Electrospray encapsulation of hydrophilic and hydrophobic drugs in poly(L-lactic acid) nanoparticles.
An electrospray method is developed for preparation of beclomethasone-dipropionate- and salbutamol-sulfate-loaded biodegradable poly(L-lactic acid) nanoparticles. Different set-up parameters for electrospraying are examined on particle size, and preparation conditions are optimized for producing spherical-drug-loaded nanoscale particles by controllable processing parameters. Polylactide (PLA)-drug nanoparticles with average diameters of around 200 nm are achieved in a stable cone-jet mode with a flow rate of 4 microL min(-1), polymer concentration of 1%, and ammonium hydroxide content of 0.05%. Morphology and size of the drug-polymer nanoparticles are analyzed by scanning electron microscopy and transmission electron microscopy. Changes in the crystallinity of the PLA polymer and the model drugs are detected by X-ray powder diffraction, and the absence of molecular interactions are confirmed by thermal analyses. The results indicate clearly that electrospraying is a potential method for producing polymeric nanoparticles and for encapsulating both hydrophilic and hydrophobic drugs efficiently into the nanoparticles.
Valo
Hanna
H
Division of Pharmaceutical Technology, FIN-00014, University of Helsinki, Finland. hanna.valo@helsinki.fi
Peltonen
Leena
L
Vehviläinen
Satu
S
Karjalainen
Milja
M
Kostiainen
Risto
R
Laaksonen
Timo
T
Hirvonen
Jouni
J
D000420:Albuterol / Q000737:chemistry; D001507:Beclomethasone / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D003460:Crystallization; D004563:Electrochemistry / Q000379:methods*; D005079:Excipients / Q000737:chemistry; D057927:Hydrophobic and Hydrophilic Interactions; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D011091:Polyesters / Q000737:chemistry*; D012997:Solvents / Q000737:chemistry; D044366:Transition Temperature; D014961:X-Ray Diffraction
D005079:Excipients; D004364:Pharmaceutical Preparations; D011091:Polyesters; D012997:Solvents; C033616:poly(lactide); D001507:Beclomethasone; D000420:Albuterol