Banca de DEFESA: SIMONE PAES BASTOS FRANCO

OBTAINING PHARMACEUTICAL GRANULES CONTAINING ETHANOLIC EXTRACT FROM GENIPA americana L. LEAVES, 

PHYTOCHEMICAL CHARACTERIZATION AND ANTIOXIDANT ACTIVITY

Genipin, iridoids, pharmaceutical granules.

Genipa americana L. is popularly known as jenipapo and has phytotherapeutic potential with various pharmacological activities. Granules are a simple and useful pharmaceutical form for obtaining herbal medicines in solid form and have the advantage of protecting the herbal extract from bioactive compounds. The aim of this study was therefore to carry out characterisation studies on Genipa americana extract and its granules in order to assess their phytochemical, physicochemical and thermal properties. Firstly, the plant drug was characterised using physicochemical tests such as determination of the swelling index, ash, foreign matter and foam, granulometry and humidity. The crude extract of Genipa americana leaves was obtained by maceration with ethanol. A total of four granules were obtained using the wet granulation process. Phytochemical characterisation was carried out using total phenol and total flavonoid content and DPPH, FRAP and MDA assays. Physico-chemical characterisation was carried out using SEM, FTIR, UV-Vis, dissolution profile and UFCL-DAD/UV analysis. Thermal characterisation was carried out using the TG technique. A cytotoxicity test was also carried out on the extract using cell viability. The characterisation of the plant drug was as recommended by the Brazilian Pharmacopoeia, with humidity of 10.31%, total ash of 5.93%, absence of foreign matter, swelling index of 2.5 mL/g and foam index of less than 100. The crude extract of Genipa americana and its granules showed the presence of iridoids (genipin and geniposides), flavonoids and phenolic compounds and genipin derivatives after the hydrolysis experiment using HPLC-DAD/UV. The DPPH assay showed antioxidant activity with an IC50 of 207.07 μg/mL for the Genipa americana extract and 198.34 to 298.71 μg/mL for the Genipa americana granules. The FRAP test showed a good ability to reduce the Iron III-TPZ complex to Iron II-TPZ with values between 1092-1532 μM ferrous sulphate/g, also explained by the presence of phenolic compounds and flavonoids. The intrinsic maloaldehyde (MDA) test showed acceptable levels, similar to those in scientific literature. SEM analysis showed granules with a morphology and particle size that characterise them as microparticles. FTIR analysis showed similarity between the identification bands of the crude Genipa americana granules and the pharmaceutical excipients. The dissolution profiles of the Genipa americana granules showed characteristics of highly water-soluble pharmaceutical compositions with total release of the genipin marker between 30 and 60 minutes. The moisture content of the Genipa americana granules ranged from 4.27 to 11.6 per cent according to thermogravimetric analysis. Finally, the crude extract of G. americana leaves showed low toxicity. The granules indicated greater protection and stability for the Genipa americana extract in these pharmaceutical formulations. The wet granulation process proved to be suitable and low-cost for Genipa americana extract. The moisture content of the granules can cause variability in the genipin content, which should be stored in a suitable environment and packaging.