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

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.

Sustained-release solid dispersion of pelubiprofen using the blended mixture of aminoclay and pH independent polymers: preparation and in vitro/in vivo characterization

“…Aminoclay was prepared by the method reported by Yang et al. ( 2013 ). Acetone was purchased from Daejung chemical & metals Co., Ltd. (Gyeonggi-Do, Korea).…”

“…Aminoclay is delaminated to cationic and water soluble nanosheets in water. Aminoclay can enhance the solubility of acidic drugs by modulating the microenvironmental pH to more basic (Yang et al., 2013 ; Yang et al., 2016 ). In addition, aminoclay can control the drug release by interacting with negatively charged drug and/or polymers (Holmström et al., 2007 ).…”

Aminoclay Nanoparticles Induce Anti-Inflammatory Dendritic Cells to Attenuate LPS-Elicited Pro-Inflammatory Immune Responses

“…ACNs are layered materials composed of magnesium phyllosilicate functionalized with aminopropyl groups [1,2] (Figure 1A). Although it has been previously reported that ACNs exhibit low toxicity in human lung and skin fibroblast cell lines [1], whether ACNs can modulate the immune system remains largely unknown.…”

“…Aminoclay nanoparticles (ACNs), one of the drug carriers that can be orally administered, are synthetic organic-inorganic layered materials delaminated to water-soluble cationic nanosheets in water [1]. ACNs with a positive charge can interact with negatively charged drugs to produce drug-ACN complexes, which enhance the dissolution and absorption rates of poorly water-soluble drugs such as flurbiprofen and telmisartan in the gastrointestinal tract [2,3]. Furthermore, ACN-based carrier systems can be employed for delivering insulin to the intestine [4].…”

Flurbiprofen: Determination of safety profile, analgesic effect, and interaction with lipoic acid in murine

“…The pharmacological effects of steroidal anti-inflammatory drugs are attributed to the inhibitory effects of NF-κB, either by direct interaction with the NF-κB p65 subunit (4) or by increasing transcription of its inhibitor (I-κB-α) (5). Pharmacokinetic data on flurbiprofen has been studied in various animal models and humans (6,7); however, it is well absorbed orally, reaching a maximum concentration in the blood in approximately 1.5 hours (range 0.5-4 hours) (8,9). Flurbiprofen was eliminated within 24 hours of the last administered dose (10).…”