Nano-formulation for topical treatment of precancerous lesions: skin penetration, in vitro, and in vivo toxicological evaluation.

With the aim of improving the topical delivery of the antineoplastic drug 5-fluorouracil (5FU), it was loaded into ultradeformable liposomes composed of soy phosphatidylcholine and sodium cholate (UDL-5FU). The liposome populations had a mean size of 70 nm without significant changes in 56 days, and the ultradeformable formulations were up to 324-fold more elastic than conventional liposomes. The interaction between 5FU and the liposomal membrane was studied by three methods, and also release profile was obtained.

Intratracheal instillation of lipopolymeric vectors and the effect on mice lung physiology.

Background/aims: The current study compared the effects of intratracheal administration of different lipopolymeric vectors on lung function and histology in normal mice.

Methods: Forty-eight BALB/c mice were randomly divided into 8 groups (6/group). All animals received intratracheal instillation of the following suspensions: polymerized [(A) 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC):1,2-bis-(tricosa-10,12-diynoyl)-sn-glycero-3-phosphocholine (DC8,9PC):1,2-dioleoyl-3-trimethylammonium-propane (DOTAP), (B) DMPC:DC8,9PC:stearylamine (SA), (C) DMPC:DC8,9PC:myristoylcholine chloride (MCl)]; nonpolymerized [(D) DMPC:DC8,9PC:DOTAP, (E) DMPC:DC8,9PC:SA, (F) DMPC:DC8,9PC:MCl] together with plasmid DNA; vehicle (control), and pDsRed2-N1 plasmid DNA (DNA).

Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer-risperidone complexes.

Risperidone is an approved antipsychotic drug belonging to the chemical class of benzisoxazole. This drug has low solubility in aqueous medium and poor bioavailability due to extensive first-pass metabolism and high protein binding (>90%). As new strategies to improve treatments efficiency are needed, we have studied cationic G4 PAMAM dendrimers' performance to act as efficient nanocarriers for this therapeutic drug.