Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 444, Issue 1-2, Pages 162-168Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2013.01.021
Keywords
Porous starch; Self-assembly; Nanoparticles; Oral absorption; Probucol
Categories
Funding
- National Basic Research Program of China [2009CB930304, 2013CB932503, 2013CB932704]
- Shanghai Rising-Star Program [11QA1407900]
- SA-SIBS Scholarship Program
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The therapeutic efficacy of lipophilic drugs is commonly restricted by the low systemic exposure after oral administration. In this work, a new delivery system combining the advantages of porous starch and self-assembled nanocarrier was designed to improve the oral absorption of lipophilic drugs. The lipophilic probucol loaded porous starch based self-assembled nano-delivery (PSN) system was developed and characterized. The probucol loaded nanocarrier (PLN) could be formed by self-assembly when PSN was dispersed into the gastrointestinal (GI) fluids. PLN was nanometer-sized particles with narrow size distribution and exhibited good stability in GI fluids. The aqueous solubility of probucol was increased over 50,000-fold by PSN delivery system and the cumulative release of lipophilic probucol was increased over 80% in GI fluids. The distribution of probucol in duodenum, jejunum and ileum was respectively improved 7.17, 15.99 and 33.61-fold by PSN. In particular, the oral bioavailability of probucol from PSN was greatly improved about 9.96-fold than that from free drug suspension and 3.71-fold higher than that from the directed adsorbed probucol loaded porous starch system, which effectively confirmed the high potential of the strategy in enhancing the oral absorption of lipophilic drugs. (C) 2013 Elsevier B. V. All rights reserved.
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