Local structure characterization and stability of amorphous systems

• Grant number: 18/11990-5
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• Effective date (Start): February 01, 2019
• Effective date (End): October 21, 2021
• Field of knowledge: Physical Sciences and Mathematics - Physics - Condensed Matter Physics
• Principal Investigator: Fabio Furlan Ferreira
• Grantee: Vinícius Danilo Nonato Bezzon
• Host Institution: Centro de Ciências Naturais e Humanas (CCNH). Universidade Federal do ABC (UFABC). Ministério da Educação (Brasil). Santo André , SP, Brazil

Abstract

In this project it is proposed the local structure analysis of amorphous solid dispersions (ASDs) and active pharmaceutical ingredients (APIs) through the X-ray total scattering and the Pair Distribution Function (PDF) method, using data obtained in conventional diffractometer with silver source (E = 17.5 keV). ASDs are systems that have been used in pharmaceutical development to enhance the bioavailability of low-solubility pharmaceuticals since they may increase the dissolution velocity and extension. The miscibility between components (in interaction) of the systems and the absence of long-range structural order increases the complexity of the characterization, and thus, more sophisticate analysis techniques are necessary to control the final formulation. Therefore, it is proposed the structural analysis of ASDs systems that have the flubendazole as model drug dispersed in hydroxypropylmethylcellulose and its derivatives (HPMCP and HPMCAS) polymer matrices. The aim is to evaluate the systems at intra and intermolecular levels, obtaining information about structural changes in amorphous phases of flubendazole obtained in different amorphization process and its interaction with the polymer matrices, relating them to the stability of the formulation. Other techniques, such as thermal analysis and vibrational spectroscopy that it is usually used in the pharmaceutical area will also be used to corroborate with the results obtained from the PDF method. In this way, this project will promote a new front of analysis in amorphous drugs in our country, developing locally cutting-edge research equated to international laboratories of excellence, in terms of technique for structural characterization of amorphous pharmaceutical materials.

Scientific publications

(6)

(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)

LOSITO, DANILO WAISMANN; DE ARAUJO, DANIELE RIBEIRO; NONATO BEZZON, VINICIUS DANILO; OSELIERO FILHO, PEDRO LEONIDAS; AFFONSO FONSECA, FERNANDO LUIZ; CHAGAS, CAMILA DOS SANTOS; BARBOSA, EMERSON; PINTO OLIVEIRA, CRISTIANO LUIS; DE ABREU FANTINI, MARCIA CARVALHO; FERREIRA, FABIO FURLAN; et al. esoporous Silica-Fe3O4 Nanoparticle Composites as Potential Drug Carrier. ACS APPLIED NANO MATERIALS, v. 4, n. 12, p. 13363-13378, DEC 24 2021. (20/13204-7, 14/50869-6, 17/17844-8, 18/11990-5, 19/12301-1)

BEZZON, VINICIUS D. N.; FERREIRA, FABIO F.; DE LIMA, JOAO C.. Local atomic structure determination of the amorphous verapamil HCl drug. Journal of Non-Crystalline Solids, v. 565, p. 10-pg., 2021-05-14. (18/11990-5)

BEZZON, VINICIUS DANILO NONATO; PINTO, ROGERIO DA SILVA; DE ARA, GABRIEL LIMA BARROS; DE LIMA, JOAO CARDOSO; FERREIRA, FABIO FURLAN. Describing the Influence of Ball-milling on the Amorphization of Flubendazole Using the PDF and RMC Methods with X-ray Powder Diffraction Data. Journal of Pharmaceutical Sciences, v. 111, n. 11, p. 10-pg., 2022-10-13. (18/11990-5, 19/04998-2)

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, MAY 1 2021. (19/04998-2, 18/11990-5)

BEZZON, VINICIUS D. N.; DE LIMA, JOAO C.; FERREIRA, FABIO F.. Combining RMC and PDF methods to characterize amorphous drug. ACTA CRYSTALLOGRAPHICA A-FOUNDATION AND ADVANCES, v. 77, p. 1-pg., 2021-08-01. (18/11990-5)

DE ASSIS, JOAO M. C.; BARBOSA, EDUARDO J.; BEZZON, VINCIUS D. N.; LOURENCO, FELIPE R.; CARVALHO, FLAVIO M. . S.; MATOS, J. R.; BOU-CHACRA, NADIA ARACI; BENMORE, CHRIS J.; BYRN, STEPHEN R.; COSTA, FANNY N.; et al. Hot-melt extrudability of amorphous solid dispersions of flubendazole-copovidone: An exploratory study of the effect of drug loading and the balance of adjuvants on extrudability and dissolution. International Journal of Pharmaceutics, v. 614, p. 10-pg., 2022-02-25. (18/11990-5, 19/04998-2)