3-aminopropyl functionalized magnesium phyllosilicate as an organoclay based drug carrier for improving the bioavailability of flurbiprofen

• Published in: International journal of nanomedicine Vol. 8; no. 1; pp. 4147 - 4155
• Main Authors: Yang, Liang, Choi, Soo-Kyung, Shin, Hyun-Jae, Han, Hyo-Kyung
• Format: Journal Article
• Language: English
• Published: New Zealand Dove Medical Press Limited 01.01.2013; Taylor & Francis Ltd; Dove Medical Press
• Subjects: Administration, Oral; Animals; Bioavailability; Biological Availability; Drug Carriers - administration & dosage; Drug Carriers - chemistry; Drug Carriers - pharmacokinetics; Drug delivery systems; Drugs; Flurbiprofen; Flurbiprofen - administration & dosage; Flurbiprofen - blood; Flurbiprofen - chemistry; Flurbiprofen - pharmacokinetics; Health aspects; Hydrogen-Ion Concentration; Magnesium Silicates - administration & dosage; Magnesium Silicates - chemistry; Magnesium Silicates - pharmacokinetics; Male; Original Research; Rats; Rats, Sprague-Dawley; Solubility; Vehicles; South Korea; poorly water-soluble drugs; oral bioavailability; aminopropyl functionalized magnesium phyllosilicate; organic clay
• ISSN: 1178-2013; 1176-9114; 1178-2013
• DOI: 10.2147/ijn.s51756

This study aimed to develop an oral delivery system using clay-based organic-inorganic hybrid materials to improve the bioavailability of the drug, flurbiprofen, which is poorly soluble in water. 3-aminopropyl functionalized magnesium phyllosilicate (AMP clay) was synthesized by a one-pot direct sol-gel method, and then flurbiprofen (FB) was incorporated into AMP clay (FB-AMP) at different drug/clay ratios. The structural characteristics of AMP and FB-AMP formulation were confirmed by X-ray diffraction, Fourier transform infrared spectroscopy, and transmission electron microscopy. Among tested formulations, FB-AMP(3), dramatically increased the dissolution of FB and achieved rapid and complete drug release within 2 hours. More than 60% of FB was released from FB-AMP(3) after 30 minutes; the drug was completely dissolved in the water within 2 hours. Under the acidic condition (pH 1.2), FB-AMP(3) also increased the dissolution of FB by up to 47.1% within 1 hour, which was three-fold higher than that of untreated FB. Furthermore, following an oral administration of FB-AMP(3) to Sprague-Dawley rats, the peak plasma concentration and area under the plasma concentration-time curve of FB increased two-fold, and the time to reach the peak plasma concentration was shortened compared with that in the untreated FB. This result suggests that the oral drug delivery system using clay-based organic-inorganic hybrid material might be useful to improve the bioavailability of FB.