Temperature-Sensitive Gels for Intratumoral Delivery of β-Lapachone: Effect of Cyclodextrins and Ethanol

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...

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Main Authors: Marcilio S. S. Cunha-Filho, Carmen Alvarez-Lorenzo, Ramón Martínez-Pacheco, Mariana Landin
Format: Article
Language:English
Published: Wiley 2012-01-01
Series:The Scientific World Journal
Online Access:http://dx.doi.org/10.1100/2012/126723
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author Marcilio S. S. Cunha-Filho
Carmen Alvarez-Lorenzo
Ramón Martínez-Pacheco
Mariana Landin
author_facet Marcilio S. S. Cunha-Filho
Carmen Alvarez-Lorenzo
Ramón Martínez-Pacheco
Mariana Landin
author_sort Marcilio S. S. Cunha-Filho
collection DOAJ
description 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 characterized regarding their rheological properties, drug solubilization capacity, and in vitro release. Pluronic F127 (18–23%) formulations combined high ability to solubilize βLAP (enhancement solubility factor up to 50), adequate gel temperature range (over 25°C), and gel strength at 37°C enough to guarantee the permanence of the formulation in the administration site for a period of time. βLAP release rate was finely tuned by the concentration of the polymer and the addition of RMβCD (diffusion coefficient ranging between 9 and 69 μg·cm−2). The ethanol increases βLAP release rate but simultaneously led to weak gels. This paper shows that βLAP formulations involving temperature-reversible Pluronic gels may be suitable for intratumoral drug delivery purposes.
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institution Kabale University
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publisher Wiley
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series The Scientific World Journal
spelling doaj-art-6c8bf2642b7a48449a594c737cb925b12025-02-03T06:06:20ZengWileyThe Scientific World Journal1537-744X2012-01-01201210.1100/2012/126723126723Temperature-Sensitive Gels for Intratumoral Delivery of β-Lapachone: Effect of Cyclodextrins and EthanolMarcilio S. S. Cunha-Filho0Carmen Alvarez-Lorenzo1Ramón Martínez-Pacheco2Mariana Landin3Faculdade de Ciências da Saúde, Universidade de Brasília (UnB), Campus Universitário Darcy Ribeiro, 70910-900 Brasília-DF, BrazilDepartamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Campus Vida, Universidad de Santiago, 15782 Santiago de Compostela, SpainDepartamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Campus Vida, Universidad de Santiago, 15782 Santiago de Compostela, SpainDepartamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Campus Vida, Universidad de Santiago, 15782 Santiago de Compostela, SpainThis 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 characterized regarding their rheological properties, drug solubilization capacity, and in vitro release. Pluronic F127 (18–23%) formulations combined high ability to solubilize βLAP (enhancement solubility factor up to 50), adequate gel temperature range (over 25°C), and gel strength at 37°C enough to guarantee the permanence of the formulation in the administration site for a period of time. βLAP release rate was finely tuned by the concentration of the polymer and the addition of RMβCD (diffusion coefficient ranging between 9 and 69 μg·cm−2). The ethanol increases βLAP release rate but simultaneously led to weak gels. This paper shows that βLAP formulations involving temperature-reversible Pluronic gels may be suitable for intratumoral drug delivery purposes.http://dx.doi.org/10.1100/2012/126723
spellingShingle Marcilio S. S. Cunha-Filho
Carmen Alvarez-Lorenzo
Ramón Martínez-Pacheco
Mariana Landin
Temperature-Sensitive Gels for Intratumoral Delivery of β-Lapachone: Effect of Cyclodextrins and Ethanol
The Scientific World Journal
title Temperature-Sensitive Gels for Intratumoral Delivery of β-Lapachone: Effect of Cyclodextrins and Ethanol
title_full Temperature-Sensitive Gels for Intratumoral Delivery of β-Lapachone: Effect of Cyclodextrins and Ethanol
title_fullStr Temperature-Sensitive Gels for Intratumoral Delivery of β-Lapachone: Effect of Cyclodextrins and Ethanol
title_full_unstemmed Temperature-Sensitive Gels for Intratumoral Delivery of β-Lapachone: Effect of Cyclodextrins and Ethanol
title_short Temperature-Sensitive Gels for Intratumoral Delivery of β-Lapachone: Effect of Cyclodextrins and Ethanol
title_sort temperature sensitive gels for intratumoral delivery of β lapachone effect of cyclodextrins and ethanol
url http://dx.doi.org/10.1100/2012/126723
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AT carmenalvarezlorenzo temperaturesensitivegelsforintratumoraldeliveryofblapachoneeffectofcyclodextrinsandethanol
AT ramonmartinezpacheco temperaturesensitivegelsforintratumoraldeliveryofblapachoneeffectofcyclodextrinsandethanol
AT marianalandin temperaturesensitivegelsforintratumoraldeliveryofblapachoneeffectofcyclodextrinsandethanol