Liposomes containing boronophenylalanine for boron neutron capture therapy.
In the present work, liposomes loaded with Boronophenylalanine (BPA), with or without stabilization, were formulated for the application in boron neutron capture therapy. BPA was encapsulated into liposomes as a complex with fructose, but also as a free drug in two different pH buffers. The influence of critical variables (cholesterol content, drug:lipid molar ratio, osmotic stress of liposomes containing hyperosmotic drug solution) on liposome morphology and drug content was evaluated. The drug content and dissolution profile of different BPA loaded liposomes were also studied. The physical stability of liposomes in terms of changes in the size distribution in different osmotic pressure buffers and the chemical oxidation of phospholipids during storing conditions were investigated. The encapsulation efficiencies of all formulations were always satisfactory, being between 20-48%; even when the liposomes were exposed to high osmotic stress, the particle size was below 200 nm. The BPA-fructose complex loaded liposomes showed a slower drug release profile.
Perugini
P
P
Department of Pharmaceutical Chemistry, University of Pavia, Italy.
Pavanetto
F
F
D001896:Boron Compounds / Q000008:administration & dosage* / Q000737:chemistry*; D016754:Boron Neutron Capture Therapy; D004337:Drug Carriers; D004355:Drug Stability; D005614:Freeze Fracturing; D006863:Hydrogen-Ion Concentration; D008055:Lipids / Q000032:analysis; D008081:Liposomes; D008854:Microscopy, Electron; D009997:Osmotic Pressure; D010316:Particle Size; D010649:Phenylalanine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D011838:Radiation-Sensitizing Agents / Q000008:administration & dosage* / Q000737:chemistry*; D013056:Spectrophotometry, Ultraviolet
D001896:Boron Compounds; D004337:Drug Carriers; D008055:Lipids; D008081:Liposomes; D011838:Radiation-Sensitizing Agents; D010649:Phenylalanine; C033685:4-boronophenylalanine