Liposomal formulations containing sodium mercaptoundecahydrododecaborate (BSH) for boron neutron capture therapy.
Sodium mercaptoundecahydrododecaborate or BSH is a compound most widely used for boron neutron capture therapy (BNCT). Liposome formulations containing BSH, with or without steric stabilization, were prepared as potential agents for delivery of boron compounds for BNCT. Liposomes composed of DPPC/CHOL in a molar ratio 1:1 (PEG concentration: 5 mol%) were prepared having an average diameter in the range of 100-110 nm 200 mu L of liposomes (l.88 mg phospholipid/mouse and 3.5-5.8 mg BSH/kg body weight) were injected in mice via the tail vein. Both types of liposomes resulted in a significant improvement in the circulation time of BSH compared to that obtained previously after injecting free BSH. The mean percent injected BSH remaining in circulation at the end of 24 h was 19% for the PEG-liposomes compared to the corresponding value of 7% for the conventional liposomes. The mean percent uptake by the liver and spleen was not significantly different for the two types of liposomes; the blood/RES ratios were higher for the PEG-liposomes at all time points indicating that a higher fraction of injected BSH was available in circulation. The PEG-liposomes could be further explored as a means of enhance boron drug delivery to tumor cells for BNCT.
Mehta
S C
SC
Department of Pharmaceutics, College of Pharmacy, University of Georgia, Athens 30602, USA.
Lai
J C
JC
Lu
D R
DR
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D001894:Borohydrides / Q000378:metabolism / Q000493:pharmacokinetics; D016754:Boron Neutron Capture Therapy; D002784:Cholesterol / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers / Q000302:isolation & purification / Q000378:metabolism; D008081:Liposomes / Q000378:metabolism*; D008099:Liver / Q000378:metabolism; D008297:Male; D051379:Mice; D010316:Particle Size; D010743:Phospholipids / Q000378:metabolism; D011092:Polyethylene Glycols / Q000378:metabolism; D013154:Spleen / Q000378:metabolism; D013438:Sulfhydryl Compounds / Q000378:metabolism / Q000493:pharmacokinetics
D000970:Antineoplastic Agents; D001894:Borohydrides; D004337:Drug Carriers; D008081:Liposomes; D010743:Phospholipids; D013438:Sulfhydryl Compounds; C014651:mercaptoundecahydrododecaborate; D011092:Polyethylene Glycols; D002784:Cholesterol