Formulation and characterisation of beads prepared from natural cyclodextrins and vegetable, mineral or synthetic oils.
A continuous external shaking for 2.5 days of a mixture composed of alpha-cyclodextrin (6%), soybean oil (19.6%) and water (74.4%) resulted in a calibrated lipid carrier namely bead with a high fabrication yield. The purpose of this work was to explore the possibility to substitute alpha-cyclodextrin by other natural cyclodextrins, i.e. beta- and gamma-cyclodextrin and then soybean oil by mineral (Primol) 352 and Marcol 82) or synthetic (Silicon 200) fluid 10, 50 or 100cSt) oils. Beads can be successfully prepared using Marcol 82 with alpha-cyclodextrin and Silicon 50 or 100cSt with gamma-cyclodextrin. The area inside oil/cyclodextrin/water ternary diagram corresponding to bead occurrence was superior for the Marcol 82/alpha-cyclodextrin couple compared to that observed with soybean oil/alpha-cyclodextrin couple. Only a few ratios of Silicon 50 and 100cSt/gamma-cyclodextrin/water led to beads. The combinations which did not induce bead occurrence gave either emulsions, two non-miscible liquids or a solid mixture. Whatever the materials used, beads exhibited similarities: presence of a crystalline organisation and viscoelastic properties. Manufacturing process of paraffin- and silicon-based beads need further optimisation to increase fabrication yield and later on, to take advantages from the high stability of both oils for the formulation of drugs with beads.
Trichard
L
L
Univ Paris-Sud, CNRS UMR 8612, Physico-chimie - Pharmacotechnie - Biopharmacie, Faculté de Pharmacie, 5 rue JB Clément, Châtenay-Malabry F-92296, France.
Fattal
E
E
Le Bas
G
G
Duchêne
D
D
Grossiord
J-L
JL
Bochot
A
A
D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D004304:Dosage Forms; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D004548:Elasticity; D004655:Emulsions; D009821:Oils / Q000737:chemistry*; D010316:Particle Size; D044367:Phase Transition; D012212:Rheology; D014783:Viscosity; D047391:alpha-Cyclodextrins / Q000737:chemistry; D047392:beta-Cyclodextrins / Q000737:chemistry; D047408:gamma-Cyclodextrins / Q000737:chemistry
D004304:Dosage Forms; D004337:Drug Carriers; D004655:Emulsions; D009821:Oils; D047391:alpha-Cyclodextrins; D047392:beta-Cyclodextrins; D047408:gamma-Cyclodextrins; C031215:betadex; C023792:gamma-cyclodextrin; C032613:alpha-cyclodextrin