Combined poly(isobutylcyanoacrylate) and cyclodextrins nanoparticles for enhancing the encapsulation of lipophilic drugs.
OBJECTIVE
The aim of this study was to prepare and characterize nanoparticulate systems constituted of poly(isobutylcyanoacrylate) and cyclodextrins and intended for increasing the loading of the particles with lipophilic substances. Progesterone was used as a model substance.


METHODS
Nanoparticles were prepared by polymerization of isobutylcyanoacrylate in presence of cyclodextrins or progesterone/ hydroxypropyl-beta-cyclodextrin complex. Particle size, zeta potential, cyclodextrin and progesterone loading of the particles were determined.


RESULTS
Nanoparticles could be easily prepared in presence of cyclodextrins. An increase in hydroxypropyl-beta-cyclodextrin concentration resulted in small nanoparticles (less than 50 nm). It was found that large amounts of cyclodextrins remained associated to the particles, resulting in a 50 fold increase in progesterone loading compared to nanoparticles prepared in absence of cyclodextrins.


CONCLUSIONS
The poly(isobutylcyanoacrylate)cyclodextrin nanoparticles were characterized by the presence of many lipophilic sites belonging to the cyclodextrins which were firmly anchored to the structure of the particles. Therefore, this new type of nanoparticles offers probably an opportunity for increasing the loading of nanoparticles with various lipophilic drugs.
Laboratoire de Pharmacotechnie et Biopharmacie, URA CNRS 1218, Faculté de Pharmacie, Châtenay-Malabry, France.
A
A
Monza da Silveira
G
G
Ponchel
F
F
Puisieux
D
D
Duchêne
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D002015:Bucrylate / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D003505:Cyclodextrins / Q000737:chemistry*; D004337:Drug Carriers; D010316:Particle Size; D011374:Progesterone / Q000008:administration & dosage; D013501:Surface-Active Agents / Q000737:chemistry; D047392:beta-Cyclodextrins
D003505:Cyclodextrins; D004337:Drug Carriers; D013501:Surface-Active Agents; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D002015:Bucrylate; D011374:Progesterone