Preparation, characterization, and biodistribution of letrozole loaded PLGA nanoparticles in Ehrlich Ascites tumor bearing mice.
Letrozole (LTZ) incorporated PLGA nanoparticles were prepared by solvent displacement technique and characterized by transmission electron microscopy, poly-dispersity index and zeta potential measurement. Radiolabeling of free LTZ and LTZ-loaded PLGA NPs was performed with technetium-99m with high labeling efficiency. The labeled complex showed good in vitro stability as verified by DTPA challenge test. The labeled complexes also showed significant in vivo stability when incubated in rat serum for 24 h. Biodistribution studies of (99m)Tc-labeled complexes were performed after intravenous administration in normal mice and Ehrlich Ascites tumor bearing mice. Compared to free LTZ, LTZ-loaded PLGA NPs exhibited significantly lower uptake by the organs of RES. The tumor concentration of LTZ-loaded PLGA NPs was 4.65 times higher than that of free LTZ at 4 h post-injection. This study indicates the capability of PLGA nanopartcles in enhancing the tumor uptake of letrozole.
Mondal
Nita
N
Division of Pharmaceutics, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India.
Halder
Kamal Krishna
KK
Kamila
Madan Mohan
MM
Debnath
Mita Chatterjee
MC
Pal
Tapan K
TK
Ghosal
Saroj K
SK
Sarkar
Bharat R
BR
Ganguly
Shantanu
S
D000818:Animals; D047072:Aromatase Inhibitors / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy*; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004355:Drug Stability; D005612:Freeze Drying; D019344:Lactic Acid; D000077289:Letrozole; D051379:Mice; D053758:Nanoparticles; D009570:Nitriles / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D010316:Particle Size; D004369:Pentetic Acid; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D013667:Technetium; D014018:Tissue Distribution; D014230:Triazoles / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use
D047072:Aromatase Inhibitors; D004337:Drug Carriers; D009570:Nitriles; D014230:Triazoles; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D013667:Technetium; D004369:Pentetic Acid; D000077289:Letrozole