Desenvolvimento de formas farmacêuticas tópicas contendo extrato seco de Endopleura uchi (Uxi-amarelo) e óleo fixo de Bertholletia excelsa (Castanha- do-Brasil

Abstract

Topical drug administration is an efficient option for treating cancer, inflammatory diseases, and infections. Even though it minimizes the problems encountered in other routes, there are still extensive searches for new formulations that can improve drug bioavailability. After research in the scientific literature, Bertholletia excelsa oil demonstrated potential for use as an excipient for formulations, and Endopleura uchi extract could be a promising plant active for the development of drugs administered to the skin and mucous membranes. Thus, the objective of this study was to develop different formulations, suppositories, and nanostructured lipid carriers for topical use using Bertholletia excelsa oil and dried extract of Endopleura uchi, with analyses for quality control and process standardization. Thus, physicochemical analyses were performed on different samples of Bertholletia excelsa oil to verify quality and damage. In the case of Endopleura uchi stem bark, 3 batches found in different periods were also compared as a quality control step. The dried extracts were obtained, and phytochemical and biological activity studies were performed. From this, suppository formulations with these plant derivatives were studied in relation to appearance, pH, disintegration test, in vitro release, and antifungal activity. In another formulation, a factorial design was used as a feasibility study for nanostructured lipid carriers with a focus on improving the release of the dried extract. The results obtained for these plant raw materials demonstrated how standardized collection, storage, and processing are important. Likewise, analytical validation was able to quantify bergenin in the aqueous extract of Endopleura uchi, without interference in the chromatographic method, ensuring the reliability of the sample for use in a pharmaceutical form. Soon after, in the development of formulations, the S4 suppository obtained a good physicochemical result and inhibition of the growth of Candida spp. Furthermore, a formulation of nanostructured carriers (E3) was viable, with a particle size of 353.10 nm and antifungal capacity for Candida spp. These proposals were important for defining the next steps to produce new pharmaceutical forms for topical application using derivatives of two Amazonian plants.