Advanced search
Start date

Nanocrystalline and amorphous solid dispersions formulations for improvement of antitumor therapies

Grant number: 19/04998-2
Support type:Regular Research Grants
Duration: November 01, 2020 - October 31, 2022
Field of knowledge:Health Sciences - Pharmacy - Pharmaceutical Technology
Principal researcher:Gabriel Lima Barros de Araujo
Grantee:Gabriel Lima Barros de Araujo
Home Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil


High dosages, unspecific targeting, clinical variability, high cost of formulations, poor water solubility, toxicity of cosolvents are recurrent problems in the development of antitumor drug therapies. Nanocrystal and Amorphous solid dispersions (ASD) are outstanding solid-state technologies suitable to overcome those problems helping to accelerate preclinical and clinical development and improve the rate of success. In this project, nanocrystals and amorphous solid dispersions of the antitumor drugs will be developed aiming at the development of better anticancer formulations with improved pharmaceutical properties. Flubendazole and niclosamide are well known antihelmintic drugs with very limited bioavailability that have been shown to pursue promising activity against a several of cancer models. Due to their poor solubility there are the urgent need for formulations that can enable administration and target delivery. Brilliant Blue G is a dye has been recently demonstrated to inhibit metastasis dissemination of neuroblastoma cells; however, the need of high dosage and it is association with undesirable and unspecific tissue targeting can compromise its use. Tyrosine Kinase Inhibitors (TKIs) are a new class of site-specific antitumor drugs that are revolutionizing the oral treatment of cancer. Marketed formulations of TKIs, however, presents clinical variability, high doses and pharmacokinetic variation due to their poor water solubility. New approaches to accelerate the development of new nanocrystal and ASD formulations such as advanced studies in solid state chemistry, thermal analysis, High-Energy X-ray Diffraction and Pair Distribution Function (PDF) will be explored to achieve efficient and stable formulations. A longer-range goal of this work is to contribute to the advancement of the use of nanocrystal and amorphous formulations in cancer therapy. The best formulations will be tested by using in silico, in vitro and in vivo models to demonstrate the proof of concept. (AU)

Articles published in Agência FAPESP Newsletter about the research grant:
Articles published in other media outlets (0 total):
More itemsLess items

Scientific publications
(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)
BEZZON, VINICIUS D. N.; FERREIRA, FABIO F.; SMITH, PAMELA; BENMORE, CHRIS J.; BYRN, STEPHEN R.; DE ARAUJO, GABRIEL L. B.. Amorphous dispersions of flubendazole in hydroxypropyl methylcellulose: Formulation stability assisted by pair distribution function analysis. International Journal of Pharmaceutics, v. 600, . (19/04998-2, 18/11990-5)

Please report errors in scientific publications list by writing to: