Respirable rifampicin-based microspheres containing isoniazid for tuberculosis treatment
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Updated: May 26, 2026
System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis
Published on: April 5, 2017
Roberta Cassano1, Sonia Trombino, Teresa Ferrarelli
1Department of Pharmaceutical Sciences, University of Calabria, 87036 Arcavacata di Rende, Cosenza, Italy.
Abstract:
The purpose of this investigation was to develop small microspheres for delivering antimycobacterial drugs to infected host macrophages. Rifampicin-based microparticles were prepared. The drug was covalently linked to acrylic moieties to obtain a polymerizable derivative for the preparation of materials useful as drug delivery systems that then were loaded with isoniazid acting in synergy with rifampicin. Their antitubercular activity was determined in vitro. Fourier transform infrared spectroscopy confirmed hydrogel structure. Morphological analysis showed microparticles with spherical shape and homogeneous surface. In vitro release studies were performed in media simulating physiologic pH (7.4) and endosomal of alveolar macrophages pH (5.2). A similar amount of isoniazid was delivered within the first 6 h at both pHs, while a smaller amount of the drug was delivered at pH 7.4 in the last phase of the study. In vitro antitubercular activity showed a behavior comparable to that of rifampicin and isoniazid free. Bioactive swelling matrices, showing a high swelling degree into a medium miming intra alveolar environment, were obtained. They could be applied for their antitubercular activity.
Insights
Researchers developed novel microspheres for targeted delivery of antimycobacterial drugs to macrophages. These rifampicin-based microparticles loaded with isoniazid demonstrated effective in vitro antitubercular activity and controlled drug release.
Area of Science:
- Biomedical Engineering
- Materials Science
- Pharmacology
Background:
- Tuberculosis (TB) remains a significant global health challenge, necessitating innovative drug delivery systems.
- Targeting antimycobacterial drugs to infected host macrophages is crucial for effective treatment.
- Developing advanced drug delivery systems can improve therapeutic efficacy and reduce side effects.
Purpose of the Study:
- To develop novel rifampicin-based microspheres for enhanced delivery of antimycobacterial drugs to host macrophages.
- To create polymerizable drug delivery systems loaded with isoniazid for synergistic action with rifampicin.
- To evaluate the in vitro antitubercular activity and drug release profiles of the developed microspheres.
Main Methods:
- Preparation of rifampicin-based microparticles with covalently linked acrylic moieties.
- Loading of isoniazid into the microspheres for synergistic drug delivery.
- Characterization of microsphere structure and morphology using Fourier transform infrared spectroscopy and morphological analysis.
- In vitro drug release studies at physiological pH (7.4) and endosomal pH (5.2).
- In vitro assessment of antitubercular activity compared to free drugs.
Main Results:
- Successful preparation of spherical, homogeneous rifampicin-based microparticles with a hydrogel structure.
- Controlled release of isoniazid observed at both pH 7.4 and pH 5.2, with differences in the later stages.
- In vitro antitubercular activity comparable to that of free rifampicin and isoniazid.
- Obtained bioactive swelling matrices with high swelling degrees in simulated alveolar environments.
Conclusions:
- The developed rifampicin-based microspheres are effective bioactive swelling matrices for delivering antimycobacterial drugs.
- These microspheres show potential for targeted delivery to infected macrophages, offering a promising strategy for tuberculosis treatment.
- The drug delivery system exhibits controlled release and sustained antitubercular activity, warranting further investigation for clinical application.
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