Encapsulation of anti-tuberculosis drugs within mesoporous silica and intracellular antibacterial activities

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

doi:10.3390/nano4030813

Encapsulation of anti-tuberculosis drugs within mesoporous silica and intracellular antibacterial activities

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

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

21 Citations (Scopus)

103 Downloads (Pure)

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.

Original language	English
Pages (from-to)	813-826
Number of pages	14
Journal	Nanomaterials
Volume	4
Issue number	3
DOIs	https://doi.org/10.3390/nano4030813
Publication status	Published - Sept 2014
Externally published	Yes

Bibliographical note

Copyright the Author(s) 2014. Version archived for private and non-commercial use with the permission of the author/s and according to publisher conditions. For further rights please contact the publisher.

Keywords

tuberculosis
mesoporous materials
solubility
intracellular
formulation
nanomedicine

Access to Document

10.3390/nano4030813Licence: CC BY

Publisher version (open access)Final published version, 864 KBLicence: CC BY

Cite this

@article{93c4d9b6bccc4635af96446a46059e25,

title = "Encapsulation of anti-tuberculosis drugs within mesoporous silica and intracellular antibacterial activities",

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.",

keywords = "tuberculosis, mesoporous materials, solubility, intracellular, formulation, nanomedicine",

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

note = "Copyright the Author(s) 2014. Version archived for private and non-commercial use with the permission of the author/s and according to publisher conditions. For further rights please contact the publisher.",

year = "2014",

month = sep,

doi = "10.3390/nano4030813",

language = "English",

volume = "4",

pages = "813--826",

journal = "Nanomaterials",

issn = "2079-4991",

publisher = "MDPI AG",

number = "3",

}

TY - JOUR

T1 - Encapsulation of anti-tuberculosis drugs within mesoporous silica and intracellular antibacterial activities

AU - Xia, Xin

AU - Pethe, Kevin

AU - Kim, Ryangyeo

AU - Ballell, Lluis

AU - Barros, David

AU - Cechetto, Jonathan

AU - Jeon, HeeKyoung

AU - Kim, Kideok

AU - Garcia-Bennett, Alfonso E.

N1 - Copyright the Author(s) 2014. Version archived for private and non-commercial use with the permission of the author/s and according to publisher conditions. For further rights please contact the publisher.

PY - 2014/9

Y1 - 2014/9

N2 - 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.

AB - 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.

KW - tuberculosis

KW - mesoporous materials

KW - solubility

KW - intracellular

KW - formulation

KW - nanomedicine

UR - http://www.scopus.com/inward/record.url?scp=84936743832&partnerID=8YFLogxK

U2 - 10.3390/nano4030813

DO - 10.3390/nano4030813

M3 - Article

C2 - 28344250

SN - 2079-4991

VL - 4

SP - 813

EP - 826

JO - Nanomaterials

JF - Nanomaterials

IS - 3

ER -

Encapsulation of anti-tuberculosis drugs within mesoporous silica and intracellular antibacterial activities

Abstract

Bibliographical note

Keywords

Access to Document

Other files and links

Fingerprint

Cite this