NDLI: Slow Release Formulations of Inhaled Rifampin

Content Provider	Springer Nature Link
Author	Coowanitwong, Intira Arya, Vikram Kulvanich, Poj Hochhaus, Günther
Copyright Year	2008
Abstract	Rifampin microspheres were prepared by spray drying using either polylactic acid (PLA) or poly(lactic-co-glycolic acid) (PLGA) polymers in different drug to polymer ratios (90:10 to 5:95, w/w). The in-vitro release characteristics, particle-size distribution, and cytotoxicity (in an alveolar macrophage cell line) and pharmacokinetics in rats after pulmonary instillation were evaluated. Increasing the polymer content from 10% to 95% slowed down the in vitro drug release with PLGA particles showing a steeper change with increasing polymer content (100% to 20% drug release over 6 h) than PLA particles (88% to 42% drug release over 6 h). PLA microsphere formulations revealed lack of cytotoxicity and a mass median aerodynamic diameter (MMDA) of 2.22–2.86 μm, while PLGA particles were larger (MMDA of 4.67–5.11 μm). Pharmacokinetics differed among the formulations with the 10% PLA formulation showing a distinct sustained release (t $_{max}$ of 2 h vs 0.5 h of free drug) and a systemic bioavailability similar to that of free drug. Formulations with high polymer content showed a lower relative bioavailability (30%). This suggested that an optimal release rate existed for which a distinct amount of drug was delivered over an extended period of time.
Starting Page	342
Ending Page	348
Page Count	7
File Format	PDF
ISSN	12341234
Journal	The AAPS Journal
Volume Number	10
Issue Number	2
e-ISSN	15507416
Language	English
Publisher	Springer US
Publisher Date	2008-06-27
Publisher Institution	American Association of Pharmaceutical Scientists
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	cytotoxicity inhalation microspheres pharmacokinetics rifampin sustained release Biotechnology Pharmacology/Toxicology Pharmacy
Content Type	Text
Resource Type	Article

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