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Sci. Pharm. 2014, 82(3), 665-682; doi:10.3797/scipharm.1307-03 (registering DOI)

Preparation, In Vitro Characterization, and In Vivo Pharmacokinetic Evaluation of Respirable Porous Microparticles Containing Rifampicin

Indukaka Ipcowala College of Pharmacy, New Vallabh Vidyanagar, Dist. Anand (Gujarat) – 388121, India
A. R. College of Pharmacy and G H Patel Institute of pharmacy, Vallabh Vidyanagar, Dist. Anand (Gujarat) – 388120, India
Author to whom correspondence should be addressed.
Received: 5 July 2013 / Accepted: 23 July 2014 / Published: 23 July 2014
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This study aimed to prepare and evaluate rifampicin microparticles for the lung delivery of rifampicin as respirable powder. The microparticles were prepared using chitosan by the spray-drying method and evaluated for aerodynamic properties and pulmonary drug absorption. To control the drug release, tripoly-phosphate in different concentrations 0.6, 0.9, 1.2, and 1.5 was employed to get a sustained drug release profile. The microparticles were evaluated for drug loading, % entrapment efficiency, tapped density, morphological characteristics, and in vitro drug release studies. Aerosol properties were determined using the Andersen cascade impactor. Porous microparticles with particle sizes (d0.5) less than 10 μm were obtained. The entrapment of rifampicin in microparticles was up to 72%. In vitro drug release suggested that the crosslinked microparticles showed sustained release for more than 12 hrs. The drug release rate was found to be decreased as the TPP concentration was increased. The microparticles showed a fine particle fraction in the range of 55–63% with mass median aerodynamic diameter (MMAD) values below 3 μm. The in vivo pulmonary absorption of the chitosan microparticles suggested a sustained drug release profile up to 72 hrs with an elimination rate of 0.010 per hr. The studies revealed that the spray-dried porous microparticles have suitable properties to be used as respirable powder in rifampicin delivery to the lungs.
Keywords: Microparticles; Chitosan; Inhalation; Sustained release Microparticles; Chitosan; Inhalation; Sustained release
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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KUNDAWALA, A.; PATEL, V.; PATEL, H.; CHOUDHARY, D. Preparation, In Vitro Characterization, and In Vivo Pharmacokinetic Evaluation of Respirable Porous Microparticles Containing Rifampicin. Sci. Pharm. 2014, 82, 665-682.

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