Banca de DEFESA: MARINA GOULART DA SILVA

Uma banca de DEFESA de DOUTORADO foi cadastrada pelo programa.
DISCENTE : MARINA GOULART DA SILVA
DATA : 16/07/2020
HORA: 13:30
LOCAL: UFSJ - CCO
TÍTULO:

NANOEMULSION CONTAINING THE SYNTHETIC COMPOUND 10- (4,5- DIXIDROTIAZOL-2-ILTIO) DECAN-1OL: DEVELOPMENT, ACTIVITY CHARACTERIZATION AND EVALUATION ANTIMALARIC IN VITRO AND IN VIVO

PALAVRAS-CHAVES:

malaria; oil-in-water (O / W) nanoemulsion; Solutol HS 15; 1,10- decanediol, 10- (4,5-dixidrothiazol-2-ylthio) decan-1ol; thiazoline.

PÁGINAS: 135
GRANDE ÁREA: Outra
ÁREA: Tecnologia e Inovação
RESUMO:

The development of resistance of Plasmodium spp. to antimalarial drugs make it difficult to treat the disease, making it necessary to search for new molecules with antimalarial activity as well as formulations that transport these drugs. The objective is to develop an oil-in-water nanoemulsion capable of incorporating 10-(4,5- dixidrothiazol-2-ylthio) decan-1ol (thiazoline), a synthetic antimalarial prototype, to treat malaria orally. The oily phase of the nanoemulsion is made up of oleic acid, butylhydroxyanisol, parabens and thiazoline, and the aqueous phase is formed by polyethylene glycol (15)-hydroxystearate (Solutol HS15) and purified water. This formulation consists of excipients that favor the bioavailability of thiazoline and its controlled and prolonged release. An analytical method was developed and validated for quantification of thiazoline. A factorial design 23 was carried out with replicates at the central point in order to assess the influence of excipients on the physical-chemical characteristics of the nanoemulsion (droplet size, PDI, zeta potential and encapsulation efficiency). The formulation, selected from the design, had a droplet size of 248.80 nm, a polydispersion index of 0.236 indicating homogeneity in droplet size, zeta potential of -38.5 mV and encapsulation efficiency of 97.17% m / m. The in vitro release assay showed the controlled release of thiazoline in acidic (pH 2.0) and neutral (pH 6.86) media, which simulate gastric and intestinal fluids, respectively. The nanoemulsion containing thiazoline remained stable for 180 days in drastic storage conditions (40 oC and 25% humidity), indicating that the formulation is stable in the various climatic conditions existing in Brazil. The nanoemulsion showed superior antimalarial activity when compared to that of free thiazoline (p <0.05) and had a selectivity index in relation to the pulmonary fibroblast (WI-26VA4) of 12.46, being selectively toxic to parasites. The in vivo antimalarial activity of the nanoemulsion containing 25 mg / kg of thiazoline showed no statistically significant difference when compared to chloroquine (p> 0.05). However, this formulation did not achieve a cure rate and had modest activity in relation to animal survival. The nanoemulsion containing thiazoline represents a strategy for the development of a new drug for the treatment of malaria, combining a new antimalarial candidate and the nanoemulsion.

MEMBROS DA BANCA:
Presidente - 050.796.656-29 - GISELE RODRIGUES DA SILVA - UFOP
Externo ao Programa - 1719911 - JULIANA TEIXEIRA DE MAGALHAES
Externo ao Programa - 1757957 - ANA JULIA PEREIRA SANTINHO GOMES
Externo à Instituição - SANDRA APARECIDA DE LIMA MOURA - UFOP
Externo à Instituição - ANDRE LUIS MORAIS RUELA - UFOP