Amphiphilic poly-N-vinylpyrrolidone nanoparticles as carriers for non-steroidal anti-inflammatory drugs: characterization and in vitro controlled release of indomethacin.
Novel amphiphilic poly-N-vinylpyrrolidone derivatives with different molecular weight of hydrophilic PVP fragment and one secondary di-n-alkyl terminal hydrophobic fragment of different length were synthesized to compare their inclination for formation of nano-scaled micelle-like aggregates in aqueous media with previously studied primary n-alkyl terminated poly-N-vinylpyrrolidones. The behavior of amphiphilies in water solutions was studied and critical aggregation concentration values for prepared polymer samples were determined by fluorescence spectroscopy and compared with those for primary n-alkyl derivatives. Polymeric micelle-like particles with or without encapsulated drug were prepared using dialysis or solvent evaporation techniques. Indomethacin was incorporated into hydrophobic inner core of these nanoparticles as a typical model drug. Dynamic light-scattering studies determined that the average size of particles formed was from 90 nm up to 600 nm with monodisperse size distribution and the nanoparticle size slightly increased with the amount of indomethacin encapsulated into inner core of the particles. In vitro release experiments carried out at different medium pH values using indomethacin-loaded nanoparticles exhibited slow and steady drug release into the medium.
D.I. Mendeleyev University of Chemical Technology, Moscow 125047, Russia.
A N
AN
Kuskov
A A
AA
Voskresenskaya
A V
AV
Goryachaya
M I
MI
Shtilman
D A
DA
Spandidos
A K
AK
Rizos
A M
AM
Tsatsakis
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D007213:Indomethacin / Q000737:chemistry / Q000493:pharmacokinetics*; D007700:Kinetics; D008055:Lipids / Q000737:chemistry; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D011760:Pyrrolidinones / Q000737:chemistry*; D013696:Temperature; D014867:Water / Q000737:chemistry
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D008055:Lipids; D011760:Pyrrolidinones; D014867:Water; C042670:N-vinyl-2-pyrrolidinone; D007213:Indomethacin