Evaluation of the Hydrophobic Drug Loading Characteristics in Nanoprecipitated Amphiphilic Cyclodextrin Nanospheres

• Published in: Pharmaceutical development and technology 1998, Vol.3 (1), p.85-94
• Main Authors: Lemos-Senna, Elenara, Wouessidjewe, Denis, Lesieur, Sylviane, Puisieux, Francis, Couarraze, G., Duch ne, Dominique
• Format: Article
• Language: English
• Subjects: Amphiphilic cyclodextrins; Biological and medical sciences; Calorimetry, Differential Scanning; Colloidal carriers; Cyclodextrins - chemistry; Drug Carriers; Evaluation Studies as Topic; General pharmacology; Hydrophobic drug; Medical sciences; Microscopy, Electron; Microspheres; Nanospheres; Particle Size; Pharmacology. Drug treatments; Physicochemical properties. Structure-activity relationships; Poloxalene; Polysorbates; Progesterone - administration & dosage; Progesterone - pharmacokinetics; Surface-Active Agents; X-Ray Diffraction
• ISSN: 1083-7450; 1097-9867
• DOI: 10.3109/10837459809028482

ABSTRACT The aim of this work was to evaluate the loading capacity and the association characteristics of the hydrophobic drug progesterone on amphiphilic cyclodextrin nanospheres prepared by the nano-precipitation method. The colloidal suspensions were prepared in the presence or absence of two different surfactants, Pluronic F68 and Tween 80. The physicochemical characteristics of the nanospheres were assessed using a nanosizer, zetameter, and transmission electron microscope. The physical state of the drug was verified using differential scanning calorimetry (DSC) and x-ray diffraction (XRD) methods. The in vitro progesterone release was investigated at 37°C after dilution of the suspensions in sink conditions. Nanospheres with a mean diameter from 100 to 300 nm and a low degree of polydispersity were prepared from amphiphilic hexanoyl-γ-cyclodextrin. The progesterone loading capacity was not affected by the formulation parameters tested. The DSC and XRD studies demonstrated the absence of the crystalline domains of progesterone in loaded nanospheres. The DSC studies also demonstrated the presence of interactions between the drug and carrier. The release of the drug from the carrier was extremely rapid and was governed by a partition phenomenon that depends only on the solubility of the drug in the release medium. From these results, we concluded that with this method, the progesterone is molecularly associated at the surface of the cyclodextrin nanospheres, probably through hydrophobic interactions in specific sites. The release profiles obtained can be of value when an improvement in the bioavailability of the drug is desired.