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

Patil JS, Devi VK, Devi K, Sarasija S - Lung India (2015 Jul-Aug)

Bottom Line: 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.Therefore, the pharmacokinetic and drug disposition studies provided a sound basis for predicting the successful treatment for tuberculosis.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, VT's Shivajirao S. Jondhle College of Pharmacy, Asangoan, Maharashtra, 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.

No MeSH data available.


Related in: MedlinePlus

Scanning Electron Microphotographs. (a) Pure Rifampicin. (b) Formulation FDFL4
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Figure 4: Scanning Electron Microphotographs. (a) Pure Rifampicin. (b) Formulation FDFL4

Mentions: The surface morphology of the particles was evaluated by scanning electron microscopy (Joel 840 A, Japan). The FDFL4 was scattered individually onto a thin film of epoxy resin and coated with a platinum layer and mounted onto the hub of SEM instrument and the particles were focused at different magnifications at room temperature and photographed with direct data capture of the images onto a personal computer. The results are shown in Figure 4.


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

Patil JS, Devi VK, Devi K, Sarasija S - Lung India (2015 Jul-Aug)

Scanning Electron Microphotographs. (a) Pure Rifampicin. (b) Formulation FDFL4
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4502196&req=5

Figure 4: Scanning Electron Microphotographs. (a) Pure Rifampicin. (b) Formulation FDFL4
Mentions: The surface morphology of the particles was evaluated by scanning electron microscopy (Joel 840 A, Japan). The FDFL4 was scattered individually onto a thin film of epoxy resin and coated with a platinum layer and mounted onto the hub of SEM instrument and the particles were focused at different magnifications at room temperature and photographed with direct data capture of the images onto a personal computer. The results are shown in Figure 4.

Bottom Line: 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.Therefore, the pharmacokinetic and drug disposition studies provided a sound basis for predicting the successful treatment for tuberculosis.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, VT's Shivajirao S. Jondhle College of Pharmacy, Asangoan, Maharashtra, 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.

No MeSH data available.


Related in: MedlinePlus