Anti-tuberculosis activity and drug interaction with nevirapine of inhalable lipid microspheres containing rifampicin in murine model.
Intranasal administration of lipid microspheres (LM) containing rifampicin (LM-RFP) exhibited the bacteriostatic effect against Mycobacterium tuberculosis H37Rv. The efficacies of intranasal LM-RFP in lung were markedly higher in immunodeficient BALB/c nude mice (p < 0.001), but not different in immunocompetent BALB/c mice (p = 1.000) compared to the results of oral rifampicin groups. When intranasal LM-RFP was given instead of oral rifampicin, the reductions of C(max) and AUC(0-3) of nevirapine were decreased from 32.2% to 11.9% and 30.5% to 12.4%, respectively. These results suggested that intranasal LM-RFP could improve the anti-tuberculosis activity in immunodeficient host and minimize drug interaction between rifampicin and nevirapine.
Disratthakit
Areeya
A
Research Institute of Tuberculosis, Japan Anti-tuberculosis Association, Kiyose, Tokyo, Japan.
Doi
Norio
N
Takenaga
Mitsuko
M
Ohta
Yuki
Y
D000281:Administration, Intranasal; D000818:Animals; D000904:Antibiotics, Antitubercular / Q000627:therapeutic use*; D004347:Drug Interactions; D005260:Female; D008055:Lipids; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D008863:Microspheres; D023421:Models, Animal; D019829:Nevirapine / Q000627:therapeutic use*; D012015:Reference Standards; D012293:Rifampin / Q000627:therapeutic use*; D014376:Tuberculosis / Q000188:drug therapy*
D000904:Antibiotics, Antitubercular; D008055:Lipids; D019829:Nevirapine; D012293:Rifampin