Merck
  • Home
  • Search Results
  • Microparticles of rifampicin: comparison of pulmonary route with oral route for drug uptake by alveolar macrophages, phagocytosis activity and toxicity study in albino rats.

Microparticles of rifampicin: comparison of pulmonary route with oral route for drug uptake by alveolar macrophages, phagocytosis activity and toxicity study in albino rats.

Drug delivery (2013-11-13)
Rajesh Parikh, Leena Patel, Sonali Dalwadi
ABSTRACT

Tuberculosis (TB) is a chronic infectious disease with increasing incidence of drug resistance. Oral treatment for TB and multidrug resistance (MDR)-TB can have serious side effects. The causative agent of TB, Mycobacterium tuberculosis, resides in alveolar macrophages (AM). Pulmonary administration of anti-TB drugs can help in delivery of high concentration to AM. The ability of AM to phagocytose can also be utilized to generate mycobactericidal nitric oxide (NO) to improve efficacy of anti-TB drugs. To compare the uptake of rifampicin (RIF) by AM post oral and pulmonary administration of RIF microparticles (RM) and to compare hepatotoxicity and phagocytosis activity. RM were produced by spray drying process. RM were administered to rats through oral as well as intratracheal route. The uptake of RIF by AM and liver was measured. NO was measured in bronchoalveolar lavage (BAL) fluid. SGOT and SGPT levels were measured in serum. Significantly higher (p < 0.05) concentration of RIF was found in AM post intratracheal administration. NO production was also significantly higher but less than toxic level. SGOT and SGPT levels as well as uptake of RIF by liver were indicative of no hepatotoxicity post intratracheal administration. Phagocytosis of RM post intratracheal administration leads to significantly higher drug level in AM as well as production of significantly higher levels of NO. The administration of RM as dry powder inhalation (DPI) formulation may reduce treatment time of TB and chances of drug resistance TB.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Citric acid, 99%
Sigma-Aldrich
Sodium DL-lactate solution, synthetic, syrup, BioXtra, suitable for mouse embryo cell culture, 60 % (w/w)
Sigma-Aldrich
Citric acid, anhydrous, suitable for cell culture, suitable for plant cell culture
Sigma-Aldrich
Trypan Blue solution, 0.4%, liquid, sterile-filtered, suitable for cell culture
Sigma-Aldrich
Phosphoric acid, BioReagent, suitable for insect cell culture, 85%
Sigma-Aldrich
Calcium chloride, anhydrous, BioReagent, suitable for insect cell culture, suitable for plant cell culture, ≥96.0%
Sigma-Aldrich
Sodium DL-lactate solution, syrup, BioReagent, 60 % (w/w), synthetic, suitable for cell culture
Sigma-Aldrich
Sodium DL-lactate solution, syrup, 60 % (w/w), synthetic
Sigma-Aldrich
Calcium chloride, meets USP testing specifications
Sigma-Aldrich
Calcium chloride, AnhydroBeads, −10 mesh, ≥99.99% trace metals basis
Sigma-Aldrich
Phosphoric acid, ≥85 wt. % in H2O, ≥99.999% trace metals basis
Sigma-Aldrich
Phosphoric acid, 85 wt. % in H2O, 99.99% trace metals basis
Sigma-Aldrich
Phosphoric acid, crystalline, ≥99.999% trace metals basis
Sigma-Aldrich
Citric acid, ≥99.5%, FCC, FG
Sigma-Aldrich
Dichloromethane, anhydrous, ≥99.8%, contains 40-150 ppm amylene as stabilizer
Sigma-Aldrich
Citric acid, ACS reagent, ≥99.5%
Sigma-Aldrich
Calcium chloride, anhydrous, powder, 99.99% trace metals basis
Sigma-Aldrich
Calcium chloride, AnhydroBeads, −10 mesh, ≥99.9% trace metals basis
Supelco
Dichloromethane, Selectophore, ≥99.5%
Sigma-Aldrich
Phosphoric acid, BioUltra, ≥85% (T)
Sigma-Aldrich
Sodium DL-lactate, ReagentPlus®, ≥99.0% (NT)
Sigma-Aldrich
Citric acid, BioUltra, anhydrous, ≥99.5% (T)
Supelco
Dichloromethane, analytical standard
Sigma-Aldrich
Calcium chloride solution, BioUltra, for molecular biology, ~1 M in H2O
Sigma-Aldrich
Trypan Blue solution, 0.4%, for microscopy
Millipore
Dichloromethane, suitable for HPLC, ≥99.8% (GC)
Supelco
Methanol solution, NMR reference standard, 4% in methanol-d4 (99.8 atom % D), NMR tube size 5 mm × 8 in.
Sigma-Aldrich
Methanol solution, NMR reference standard, 4% in methanol-d4 (99.8 atom % D), NMR tube size 3 mm × 8 in.
Citric acid, anhydrous, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
Phosphoric acid-16O4 solution, 70 wt. % in D2O, 99.9 atom % 16O