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Fenofibrate Nanocrystal Composite Microparticles for Intestine-Specific Oral Drug Delivery System

1
New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Warren Street, Newark, NJ 07102, USA
2
Pandorum Technologies Pvt Ltd, Bangalore Bioinnovation Centre, Helix Biotech Park, Electronic City Phase 1, Bangalore, Karnataka 560100, India
*
Authors to whom correspondence should be addressed.
Current address: Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE 68198-5880, USA.
Pharmaceuticals 2019, 12(3), 109; https://doi.org/10.3390/ph12030109
Received: 16 June 2019 / Revised: 9 July 2019 / Accepted: 10 July 2019 / Published: 16 July 2019
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Abstract

Hydrophobic drug nanocrystals (NCs) manufactured by particle engineering have been extensively investigated for enhanced oral bioavailability and therapeutic effectiveness. However, there are significant drawbacks, including fast dissolution of the nanocrystals in the gastric environment, leading to physicochemical instability. To solves this issue, we developed an innovative technique that involves the encapsulation of nanocrystals in composite spherical microparticles (NCSMs). Fenofibrate (FNB) NCs (FNB-NCs) manufactured by a wet stirred media milling (WSMM) technique and an ionotropic crosslinking method were used for FNB-NC encapsulation within gastroresistant NCSMs. Various solid-state methods were used for characterizing NCSMs. The pH-sensitive NCSMs showed a site-specific release pattern at alkaline pH and nearly 0% release at low pH (gastric environment). This phenomenon was confirmed by a real-time in situ UV-imaging system known as the surface dissolution imager (SDI), which was used to monitor drug release events by measuring the color intensity and concentration gradient formation. All these results proved that our NCSM approach is an innovative idea in oral drug delivery systems, as it resolves significant challenges in the intestine-specific release of hydrophobic drugs while avoiding fast dissolution or burst release. View Full-Text
Keywords: bioavailability; fenofibrate; media milling; nanocrystals; intestine-specific delivery; composites spherical microparticles bioavailability; fenofibrate; media milling; nanocrystals; intestine-specific delivery; composites spherical microparticles
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Kevadiya, B.D.; Chen, L.; Zhang, L.; Thomas, M.B.; Davé, R.N. Fenofibrate Nanocrystal Composite Microparticles for Intestine-Specific Oral Drug Delivery System. Pharmaceuticals 2019, 12, 109.

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