Cited by 98Inhalation and Respiratory Drug DeliveryNanoparticle-Based Drug DeliveryAdvanced Drug Delivery Systems

A novel approach for lung delivery of rifampicin-loaded liposomes in dry powder form for the treatment of tuberculosis

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Patil, JagadevappaS, Devi, VKusum, Devi, Kshama, Sarasija, S·2015·Lung India

Abstract

BACKGROUND: Lung administration of antibiotics by nebulization is promising for improved treatment efficiency for pulmonary infections, as it increases drug concentration at sites of infection while minimizing systemic side effects. For poorly soluble molecules like rifampicin, lipid particulate system may improve lung delivery. MATERIALS AND METHODS: We investigated rifampicin-loaded freeze-dried liposomes. Various formulations were prepared with different drug lipid ratios and one formulation was optimized. Optimized colloidal liposome formulation was freeze-dried and subsequently subjected for various evaluation and characterization parameters such as in-vitro dissolution, in-vitro antitubercular activity, aerodynamic characters, surface morphology, and thermal behavior. The optimized formulation of rifampicin-loaded freeze-dried liposome and free rifampicin was subjected for the in-vivo drug disposition study in Wister rat model by intra-tracheal instillation in comparison with an oral route of administration. RESULTS: The results of pharmacokinetic study for both free drug and the formulation suggested that liposomes released the drug in a controlled manner for a longer period of time. The enhanced efficiency of drug incorporated into liposomes suggested that the delivery of encapsulated drugs to macrophages was more rapid than that of free drug. CONCLUSION: Therefore, the pharmacokinetic and drug disposition studies provided a sound basis for predicting the successful treatment for tuberculosis.

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Crossref · 10.4103/0970-2113.159559

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  • Drug release decreases with increasing concentrations of cholesterol, as confirmed using rifampicin-loaded freeze-dried liposomes.

    “In a recent investigation, Patil et al. suggested that drug release decreases with increasing concentrations of chol, as confirmed using rifampicin-loaded freeze-dried liposomes.211”
  • Rifapentine-loaded proliposomal dry powder was effective in direct delivery of the drug to the lungs and eventually had a better therapeutic effect.

    “Similarly, rifapentine-loaded proliposomal dry powder was effective in the direct delivery of the drug to the lungs and eventually had a better therapeutic effect.211”
  • The rifampicin-loaded freeze-dried liposome formulation was optimized with a drug entrapment efficiency of 79%, and a sustained release pattern could be achieved showing higher anti-TB activity than that of the pure drug.

    “This formulation was optimized with a drug entrapment efficiency of 79%, and a sustained release pattern could be achieved showing higher anti-TB activity than that of the pure drug.211”

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Authors
Patil, J., Devi, V., Devi, K., & Sarasija, S.
Affiliations
National Institute of Pharmaceutical Education and Research (IN)
Corresponding author
Patil, JagadevappaS
Venue
Lung India
Published
2015
Volume
32
Issue
4
Pages
331
ISSN
0970-2113 (ISSN-L)
OpenAlex
W2248088237
Cited by
98
References
25
Citations by year
2026: 5 · 2025: 12 · 2024: 10 · 2023: 9 · 2022: 7 · 2021: 8 · 2020: 16 · 2019: 10 · 2018: 7 · 2017: 7 · 2016: 4 · 2015: 3
FWCI
5.54
Type
journal article
Language
en
Open access
Licence
cc-by-nc-sa
Locations
  • Lung India (publishedVersion, cc-by-nc-sa)
  • PubMed Central (publishedVersion, cc-by-nc-sa)
  • PubMed (publishedVersion)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion)
Topics
  • Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
Keywords
rifampicin, liposomes, dry powder inhalation, nebulization, pulmonary drug delivery, tuberculosis treatment, poorly water-soluble drugs, pharmacokinetics, drug disposition, macrophage targeting, antitubercular activity, drug release

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