title: Ursolic Acid Loaded PLGA Nanoparticles: in vitro and in vivo Evaluation to Explore Tumor Targeting Ability on B16F10 Melanoma Cell Lines.
abstract: Ursolic acid (UA), a pentacyclic triterpenoid extracted from plants, shows promising inhibitory effect in different tumor bearing cell lines. In the present study we fabricated UA loaded PLGA nanoparticles (UA-NPs) as the drug carrier and thoroughly evaluated in vitro and in vivo the differential tumor targeting effects of UA and UA-NPs in B16F10 melanoma cells.
  
  
  
  Ursolic acid loaded PLGA nanoparticles were prepared by emulsion solvent evaporation technique and evaluated for particle size, polydispersity, zeta potential and drug release potency. MTT assay as well as flow cytometric and confocal microscopic analyses were done in B16F10 mouse melanoma cell lines. Formulations were labeled with technetium-99m to evaluate the biodistribution and perform scintigraphic imaging studies following intravenous administration in tumor bearing mice model.
  
  
  
  Single emulsification technique produced smooth spherical nanoparticles of small size with relatively narrow size distribution (154 ± 4.56 nm). On B16F10 cell line, the formulation showed higher cytotoxicity compared to the free drug due to increased in vitro cellular uptake. The formulation was successfully radiolabeled and remained substantially (>90%) stable when incubated (37°C, 6 h) separately in normal saline or freshly collected rat serum or histidine solution. The radiolabeled UA-NPs exhibited slower blood clearance and comparatively high uptake in tumor region as evidenced by biodistribution and scintigraphic studies.
  
  
  
  The in vitro and in vivo studies have proved the tumor targeting potential of UA-NPs in B16F10 melanoma cell lines.
authors.affiliation: Infectious Diseases and Immunology Division, CSIR-Indian Institute of Chemical Biology, 4 Raja S. C. Mullick Road, Kolkata, 700032, India.
authors.forename: Rinku
authors.initials: R
authors.lastname: Baishya
authors.affiliation: Infectious Diseases and Immunology Division, CSIR-Indian Institute of Chemical Biology, 4 Raja S. C. Mullick Road, Kolkata, 700032, India.
authors.forename: Dipak K
authors.initials: DK
authors.lastname: Nayak
authors.affiliation: Department of Natural Products, National Institute of Pharmaceutical Education and Research, Kolkata, India.
authors.forename: Deepak
authors.initials: D
authors.lastname: Kumar
authors.affiliation: Regional Radiation Medicine Center, Thakurpukur Cancer Center and Welfare Home Campus, Kolkata, India.
authors.forename: Samarendu
authors.initials: S
authors.lastname: Sinha
authors.affiliation: Regional Radiation Medicine Center, Thakurpukur Cancer Center and Welfare Home Campus, Kolkata, India.
authors.forename: Amit
authors.initials: A
authors.lastname: Gupta
authors.affiliation: Regional Radiation Medicine Center, Thakurpukur Cancer Center and Welfare Home Campus, Kolkata, India.
authors.forename: Shantanu
authors.initials: S
authors.lastname: Ganguly
authors.affiliation: Infectious Diseases and Immunology Division, CSIR-Indian Institute of Chemical Biology, 4 Raja S. C. Mullick Road, Kolkata, 700032, India. mitacd@iicb.res.in.
authors.forename: Mita Chatterjee
authors.initials: MC
authors.lastname: Debnath
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry; D045744:Cell Line, Tumor; D002470:Cell Survival; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D065546:Drug Liberation; D004655:Emulsions; D019344:Lactic Acid / Q000737:chemistry*; D008546:Melanoma, Experimental / Q000188:drug therapy* / Q000473:pathology; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D019275:Radiopharmaceuticals / Q000737:chemistry; D017207:Rats, Sprague-Dawley; D013499:Surface Properties; D013667:Technetium / Q000737:chemistry; D014018:Tissue Distribution; D014315:Triterpenes / Q000008:administration & dosage* / Q000737:chemistry; D000097245:Ursolic Acid
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D004655:Emulsions; D019344:Lactic Acid; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D019275:Radiopharmaceuticals; D013667:Technetium; D014315:Triterpenes; D000097245:Ursolic Acid
keywords: B16F10 cell line; PLGA nanoparticle; biodistribution; radiolabeling; tumor; ursolic acid