Chloramphenicol-incorporated poly lactide-co-glycolide (PLGA) nanoparticles: formulation, characterization, technetium-99m labeling and biodistribution studies.
Chloramphenicol-loaded (CHL) poly-d,l-lactic-co-glycolic acid (PLGA) nanoparticles (NPs) were prepared by emulsification solvent evaporation technique either by using polyvinyl alcohol (PVA) as emulsion stabilizer or polysorbate-80 (PS-80) as surfactant and characterised by transmission electron microscopy, zeta-potential measurements. The NPs were radiolabeled with technetium-99m ((99m)Tc) by stannous reduction method. Labeling conditions were optimised to achieve high-labeling efficiency, in vitro and in vivo (serum) stability. The labeled complexes also showed very low transchelation as determined by DTPA challenge test. Biodistribution studies of (99m)Tc-labeled complexes were performed after intravenous administration in mice. The CHL-loaded PLGA NPs coated with PS-80 exhibited relatively high brain uptake with comparatively low accumulation in bone marrow to that of free drug and CHL-loaded PLGA NPs (PVA, used as emulsion stabilizer) at 24 h post injection time period. This indicates the usefulness of the above delivery system for prolonged use of the antibiotic.
Halder
Kamal Krishna
KK
Nuclear Medicine Division, Indian Institute of Chemical Biology, Kolkata, India.
Mandal
Bivash
B
Debnath
Mita Chatterjee
MC
Bera
Hriday
H
Ghosh
Lakshmi Kanto
LK
Gupta
Bijon Kumar
BK
D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D002614:Chelating Agents / Q000737:chemistry; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002627:Chemistry, Physical; D002701:Chloramphenicol / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D004355:Drug Stability; D004563:Electrochemistry; D006863:Hydrogen-Ion Concentration; D007275:Injections, Intravenous; D007553:Isotope Labeling; D019344:Lactic Acid; D051379:Mice; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D004369:Pentetic Acid / Q000737:chemistry; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D013667:Technetium; D017971:Tin Compounds / Q000737:chemistry; D014018:Tissue Distribution
D000900:Anti-Bacterial Agents; D002614:Chelating Agents; D017971:Tin Compounds; C023599:stannous chloride; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D002701:Chloramphenicol; D013667:Technetium; D004369:Pentetic Acid