Enhancement of Oral Bioavailability of Tripterine Through Lipid Nanospheres: Preparation,Characterization, and Absorption Evaluation |
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| Institution: | 1. Department of Environmental Engineering, São Paulo State University, Sorocaba, SP, Brazil;2. Department of Biochemistry, State University of Campinas, Campinas, SP, Brazil;3. Human and Natural Sciences Center, Federal University of ABC (UFABC), Santo André, SP, Brazil;1. Department of Biomedical Engineering, School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, China;2. Department of Pharmacology, Medical College, Nantong University, Nantong 226001, China;3. Department of Biomedical Engineering, School of Automation, Nanjing University of Aeronautics and Astronautics, Nanjing 210016, China;1. Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC, Australia;2. Starpharma Pty Ltd, Melbourne, VIC, Australia;3. ARC Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC, Australia |
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| Abstract: | Oral delivery of anticancer drugs remains challenging because of limited water-solubility and/or poor permeability. Here, we aimed to enhance the oral bioavailability of tripterine (TRI, a plant-derived anticancer compound) using lipid nanospheres (LNs) and to determine the mechanisms of oral absorption. TRI-loaded LNs (TRI-LNs) were prepared by rapid dispersion of an ethanol mixture of TRI, lecithin, sodium oleate, and soybean oil into water. The obtained LNs were 150 nm in size with a high value of entrapment efficiency (99.95%). TRI-LNs were fairly stable and the drug release was negligible (< 0.2%) in simulated physiological fluid. The pharmacokinetic results showed that LNs significantly enhanced the oral bioavailability of TRI with a relative bioavailability of 224.88% (TRI suspensions was used as a reference). The mechanistic studies demonstrated that improved intestinal permeability and post-enterocyte lymphatic transport were mainly responsible for the enhanced oral absorption. Our findings suggested that LNs may be a viable oral carrier for poorly bioavailable drugs. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:171 1-1719, 2014 |
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