title: Lectin-functionalized multiple emulsions for improved cancer therapy.
abstract: Fine-multiple emulsions bearing 6-mercaptopurine (6-MP) in internal aqueous phase were prepared by two step emulsification using sonication technique. It was coated with Concanavalin-A (Con-A) using carbodiimide method to obtain lectin-functionalized multiple emulsions. The Con-A coated multiple emulsion was characterized for antitumour activity on murine leukemia cell line L-1210 in vitro and compared with uncoated multiple emulsion and free drug. An increased uptake and cytotoxicity were observed for Con-A coated multiple emulsion in vitro. The IC50 was decreased upto 4-fold with Con-A coated emulsion. In vivo antitumour activity was seen by recording survival times of mice injected with L-1210 cells i.v. or i.p. The mean survival time was found to increase upon treatment with Con-A coated multiple emulsion. The tumour cell count in the peritoneal cavity was decreased significantly when animal was treated by i.p. route while there was no significant difference when it was treated by i.v. route. The normal peritoneal cells remained unaltered in number and blood parameters were also restored on treatment to tumour bearing mice. The formulation was found to be effective for the treatment of cancer.
authors.affiliation: National Center For Cell Science, Ganeshkhind, Pune University Campus, Maharashtra, India.
authors.forename: A J
authors.initials: AJ
authors.lastname: Khopade
authors.forename: K S
authors.initials: KS
authors.lastname: Nandakumar
authors.forename: N K
authors.initials: NK
authors.lastname: Jain
mesh_terms: D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000493:pharmacokinetics* / Q000627:therapeutic use / Q000633:toxicity; D003208:Concanavalin A; D004339:Drug Compounding; D004655:Emulsions; D005079:Excipients; D037102:Lectins; D007939:Leukemia L1210 / Q000188:drug therapy / Q000473:pathology; D015122:Mercaptopurine / Q000493:pharmacokinetics* / Q000627:therapeutic use / Q000633:toxicity; D051379:Mice; D008807:Mice, Inbred BALB C; D009368:Neoplasm Transplantation; D014407:Tumor Cells, Cultured
chemical_list: D000964:Antimetabolites, Antineoplastic; D004655:Emulsions; D005079:Excipients; D037102:Lectins; D003208:Concanavalin A; D015122:Mercaptopurine