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.
Highlights
Despite significant advancements in nanoparticulate drug delivery systems, oral drug administration is still preferred over parenteral routes due to ease of administration, convenience, low cost, and versatility in dosage form preparations
The objective of the present study was the site-specific controlled release of FNB. This was achieved by making stable FNB-NCs using wet stirred media milling (WSMM), which were further encapsulated in nanocrystals in composite spherical microparticles (NCSMs) for intestinal site-specific release
The objective of the present study was to determine if FNB-NC encapsulation in NCSMs could be useful in developing improved bioavailability by site-specific release of FNB-NCs
Summary
Despite significant advancements in nanoparticulate drug delivery systems, oral drug administration is still preferred over parenteral routes due to ease of administration, convenience, low cost, and versatility in dosage form preparations. It reduces the risk of cross-infection and needle-stick injuries [1,2]. Improvements in BCS-II drug dissolution rates and stability pose a significant challenge for formulation scientists. Direct oral administration of a BCS-II drug nanosuspension is not suitable due to the potential for very fast dissolution of the drug in Pharmaceuticals 2019, 12, 109; doi:10.3390/ph12030109 www.mdpi.com/journal/pharmaceuticals
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