RESUMO
The use of lipids in the composition of polymeric-based films for topical administration of bioactive ingredients is a recent research topic; while few products are commercially available, films containing lipids represent a strategic area for the development of new products. Some lipids are usually used in polymeric-based film formulations due to their plasticizing action, with a view to improving the mechanical properties of these films. On the other hand, many lipids have healing, antimicrobial, anti-inflammatory, anti-aging properties, among others, that make them even more interesting for application in the medical-pharmaceutical field. This manuscript discusses the production methods of these films both on a laboratory and at industrial scales, the properties of the developed biopolymers, and their advantages for the development of dermatologic and cosmetic products.
RESUMO
Isopentyl caffeate (ICaf) is a bioactive ester widely distributed in nature. Our patented work has shown promising results of this molecule against Leishmania. However, ICaf shows poor solubility, which limits its usage in clinical settings. In this work, we have proposed the development of an inclusion complex of ICaf in ß-cyclodextrin (ß-CD), with the aim to improve the drug solubility, and thus, its bioavailability. The inclusion complex (ICaf:ß-CD) was developed applying three distinct methods, i.e., physical mixture (PM), kneading (KN) or co-evaporation (CO) in different molar proportions (0.25:1, 1:1 and 2:1). Characterization of the complexes was carried out by thermal analysis, Fourier-transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM) and molecular docking. The ICaf:ß-CD complex in a molar ratio of 1:1 obtained by CO showed the best complexation and, therefore, was selected for further analysis. Solubility assay showed a marked improvement in the ICaf:ß-CD (CO, 1:1) solubility profile when compared to the pure ICaf compound. Cell proliferation assay using ICaf:ß-CD complex showed an IC50 of 3.8 and 2.7 µg/mL against L. amazonesis and L. chagasi promastigotes, respectively. These results demonstrate the great potential of the inclusion complex to improve the treatment options for visceral and cutaneous leishmaniases.
