PMID- 12672618
OWN - NLM
STAT- MEDLINE
DCOM- 20030916
LR  - 20190910
IS  - 0378-5173 (Print)
IS  - 0378-5173 (Linking)
VI  - 255
IP  - 1-2
DP  - 2003 Apr 14
TI  - Enhanced schistosomicidal efficacy of tartar emetic encapsulated in pegylated 
      liposomes.
PG  - 227-30
AB  - The aim of the present study was to evaluate the ability of liposomes to improve 
      the efficacy of tartar emetic (TA) against established Schistosoma mansoni 
      infection. TA was used as a schistosomicidal drug model and both conventional 
      liposomes (CL) and long-circulating pegylated liposomes (LCL) were evaluated. In 
      the first experiment, TA, either free or encapsulated within CL or LCL, was given 
      intraperitoneally (i.p.) as a single dose of 11 mg Sb/kg to mice experimentally 
      infected with S. mansoni. Only the group treated with LCL showed a significant 
      (55%) reduction in the worm burden, compared to the control groups (untreated or 
      treated with empty LCL). In the second experiment, the efficacy of TA-containing 
      LCL was evaluated at a higher dose (27 mg Sb/kg) by both subcutaneous (s.c.) and 
      i.p. routes. Reduction levels of 67 and 82% were achieved by s.c. and i.p. 
      routes, respectively. Strikingly, all mice survived to this high dose of 
      antimony. This is in contrast with free TA that was lethal in 100% of mice at the 
      same dose. The present work demonstrates that LCL reduce the acute toxicity of TA 
      and effectively deliver this drug to S. mansoni during the late stages of 
      parasite infection.
FAU - de Melo, Alan L
AU  - de Melo AL
AD  - Departamento de Parasitologia, Instituto de Ciencias Biologicas, Universidade 
      Federal de Minas Gerais, Av. Antonio Carlos 6627, Pampulha, 31270-901 Belo 
      Horizonte, MG, Brazil.
FAU - Silva-Barcellos, Neila M
AU  - Silva-Barcellos NM
FAU - Demicheli, Cynthia
AU  - Demicheli C
FAU - Frezard, Frederic
AU  - Frezard F
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Netherlands
TA  - Int J Pharm
JT  - International journal of pharmaceutics
JID - 7804127
RN  - 0 (Delayed-Action Preparations)
RN  - 0 (Liposomes)
RN  - 0 (Schistosomicides)
RN  - 3WJQ0SDW1A (Polyethylene Glycols)
RN  - DL6OZ476V3 (Antimony Potassium Tartrate)
SB  - IM
MH  - Animals
MH  - Antimony Potassium Tartrate/*administration & dosage/chemistry/therapeutic use
MH  - Delayed-Action Preparations
MH  - Injections
MH  - Injections, Intraperitoneal
MH  - Injections, Subcutaneous
MH  - Kinetics
MH  - Liposomes
MH  - Male
MH  - Mice
MH  - *Polyethylene Glycols
MH  - Schistosomiasis mansoni/*drug therapy
MH  - Schistosomicides/*administration & dosage/chemistry/therapeutic use
EDAT- 2003/04/04 05:00
MHDA- 2003/09/17 05:00
CRDT- 2003/04/04 05:00
PHST- 2003/04/04 05:00 [pubmed]
PHST- 2003/09/17 05:00 [medline]
PHST- 2003/04/04 05:00 [entrez]
AID - S037851730300125X [pii]
AID - 10.1016/s0378-5173(03)00125-x [doi]
PST - ppublish
SO  - Int J Pharm. 2003 Apr 14;255(1-2):227-30. doi: 10.1016/s0378-5173(03)00125-x.