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Characterization of beta-lapachone and methylated beta-cyclodextrin solid-state systems.
AAPS PharmSciTech. 2007 Jul 27; 8(3):E60.AP

Abstract

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 problem of its poor water solubility. RMbetaCD presented the highest efficiency for betaLAP solubilization and was selected to develop solid-state binary systems. Differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD), Fourier transform infrared (FTIR) and optical and scanning electron microscopy results suggest the formation of inclusion complexes by both freeze-drying and kneading techniques with a dramatic improvement in drug dissolution efficiency at 20-minute dissolution efficiency (DE(20-minute) 67.15% and 88.22%, respectively) against the drug (DE(20-minute) 27.11%) or the betaCD/drug physical mixture (DE(20-minute) 27.22%). However, the kneading method gives a highly crystalline material that together with the adequate drug dissolution profile make it the best procedure in obtaining inclusion complexes of RMbetaCD/betaLAP convenient for different applications of betaLAP.

Authors+Show Affiliations

Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Santiago de Compostela, Santiago de Compostela, 15782, Spain.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17915810

Citation

Cunha-Filho, Marcílio S S., et al. "Characterization of Beta-lapachone and Methylated Beta-cyclodextrin Solid-state Systems." AAPS PharmSciTech, vol. 8, no. 3, 2007, pp. E60.
Cunha-Filho MS, Dacunha-Marinho B, Torres-Labandeira JJ, et al. Characterization of beta-lapachone and methylated beta-cyclodextrin solid-state systems. AAPS PharmSciTech. 2007;8(3):E60.
Cunha-Filho, M. S., Dacunha-Marinho, B., Torres-Labandeira, J. J., Martínez-Pacheco, R., & Landín, M. (2007). Characterization of beta-lapachone and methylated beta-cyclodextrin solid-state systems. AAPS PharmSciTech, 8(3), E60.
Cunha-Filho MS, et al. Characterization of Beta-lapachone and Methylated Beta-cyclodextrin Solid-state Systems. AAPS PharmSciTech. 2007 Jul 27;8(3):E60. PubMed PMID: 17915810.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Characterization of beta-lapachone and methylated beta-cyclodextrin solid-state systems. AU - Cunha-Filho,Marcílio S S, AU - Dacunha-Marinho,Bruno, AU - Torres-Labandeira,Juan J, AU - Martínez-Pacheco,Ramón, AU - Landín,Mariana, Y1 - 2007/07/27/ PY - 2007/10/6/pubmed PY - 2007/10/18/medline PY - 2007/10/6/entrez SP - E60 EP - E60 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 8 IS - 3 N2 - 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 problem of its poor water solubility. RMbetaCD presented the highest efficiency for betaLAP solubilization and was selected to develop solid-state binary systems. Differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD), Fourier transform infrared (FTIR) and optical and scanning electron microscopy results suggest the formation of inclusion complexes by both freeze-drying and kneading techniques with a dramatic improvement in drug dissolution efficiency at 20-minute dissolution efficiency (DE(20-minute) 67.15% and 88.22%, respectively) against the drug (DE(20-minute) 27.11%) or the betaCD/drug physical mixture (DE(20-minute) 27.22%). However, the kneading method gives a highly crystalline material that together with the adequate drug dissolution profile make it the best procedure in obtaining inclusion complexes of RMbetaCD/betaLAP convenient for different applications of betaLAP. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/17915810/Characterization_of_beta_lapachone_and_methylated_beta_cyclodextrin_solid_state_systems_ L2 - https://antibodies.cancer.gov/detail/CPTC-CTLA4-1 DB - PRIME DP - Unbound Medicine ER -