Banca de DEFESA: LUANA CARVALHO DE OLIVEIRA

Uma banca de DEFESA de MESTRADO foi cadastrada pelo programa.
STUDENT : LUANA CARVALHO DE OLIVEIRA
DATE: 26/10/2020
TIME: 09:00
LOCAL: Videoconferência
TITLE:

In silico study, physicochemical and in vitro lipase inhibitory activity of α, β-amyrenone inclusion complexes with natural cyclodextrins

KEY WORDS:

Amirenone. Triterpenes. Cyclodextrins. Binary systems. Lipase.

PAGES: 76
BIG AREA: Ciências da Saúde
AREA: Farmácia
SUMMARY:

Α, β-amirenone (ABAME), a triterpene derivative, as well as other derivatives of this class, has many biological activities and, in turn, potential pharmacological applicability. However, ABAME has problems with its physical-chemical characteristics, such as low aqueous solubility, which makes it difficult to be administered orally and, consequently, its bioavailability, limiting its pharmacological use. In the pharmaceutical area, cyclodextrins (CD) are used as a strategy to increase the solubility, stability and bioavailability of drugs. The development of inclusion complexes (CI) with cyclodextrins makes it possible to overcome the limitations imposed by ABAME, thus enabling an increase in the solubility and protection of this prototype, an improvement in the dissolution profile and an increase in bioavailability, allowing the exploration of pharmacological activities. In this context, the present work aimed to develop complexes for the inclusion of this triterpene with CD and to improve biological activities. The complexes obtained were systematically characterized through molecular modeling studies, analysis by FTIR, DRX, DSC, TG and SEM. Then, in vitro tests for lipase enzyme were performed. The physico-chemical characterization combined with molecular modeling studies indicated the formation of CI with CD being able to induce changes in the physical-chemical properties of ABAME. In addition to the CI, they present results above 90% when compared to the reference standard (77% inhibition) in tests for enzyme lipase, showing superiority in inhibitory effects. Proving that the ABAME ICs are capable of potentiating the inhibitory effects of ABAME in swine pancreas enzymes. In conclusion, this study developed a new pharmaceutical ingredient with potential improvement in the physical-chemical characteristics and in the enzymatic lipo inhibitory activity, demonstrating to be a promising compound for a future formulation.

BANKING MEMBERS:
Presidente - 1789788 - ADLEY ANTONINI NEVES DE LIMA
Externo à Instituição - ADRIANO ANTUNES DE SOUZA ARAÚJO - UFS
Interno - 2275890 - MARCELO DE SOUSA DA SILVA