A Self-Assembled Nanodelivery System Enhances The Oral Bioavailability of Daidzein: In Vitro Characteristics and In Vivo Performance

Abstract

Aim: A self-assembled nano-based delivery system was designed and developed to increase the oral bioavailability of poor hydrophilic and lipophilic daidzein. Methods: Daidzein was firstly combined with lecithin to form the daidzein–lecithin complex, then self-assembled into micelles (DLMs) with lecithin and sodium bile. The physiochemical properties and intestinal absorption of DLMs were characterized, and the pharmacokinetic behavior was evaluated in rats. Results: DLMs exhibited nanometer-sized particles. DLMs were mainly distributed in the stomach and proximal intestine after oral administration. The intestinal absorption of DLMs was significantly improved, and DLMs could be absorbed via both endocytosis and passive transport. The AUC_0-t value of daidzein in rats treated with DLMs was ninefold greater than that of free daidzein suspension. Conclusion: The presented delivery system could provide a new promising strategy for enhancing the oral bioavailability of drugs with poor hydrophilicity and lipophilicity.

Original submitted: 3/10/2010; Revised submitted: 22/12/2010

Keywords::

• bioavailability
• daidzein
• intestinal absorption
• mixed micelle
• oral delivery

Financial & competing interests disclosure

The National Basic Research Program of China (2009CB930304 and 2007CB935800), the National Natural Science Foundation of China (30925041, 30901866), Shanghai Nanomedicine Program (1052nm06300), National Science & Technology Major Project ‘Key New Drug Creation and Manufacturing Program’ (No 2009ZX09501–024 and 2009ZX09301–001) are gratefully acknowledged for their financial support. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

Ethical conduct of research

The authors state that they have obtained appropriate institutional review board approval or have followed the principles outlined in the Declaration of Helsinki for all human or animal experimental investigations. In addition, for investigations involving human subjects, informed consent has been obtained from the participants involved.

Additional information

Funding

The National Basic Research Program of China (2009CB930304 and 2007CB935800), the National Natural Science Foundation of China (30925041, 30901866), Shanghai Nanomedicine Program (1052nm06300), National Science & Technology Major Project ‘Key New Drug Creation and Manufacturing Program’ (No 2009ZX09501–024 and 2009ZX09301–001) are gratefully acknowledged for their financial support. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.