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| Title: | Inhalable microparticles containing large payload of antituberculosis |
| Authors: | Muttil, Pavan
Kaur, Jatinder
Kumar, Kaushlendra
Yadav, Awadh Bihari
Sharma, Rolee
Misra, Amit
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| Keywords: | Dry powder inhalation
Respirable microspheres
Targeting
Macrophages
Pulmonary delivery
Tuberculosis |
| Issue Date: | 2007 |
| Citation: | EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES 32 (2007) 140-150 |
| Series/Report no.: | CDRI Communication No 6857 |
| Abstract: | Microparticles containing large payloads of two anti-tuberculosis (TB) drugs were prepared and evaluated for suitability as a dry powder inhalation targeting alveolar macrophages. A solution containing one part each of isoniazid and rifabutin, plus two parts poly(lactic acid) (L-PLA) was spraydried.
Drug content and in vitro release were assayed by HPLC, and DSC was used to elucidate release behaviour. Particle size was measured by
laser scattering and aerosol characteristics by cascade impaction using a Lovelace impactor. Microparticles were administered to mice using an inhouse
inhalation apparatus or by intra-tracheal instillation. Drugs in solution were administered orally and by intra-cardiac injection. Flow cytometry
and HPLC were used to investigate the specificity and magnitude of targeting macrophages. Microparticles having drug content -50% (w/w), particle
size -5 m and satisfactory aerosol characteristics (median mass aerodynamic diameter, MMAD = 3.57 m;
geometric standard deviation, GSD = 1.41m; fine particle fraction, FPF <4.6"", = 78.91:1: 8.4%) were obtained in yields of >60%. About 70% of the
payload was released in vitro in 10 days. Microparticles targeted macrophages and not epithelial cells on inhalation. Drug concentrations in
macrophages were -20 times higher when microparticles were inhaled rather than drug solutions administered. Microparticles were thus deemed suitable for enhanced targeted drug delivery to lung macrophages. |
| URI: | http://hdl.handle.net/123456789/56 |
| Appears in Collections: | Pharmaceutics
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| amitmisra-eurjphasc-32-140.pdf | | 569Kb | Adobe PDF | View/Open |
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