MIL-101 (Cr) metal–organic frameworks for systemic delivery of rifampicin antibiotic to lungs

Металлоорганические каркасы MIL-101 (Cr) для системной доставки антибиотика рифампицина в легкие
Sergey M. Deyev, Daria B. Trushina, Ivan V. Zelepukin, Aziz B. Mirkasymov, Polina A. Kotelnikova, Aziz Mirkasymov, Danila Pokhorukov, Iaroslav B Belyaev, Olga Yu. Griaznova
2026-01-02

MIL-101 (Cr) metal–organic frameworksamino-modified NH2-MIL-101 (Cr)antibiotic loading and release kineticspulmonary/lung-targeted nanoparticle accumulationrifampicin delivery
Abstract Respiratory pulmonary infections are a serious threat to human health. Their therapy is primarily based on the use of antibiotics. However, non-specific accumulation and low concentration in the target tissue reduce therapeutic effectiveness, cause side effects, and promote the development of antibiotic resistance. In this study, metal–organic frameworks (MOFs) with MIL-101 (Cr) structure were used for delivery of rifampicin to the lungs. The nanoparticles (NPs) showed high antibiotic loading by mass, namely (127 ± 8)% for MIL-101 (Cr) and (82 ± 7)% for amino-modified NH 2 -MIL-101 (Cr). The kinetics of drug release had rapid and prolonged phases with up to 40% of the loaded drug released in 7 h. It induces a significant inhibition of bacterial viability at a concentration of NPs as low as 1 mg l −1 . After intravenous administration, the particles showed high tropism for lung accumulation reaching concentration of almost 300%/g of tissue, more than 10 times higher than concentrations in other tissues. This study demonstrates the effectiveness of using MIL-101 (Cr) MOFs for pulmonary drug delivery and holds significant promise for developing antibacterial therapies.
1
After intravenous administration, MIL-101 (Cr) particles accumulated preferentially in lungs, reaching nearly 300%/g of tissue—over tenfold higher than in other tissues.
2
Drug release kinetics showed rapid and prolonged phases with up to 40% of loaded rifampicin released within 7 hours.
3
MIL-101 (Cr) NPs achieved very high rifampicin loading by mass: (127 ± 8)% for MIL-101 (Cr) and (82 ± 7)% for NH2-MIL-101 (Cr).
4
MIL-101 (Cr) metal–organic framework nanoparticles were used to deliver rifampicin to the lungs.
5
Rifampicin-loaded MIL-101 (Cr) NPs significantly inhibited bacterial viability at concentrations as low as 1 mg·L⁻¹.

MIL-101 (Cr) metal–organic framework nanoparticles used for pulmonary delivery of rifampicin

Loading, release kinetics, lung-targeting biodistribution, and antibacterial efficacy of rifampicin when delivered by MIL-101 (Cr) MOF nanoparticles

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2026-01-02
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Sergey M. Deyev
Daria B. Trushina
Ivan V. Zelepukin
Aziz B. Mirkasymov
Polina A. Kotelnikova
Aziz Mirkasymov
Danila Pokhorukov
Iaroslav B Belyaev
Olga Yu. Griaznova
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