Synergistic role of self-emulsifying lipids and nanostructured porous silica particles in optimizing the oral delivery of lovastatin
Date
2014
Authors
Rao, S.
Tan, A.
Boyd, B.J.
Prestidge, C.A.
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Journal article
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Nanomedicine, 2014; 9(18):2745-2759
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Abstract
Aim: To investigate the role of self-emulsifying lipids and porous silica particlesin enhancing supersaturated drug loading and biopharmaceutical performanceof nanostructured silica-lipid hybrid (SLH) systems.
Conclusion: In conclusion, SLHs profit from advantages associated with both self-emulsifying lipids and porous silica, and provide potentially improved therapyagainst coronary artery disease.
Materials & methods: Two lovastatin (LOV)-SLHs were engineered from self-emulsifying lipid (Gelucire® 44/14; Gattefossé, Lyon, France) and Aerosil® 380 (SLH-A; Evonik Industries, Essen, Germany) or Syloid® 244FP silica (SLH-S; Grace Davison Discovery Sciences, Rowville, Australia).
Results & discussion: The LOV-SLHs encapsulated LOV at 10% w/w, which is ≥3-foldhigher than typical lipid formulations in the absence of porous silica. The LOV-SLHsretained self-emulsifying lipid-associated solubilization benefits and improved drug solubilization by twofold in simulated intestinal condition. SLH-S, with larger surface area (299 m2/g), was superior to SLH-A (184 m2/g) in optimizing oral bioavailability, suggesting a critical role of the silica geometry. Bioavailability of SLH-S was 2.8- and1.3-fold higher than pure drug and drug suspension in Gelucire 44/14, respectively.
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Copyright 2014 Future Medicine