PMID- 16199372 OWN - NLM STAT- MEDLINE DCOM- 20051031 LR - 20191109 IS - 1061-186X (Print) IS - 1026-7158 (Linking) VI - 13 IP - 5 DP - 2005 Jun TI - Targeting of mannosylated liposome incorporated benzyl derivative of Penicillium nigricans derived compound MT81 to reticuloendothelial systems for the treatment of visceral leishmaniasis. PG - 285-93 AB - The antileishmanial property of a Benzyl derivative of a new antibiotic MT81 (Bz2MT81), isolated and purified from a fungal strain of Penicillium nigricans NRRL 917 was tested in free, liposome intercalated and mannose coated liposome intercalated forms in vivo against visceral leishmaniasis in hamsters. Mannose grafted liposome intercalated Bz2MT81 eliminated intracellular amastigotes of Leishmania donovani within splenic macrophages more efficiently than the liposome intercalated Bz2MT81 or free Bz2MT81. At a dose equivalent to 7.5 microg/Kg body weight when injected subcutaneously (s.c) in mannose grafted liposome intercalated form for 15 days in an interval of three days, the splenic parasitic load decreased to the extent of 79.1% of the total parasite present in infected control animals. Whereas, an identical amount (7.5 mug/Kg body weight) of Bz2MT81 in free or liposome intercalated form was found less effective in controlling the parasite in spleen (in free Bz2MT81 form, suppression of parasitic load is 49.8% and in liposome intercalated form, it is 55.1%). Both mannosylated liposomes and Bz2MT81 were noted non-toxic to the host peritoneal macrophages. Histological examinations of spleen and liver, kidney function tests (SGPT, alkaline phosphatase, creatinine and urea in blood plasma) showed that the toxicity of Bz2MT81 was reduced up to normal level when mannose grafted liposomal Bz2MT81 were administered. FAU - Mitra, Maitreyi AU - Mitra M AD - Jadavpur University, Department of Pharmaceutical Technology, Kolkata, 700 032, India. FAU - Mandal, Ardhendu K AU - Mandal AK FAU - Chatterjee, Tapan Kumar AU - Chatterjee TK FAU - Das, Nirmalendu AU - Das N LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - England TA - J Drug Target JT - Journal of drug targeting JID - 9312476 RN - 0 (Anthraquinones) RN - 0 (Antiprotozoal Agents) RN - 0 (Benzyl Compounds) RN - 0 (Drug Carriers) RN - 0 (Excipients) RN - 0 (Fluoresceins) RN - 0 (Fluorescent Dyes) RN - 0 (Intercalating Agents) RN - 0 (Liposomes) RN - 11028-71-0 (Concanavalin A) RN - 3301-79-9 (6-carboxyfluorescein) RN - 82197-56-6 (MT81 mycotoxin) RN - 8T3HQG2ZC4 (Trinitrobenzenesulfonic Acid) RN - I2ZWO3LS3M (Trypan Blue) RN - PHA4727WTP (Mannose) SB - IM MH - Animals MH - Anthraquinones/*administration & dosage/pharmacokinetics/*therapeutic use MH - Antiprotozoal Agents/*administration & dosage/pharmacokinetics/*therapeutic use MH - Benzyl Compounds/*administration & dosage/pharmacokinetics/therapeutic use MH - Concanavalin A/pharmacology MH - Cricetinae MH - Drug Carriers MH - *Drug Delivery Systems MH - Excipients MH - Fluoresceins MH - Fluorescent Dyes MH - Intercalating Agents/pharmacology MH - Kidney Function Tests MH - Leishmaniasis, Visceral/*drug therapy/parasitology MH - Liposomes/*chemistry MH - Liver Function Tests MH - Macrophages/drug effects MH - Mannose/*chemistry MH - Mesocricetus MH - Mice MH - Mice, Inbred BALB C MH - Mononuclear Phagocyte System/*drug effects MH - Particle Size MH - Penicillium/*chemistry MH - Trinitrobenzenesulfonic Acid/pharmacology MH - Trypan Blue EDAT- 2005/10/04 09:00 MHDA- 2005/11/01 09:00 CRDT- 2005/10/04 09:00 PHST- 2005/10/04 09:00 [pubmed] PHST- 2005/11/01 09:00 [medline] PHST- 2005/10/04 09:00 [entrez] AID - X66440285953370U [pii] AID - 10.1080/10611860500233306 [doi] PST - ppublish SO - J Drug Target. 2005 Jun;13(5):285-93. doi: 10.1080/10611860500233306.