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Screening, characterization and evaluation for novel crystal forms from antiretroviral and antineoplastic drugs

Grant number: 07/07185-5
Support Opportunities:Scholarships in Brazil - Doctorate
Effective date (Start): March 01, 2008
Effective date (End): October 31, 2010
Field of knowledge:Biological Sciences - Biophysics - Molecular Biophysics
Principal Investigator:Javier Alcides Ellena
Grantee:Felipe Terra Martins
Host Institution: Instituto de Física de São Carlos (IFSC). Universidade de São Paulo (USP). São Carlos , SP, Brazil

Abstract

This research proposal, Screening, characterization and evaluation for novel crystal forms from antiretroviral and antineoplastic drugs, is sought to synthesis of unpublished polymorphic forms from drugs that have been widely used for the antiretroviral and antineoplastic therapies, followed by characterization of its physical and chemical properties at the solid state and evaluation of the solubility and pharmaceutical dissolution. For this purpose, antiretroviral drugs belonging to the inhibitor classes targeted on reverse transcriptase, both nucleoside and nonnucleoside compounds, and aspartate HIV protease, as well as antineoplastic drugs from alkylating agents and antifolate classes will be crystallized by mean of several methods in order to obtain polymorphs different from those reported in the literature until this moment. After the crystallization step, the obtained crystalline materials will be analyzed by photonic and scanning electron microscopy, X-ray single crystal and powder diffraction, Fourier Transform infrared and Raman vibrational spectroscopy, thermogravimetry and differential scanning calorimetry. Once the novel polymorphic forms from the tested drugs have been identified, these samples and reference drugs at the crystalline forms previously described in the literature will be evaluated comparatively in solubility and dissolution experiments. (AU)

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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)
MARTINS, FELIPE T.; LEGENDRE, ALEXANDRE O.; HONORATO, SARA B.; AYALA, ALEJANDRO P.; DORIGUETTO, ANTONIO C.; ELLENA, JAVIER. Solvothermal Preparation of Drug Crystals: Didanosine. Crystal Growth & Design, v. 10, n. 4, p. 1885-1891, . (09/14705-0, 07/07185-5)
MARTINS, FELIPE T.; PAPARIDIS, NIKOLAS; DORIGUETTO, ANTONIO C.; ELLENA, JAVIER. Crystal Engineering of an Anti-HIV Drug Based on the Recognition of Assembling Molecular Frameworks. Crystal Growth & Design, v. 9, n. 12, p. 5283-5292, . (07/07185-5)
MARTINS, FELIPE T.; DORIGUETTO, ANTONIO C.; ELLENA, JAVIER. From Rational Design of Drug Crystals to Understanding of Nucleic Acid Structures: Lamivudine Duplex. Crystal Growth & Design, v. 10, n. 2, p. 676-684, . (07/07185-5)
Academic Publications
(References retrieved automatically from State of São Paulo Research Institutions)
MARTINS, Felipe Terra. Supramolecular chemistry of antiretroviral nucleoside reverse transcriptase inhibitor drugs. 2010. Doctoral Thesis - Universidade de São Paulo (USP). Instituto de Física de São Carlos (IFSC/BT) São Carlos.

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Filed patent(s) as a result of this research project

MÉTODO DE OBTENÇÃO DE NOVA FORMA CRISTALINA DE LAMIVUDINA, SEU SAL CLORIDRATO MONOIDRATADO, FORMULAÇÕES FARMACÊUTICAS E SEUS USOS PI0903664-4 - Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) ; Universidade de São Paulo (USP) . Javier Alcides Ellena ; Felipe Terra Martins ; Nikolas Paparidis - September 2009, 22

MÉTODO DE OBTENÇÃO DE UM CO-CRISTAL DE LAMIVUDINA, SEU SAL MALEATO, FORMULAÇÕES FARMACÊUTICAS E SEU USO PI0904938-0 - Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) ; Universidade de São Paulo (USP) . Javier Alcides Ellena ; Felipe Terra Martins ; Nikolas Paparidis - July 2009, 28

MÉTODO DE OBTENÇÃO DE UM COMPLEXO SUPRAMOLECULAR DE LAMIVUDINA, ESTRUTURADA DE DUPLA HÉLICE MONOMÉRICA, COMPOSIÇÕES FARMACÉUTICAS E SEU USO PI0905355-7 - Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) ; Universidade de São Paulo (USP) . Felipe Terra Martins ; Javier Alcides Ellena ; Marcio David Bocelli - December 2009, 14

MÉTODO DE OBTENÇÃO DE NOVA FORMA CRISTALINA DE LAMIVUDINA, SEU SAL CLORIDRATO, FORMULAÇÕES FARMACÊUTICAS E SEUS USOS PI0907290-0 - Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) ; Universidade de São Paulo (USP) . Javier Alcides Ellena ; Felipe Terra Martins ; Nikolas Paparidis - September 2009, 23