose strategies so that technological development is based on awareness and preservation of the biome.