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

Nanomaterials

Xin Xia³  Kevin Pethe²  Ryangyeo Kim²  Lluis Ballell¹  David Barros¹  Jonathan Cechetto²  HeeKyoung Jeon²  Kideok Kim² 

[1] The Diseases of the Developing World Centre, GlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain; E-Mails:;Screening Technologies and Pharmacology Group, Institute Pasteur Korea, Bundang gu, Seongnam-si, Gyeonggi-do 463-742, Korea; E-Mails:;Department of Materials and Environmental Chemistry, Arrhenius Laboratory, Stockholm University, Stockholm SE-106 91, Sweden; E-Mail:

关键词: tuberculosis;    mesoporous materials;    solubility;    intracellular;    formulation;    nanomedicine;   

DOI  :  10.3390/nano4030813

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.