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

Authors Yang L, Choi SK, Shin HJ, Han HK

Received 18 July 2013

Accepted for publication 11 September 2013

Published 30 October 2013 Volume 2013:8(1) Pages 4147—4155

DOI https://doi.org/10.2147/IJN.S51756

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Liang Yang,1 Soo-Kyung Choi,2 Hyun-Jae Shin,2 Hyo-Kyung Han1

1College of Pharmacy, Dongguk University-Seoul, Siksa-dong, Ilsan-Donggu, Goyang, Gyunggi-do, Korea; 2Department of Chemical and Biochemical Engineering, Chosun University, Gwangju, Korea

Abstract: 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.

Keywords: poorly water-soluble drugs, aminopropyl functionalized magnesium phyllosilicate, organic clay, oral bioavailability

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