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1. Encapsulation of Anti-Tuberculosis Drugs within Mesoporous Silica and Intracellular Antibacterial Activities

Author

Xin Xia, Kevin Pethe, Ryangyeo Kim, Lluis Ballell, David Barros, Jonathan Cechetto, HeeKyoung Jeon, Kideok Kim, and Alfonso E. Garcia-Bennett

Subjects
tuberculosis, mesoporous materials, solubility, intracellular, formulation, nanomedicine, Chemistry, QD1-999
Abstract

Tuberculosis is a major problem in public health. While new effective treatments to combat the disease are currently under development, they tend suffer from poor solubility often resulting in low and/or inconsistent oral bioavailability. Mesoporous materials are here investigated in an in vitro intracellular assay, for the effective delivery of compound PA-824; a poorly soluble bactericidal agent being developed against Tuberculosis (TB). Mesoporous materials enhance the solubility of PA-824; however, this is not translated into a higher antibacterial activity in TB-infected macrophages after 5 days of incubation, where similar values are obtained. The lack of improved activity may be due to insufficient release of the drug from the mesopores in the context of the cellular environment. However, these results show promising data for the use of mesoporous particles in the context of oral delivery with expected improvements in bioavailability.

Published
2014
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2. Encapsulation of Anti-Tuberculosis Drugs within Mesoporous Silica and Intracellular Antibacterial Activities

Author

Kideok Kim, Alfonso E. Garcia-Bennett, Jonathan Cechetto, Xin Xia, Ryangyeo Kim, Lluis Ballell, David Barros, Kevin Pethe, and Heekyoung Jeon

Subjects
Drug, Materials science, Tuberculosis, General Chemical Engineering, media_common.quotation_subject, formulation, Pharmacology, mesoporous materials, Article, Mycobacterium tuberculosis, lcsh:Chemistry, medicine, General Materials Science, Solubility, media_common, tuberculosis, solubility, intracellular, nanomedicine, biology, Mesoporous silica, medicine.disease, biology.organism_classification, 3. Good health, Bioavailability, lcsh:QD1-999, Antibacterial activity, Mesoporous material
Abstract

Tuberculosis is a major problem in public health. While new effective treatments to combat the disease are currently under development, they tend suffer from poor solubility often resulting in low and/or inconsistent oral bioavailability. Mesoporous materials are here investigated in an in vitro intracellular assay, for the effective delivery of compound PA-824; a poorly soluble bactericidal agent being developed against Tuberculosis (TB). Mesoporous materials enhance the solubility of PA-824; however, this is not translated into a higher antibacterial activity in TB-infected macrophages after 5 days of incubation, where similar values are obtained. The lack of improved activity may be due to insufficient release of the drug from the mesopores in the context of the cellular environment. However, these results show promising data for the use of mesoporous particles in the context of oral delivery with expected improvements in bioavailability.

Published
2014

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