title: Trypanocidal activity of free and carrier bound daunorubicin.
abstract: Activities of a range of macromolecular conjugates of daunorubicin against Trypanosoma brucei rhodesiense in vitro and in vivo are described and compared to those of free daunorubicin. Conjugates tested were daunorubicin attached to bovine serum albumin by (i) a labile 'glutaraldehyde' linkage (D-BSAG), and (ii) a stable succinyl linkage (D-BSAS), daunorubicin covalently linked to agarose beads (D-AG), and daunorubicin adsorbed onto polyisobutylcyanoacrylate nanoparticles (D-PICA). Trypanocidal activity in vitro was retained in all except D-BSAS, whereas in vivo only D-BSAG had any activity. The results indicate that daunorubicin must be released from the conjugate before it can exert its activity.
authors.affiliation: Tropical Diseases Chemotherapy Research Unit, Sunderland Polytechnic.
authors.forename: L
authors.initials: L
authors.lastname: Golightly
authors.forename: J E
authors.initials: JE
authors.lastname: Brown
authors.forename: J B
authors.initials: JB
authors.lastname: Mitchell
authors.forename: J R
authors.initials: JR
authors.lastname: Brown
mesh_terms: D000818:Animals; D003487:Cyanoacrylates; D003630:Daunorubicin / Q000494:pharmacology*; D004337:Drug Carriers; D004659:Enbucrilate; D051379:Mice; D011108:Polymers; D012685:Sepharose; D012710:Serum Albumin, Bovine; D014346:Trypanosoma brucei brucei / Q000187:drug effects*; D014353:Trypanosomiasis, African / Q000188:drug therapy* / Q000469:parasitology
chemical_list: D003487:Cyanoacrylates; D004337:Drug Carriers; D011108:Polymers; D012710:Serum Albumin, Bovine; D012685:Sepharose; D004659:Enbucrilate; D003630:Daunorubicin