Investigation of diazepam lipospheres based on Witepsol and lecithin intended for oral or rectal delivery.
Diazepam was incorporated in lipospheres prepared by high pressure homogenization of melted Witepsol (10%) dispersed in aqueous lecithin (2.4%). Diazepam content was 0.4% and more than 98% of the dose was found to be encapsulated in the lipospheres. Although the initial mean particle size was 0.3 micron, the liposhperes agglomerated during storage and this phenomenon was not eliminated by increasing lecithin concentration to 4% or incorporation of oleic acid (0.1%) and co-surfactants, polysorbate 80 (0.5%) or poloxamer (up to 6%). The formulation was not able to mask effectively bitter taste of diazepam, even when lipids of higher melting temperature, namely glyceryl tripalmitate or stearic acid, were introduced.
Sznitowska
M
M
Department of Pharmaceutical Technology, Medical University of Gdańsk, Poland.
Janicki
S
S
Gajewska
M
M
Kulik
M
M
D000284:Administration, Oral; D000285:Administration, Rectal; D014151:Anti-Anxiety Agents / Q000008:administration & dosage / Q000737:chemistry*; D003975:Diazepam / Q000008:administration & dosage / Q000737:chemistry*; D004337:Drug Carriers; D008081:Liposomes; D010316:Particle Size; D014677:Pharmaceutical Vehicles; D010713:Phosphatidylcholines; D014280:Triglycerides
D014151:Anti-Anxiety Agents; D004337:Drug Carriers; D008081:Liposomes; D014677:Pharmaceutical Vehicles; D010713:Phosphatidylcholines; D014280:Triglycerides; C009683:witepsol; D003975:Diazepam