Nanoemulsion for Solubilization, Stabilization, and In Vitro Release of Pterostilbene for Oral Delivery
- 399 Downloads
Pterostilbene, being extracted from many plants, has significant biological activities in preventing cancer, diabetes, and cardiovascular diseases so as to have great potential applications in pharmaceutical fields. But the poor solubility and stability of pterostilbene strictly restrained its applications. As a good protection and oral delivery system, an optimal nanoemulsion for pterostilbene was developed by using low-energy emulsification method. Systematic pseudo-ternary phase diagrams have been studied in optimization of nanoemulsion formulations. The prepared pterostilbene nanoemulsion was characterized by transmission electron microscope, Fourier transform Raman spectrum, and laser droplet size analyzer. Nanoemulsion droplets are circular with smooth margin, and the mean size is 55.8 ± 10.5 nm. The results illustrated that the nanoemulsion as oral delivery system dramatically improved the stability and solubility of pterostilbene, and in vitro release of pterostilbene was significantly improved (96.5% in pH 3.6 buffer; 13.2% in pH 7.4 buffer) in comparison to the pterostilbene suspension (lower than 21.4% in pH 3.6 buffer; 2.6% in pH 7.4 buffer).
KEY WORDS3,5-dimethoxyl-4′-hydroxystilbene nanoemulsion pseudo-ternary phase diagram pterostilbene release study
We express our gratitude for the team fund of Hebei University of Science and Technology (XL201114, QD201211), Hebei Medical and Chemical Engineering Centre, and Pharmaceutical Molecular Chemistry Key Laboratory of Ministry Technology.
- 2.Spath E, Schlager J. Constituents of red sandalwood. II. Constitution of pterostilbene. Berichte der Deutschen Chemischen Gesellschaft [Abteilung] B: Abhandlungen. 1940;73B:881–4Google Scholar
- 6.Mathew J, Rao A. Chemical examination of Pterocarpus marsupium. J Indian Chem Soc. 1984;61:728–9.Google Scholar
- 7.Rimando A, Cody R. Determination of stilbenes in blueberries. LCGC North America. 2005;23:1192, 1194, 1196, 1198, 1200.Google Scholar
- 9.Wang X, Lu W, Chen J, Lu Y, Wu N, Kang W, et al. Studies on the chemical constituents of chloroform extract of Dracaena cochinchinensis. Yaoxue Xuebao. 1998;33(10):755–8.Google Scholar
- 10.King FE, King TJ, Manning LC. The Gibbs reaction and the constitution of jacareubin. J Chem Soc. 1957;51:563–6.Google Scholar
- 13.Chiou Y, Tsai M, Nagabhushanam K, Wang YJ, Wu CH, Ho CT, et al. Pterostilbene is more potent than resveratrol in preventing azoxymethane (AOM)-induced colon tumorigenesis via activation of the NF-E2-related factor 2 (Nrf2)-mediated antioxidant signaling pathway. J Agric Food Chem. 2011;59:2725–33.PubMedCrossRefGoogle Scholar
- 19.Lee M, Pan M, Chiou Y, Cheng A, Huang H. Resveratrol modulates MED28 (magicin/EG1) expression and inhibits epidermal growth factor (EGF)-induced migration in MDA-MB-231. human breast cancer cells. J Agric Food Chem. 2011; Online Computer File.Google Scholar
- 32.Zhang Y, Zhao SC. Process for preparation of stilbene compounds by Kornblum oxidation, C.N.; 2010. Patent 101,838,173 Sep 22.Google Scholar
- 34.Liu G, Zhang J, Wu P, Li J, Liu Y, Zhou X, et al. Preparation and evaluation of O/W pharmaceutical microemulsions. Zhongguo Nongye Kexue (Beijing, China). 2009;42(9):3328–33.Google Scholar
- 35.Chinese State Food and Drug Administration. Chinese Pharmacopoeia, 2010 ed. Appendix XIX c, Material medicine and pharmaceutical preparations stability experiment principle; Appendix V C, HPLC method; 2010.Google Scholar
- 36.Pan G, Jia X, Wei H. Comparison among several preparation methods for pseudo-ternary phase diagrams of pharmaceutical microemulsions. J Chin Pharm. 2006;17:21–3.Google Scholar