Marcílio S. S. Cunha-Filho

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The purpose of this research was to explore the utility of beta cyclodextrin (betaCD) and beta cyclodextrin derivatives (hydroxypropyl-beta-cyclodextrin [HPbetaCD], sulfobutylether-beta-CD [SBbetaCD], and a randomly methylated-beta-CD [RMbetaCD]) to form inclusion complexes with the antitumoral drug, beta-lapachone (betaLAP), in order to overcome the(More)
beta-Lapachone [betaLAP] is a novel antitumor drug, which was recently on clinical trials with promising preliminary results. Problems derived from its low water solubility, its instability in solution and its high therapeutic dose constitute some challenges for pharmaceutical researchers. The purpose of the present work is to enhance the limited(More)
The objective of the present study was to evaluate the compatibility of the beta-lapachone (betaLAP), an antitumoral drug in clinical phase, with pharmaceutical excipients of common use including diluents, binders, disintegrants, lubricants and solubilising agents. Differential scanning calorimetry (DSC) was used for a first screening to find small(More)
This work evaluated the potential of Pluronics (varieties F127 and P123) in combination with solubilizing agents to be used as syringeable in situ gelling depots of intratumoral β-lapachone (βLAP). Pluronic dispersions prepared at various concentrations in the absence and the presence of ethanol and randomly methylated β-cyclodextrin (RMβCD) were(More)
BACKGROUND β-lapachone (βLAP) is obtained from natural resources with promising preliminary results against the etiologic agent of Chagas disease. βLAP activity is associated with generation of free radical and inhibition of nucleic acids and protein synthesis leading an outstanding antichagasic action. Low water solubility and large therapeutic doses(More)
OBJECTIVES The purpose of this work was to study the chemical stability of the new antitumoral β-lapachone (βLAP) to determine the degradation pathway/s of the molecule and the degradation kinetics in addition to identifying several degradation products. METHOD Samples of βLAP in solution were stored under conditions of darkness and illumination at 40°C(More)
OBJECTIVES In this work, the effects of several technological factors on the stability of β-lapachone (βLAP) in solution and in the solid state were investigated. METHODS The effects of relative humidity and light on the stability of βLAP in the solid state were studied. Samples were characterized by liquid chromatography, thermal analysis, X-ray powder(More)
THE CONFORMATION OF THE TITLE COMPOUND [SYSTEMATIC NAME: N-benzyl-2-(2-nitro-imidazol-1-yl)acetamide], C(12)H(12)N(4)O(3), can be described in terms of the relative orientation of three planar fragments, the imidazol group (A), benzyl group (B), and the acetamide fragment (C), with corresponding dihedral angles: A/C = 88.17 (4), B/C = 67.12 (5) and A/B =(More)
The purpose of this research was to explore the utility of β cyclodextrin (βCD) and β cyclodextrin derivatives (hydroxypropyl-β-cyclodextrin [HPβCD], sulfobutylether-β-CD [SB\CD], and a randomly methylated-β-CD [RMβCD]) to form inclusion complexes with the antitumoral drug, β-lapachone (βLAP), in order to overcome the problem of its poor water solubility.(More)