DEVELOPMENT OF SOLID DISPERSIONS CONTAINING ENDOPLEURA UCHI EXTRACTS FOR PHYTOPHARMACEUTICAL PURPOSES

• Grant number: 15/25128-5
• Support Opportunities: Regular Research Grants
• Start date: March 01, 2016
• End date: February 28, 2018
• Field of knowledge: Engineering - Chemical Engineering - Chemical Technology
• Principal Investigator: Luis Alexandre Pedro de Freitas
• Grantee: Luis Alexandre Pedro de Freitas
• Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil

Abstract

This project aims at preparing solid dispersions containing uxi extracts enriched in bergenin. The Endopleura uchi (Huber) Cuatrec, Humiriaceae, popularly known as uchi, uxi-yellow, uxi, uchi-Pucu, axuá, pururu, among other synonyms is a promising plant with anti-inflammatory activity. The bark extract is used for treating hypercholesterolemia, hyperglycemia, inflammatory processes, female urinary tract infections and uterine fibroids. The popular use includes its association with Amazon cat's claw (Uncaria tomentosa Will DC) as anti-inflammatory. The anti-inflammatory activity of extracts of uxi bark was investigated and revealed the antimicrobial activity of methanolic fractions of uxi against various microorganisms. Uxi dry extracts with high bergenin content were studied, resulting in good antioxidant and antimicrobial activity. The literature agrees its main marker is bergenin. The bergenin is a recognized and important bioactive found in many plants, whose structure has been elucidated and is also known as ardisic acid, B bergenite, bergenitol, cuscutin,peltoforin and vaquerin. Among the activities proven to bergenin are antiviral, antifungal, antitussive, antiplasmodial, anti-inflammatory, anti-hepatotoxic, antiarrhythmic, anti-tumor, anti-ulcerogenic, anti-diabetic and healing. The bergenin has low water solubility and is easily degraded in alkaline solution, resulting in a poor stability, dependent on storage conditions. The preparation of solid dispersions of uxi extracts enriched with bergenin can solve the problem of its low solubility making it feasible to be used as herbal medicine. Thus, this project aims to develop cutting-edge technology in the drying area, which is microencapsulation by spray drying or congealing spray, and apply it to technological development derived from the Brazilian plant Encopleura uchi (Huber) Cuatrec, Humiriaceae, with promising biological activities as recently proven by scientific studies. The uxi extracts are obtained by dynamic and turbólise maceration, aimed at maximizing bergenin extraction. The possible interactions between drug-carrier will be evaluated through solubility and dissolution tests as a form of screening of carriers and multivariate planning. Solid microparticulate Ddispersões of Endopleura uchi be prepared by the process of "spray drying" and "spray congealing" with the use of multivariate planning. Solid dispersions will be evaluated by solubility tests, dissolution and antioxidant activity; verification of the carrier-drug interaction by thermal analysis, X-ray diffraction, FTIR and SEM, as well as its stability in accordance with the standards. The best systems and process conditions are chosen with the help of optimization tools for further evaluation of in vivo activity by the legs edema method. It is important to note that one of the objectives of this project is also the training of human resources in a poor area in the country, which is the herbal technology (AU)

Scientific publications

(7)

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

PEREIRA, SIMONE VIEIRA; REIS, RAYSSA A. S. P.; GARBUIO, DANIELLE CRISTINA; PEDRO DE FREITAS, LUIS ALEXANDRE. Dynamic maceration of Matricaria chamomilla inflorescences: optimal conditions for flavonoids and antioxidant activity. REVISTA BRASILEIRA DE FARMACOGNOSIA-BRAZILIAN JOURNAL OF PHARMACOGNOSY, v. 28, n. 1, p. 111-117, JAN-FEB 2018. (15/25128-5)

TEIXEIRA, CRISTIANE C. C.; DE PAIVA JUNIOR, ELIAS; PEDRO DE FREITAS, LUIS ALEXANDRE. Fluidized Bed Hot-Melt Granulation as a Tool to Improve Curcuminoid Solubility. AAPS PHARMSCITECH, v. 19, n. 3, p. 1061-1071, APR 2018. (15/25128-5, 13/23327-5)

PEREIRA, SIMONE VIEIRA; REIS, RAYSSA A. S. P.; GARBUIO, DANIELLE CRISTINA; PEDRO DE FREITAS, LUIS ALEXANDRE. Dynamic maceration of Matricaria chamomilla inflorescences: optimal conditions for flavonoids and antioxidant activity. REVISTA BRASILEIRA DE FARMACOGNOSIA-BRAZILIAN JOURNAL OF PHARMACOGNOSY, v. 28, n. 1, p. 7-pg., 2018-01-01. (15/25128-5)

PEDRO DE FREITAS, LUIS ALEXANDRE. Pharmaceutical applications of spouted beds: A review on solid dosage forms. PARTICUOLOGY, v. 42, p. 11-pg., 2019-02-01. (15/25128-5)

FREITAS, L. V. D.; MONTES, A. C. R.; CAMPOS, E. I. A.; CONCEICAO, E. C.; TACON, L. A.; LANCHOTE, A. D.; FREITAS, L. A. P.. Rice spouted bed for manufacturing inclusion complexes of Endopleura uchi L extracts in beta-cyclodextrin. PARTICUOLOGY, v. 42, p. 8-pg., 2019-02-01. (15/25128-5)

PEDRO DE FREITAS, LUIS ALEXANDRE. Pharmaceutical applications of spouted beds: A review on solid dosage forms. PARTICUOLOGY, v. 42, n. SI, p. 126-136, FEB 2019. (15/25128-5)

FREITAS, L. V. D.; MONTES, A. C. R.; CAMPOS, E. I. A.; CONCEICAO, E. C.; TACON, L. A.; LANCHOTE, A. D.; FREITAS, L. A. P.. Rice spouted bed for manufacturing inclusion complexes of Endopleura uchi L extracts in beta-cyclodextrin. PARTICUOLOGY, v. 42, n. SI, p. 208-215, FEB 2019. (15/25128-5)