Nanoemulsion for Solubilization, Stabilization, and in Vitro Release of Pterostilbene for Oral Delivery

Overview

Journal AAPS PharmSciTech

Publisher Springer

Specialty Pharmacology

Date 2014 May 17

PMID 24831090

Citations 24

Authors

Yue Zhang

Zhenhua Shang

Chunhui Gao

Man Du

Shixia Xu

Haiwen Song

Tingting Liu

Affiliations

Soon will be listed here.

Abstract

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).

Citing Articles

Formulation and optimisation of bedaquiline nanoemulsions for the potential treatment of multi drug resistant tuberculosis in paediatrics using quality by design.

Ajayi T, Poka M, Witika B Sci Rep. 2024; 14(1):31891.

PMID: 39738619 PMC: 11686176. DOI: 10.1038/s41598-024-83408-1.

Therapeutic Implications of Dietary Polyphenols-Loaded Nanoemulsions in Cancer Therapy.

Tomar R, Das S, Balaga V, Tambe S, Sahoo J, Rath S ACS Appl Bio Mater. 2024; 7(4):2036-2053.

PMID: 38525971 PMC: 11530091. DOI: 10.1021/acsabm.3c01205.

Enhanced Antioxidant and Neuroprotective Properties of Pterostilbene (Resveratrol Derivative) in Amorphous Solid Dispersions.

Rosiak N, Tykarska E, Cielecka-Piontek J Int J Mol Sci. 2024; 25(5).

PMID: 38474022 PMC: 10932125. DOI: 10.3390/ijms25052774.

Folic/lactobionic acid dual-targeted polymeric nanocapsules for potential treatment of hepatocellular carcinoma.

Kabil M, Abdel Gaber S, Hamzawy M, El-Sherbiny I, Nasr M Drug Deliv Transl Res. 2023; 14(5):1338-1351.

PMID: 37930630 DOI: 10.1007/s13346-023-01467-9.

Nanoemulsion: An Emerging Novel Technology for Improving the Bioavailability of Drugs.

Preeti , Sambhakar S, Malik R, Bhatia S, Al Harrasi A, Rani C Scientifica (Cairo). 2023; 2023:6640103.

PMID: 37928749 PMC: 10625491. DOI: 10.1155/2023/6640103.

References

Lee M, Pan M, Chiou Y, Cheng A, Huang H . Resveratrol modulates MED28 (Magicin/EG-1) expression and inhibits epidermal growth factor (EGF)-induced migration in MDA-MB-231 human breast cancer cells. J Agric Food Chem. 2011; 59(21):11853-61. DOI: 10.1021/jf202426k. View

Wang L, Li X, Zhang G, Dong J, Eastoe J . Oil-in-water nanoemulsions for pesticide formulations. J Colloid Interface Sci. 2007; 314(1):230-5. DOI: 10.1016/j.jcis.2007.04.079. View

Desai N, Nagarsenker M . Design and evaluation of self-nanoemulsifying pellets of repaglinide. AAPS PharmSciTech. 2013; 14(3):994-1003. PMC: 3755138. DOI: 10.1208/s12249-013-9990-9. View

Adrian M, Jeandet P, Tesson L, Bessis R . Stilbene content of mature Vitis vinifera berries in response to UV-C elicitation. J Agric Food Chem. 2001; 48(12):6103-5. DOI: 10.1021/jf0009910. View

Lu W, Wang X, Chen J, Lu Y, Wu N, Kang W . [Studies on the chemical constituents of chloroform extract of Dracaena cochinchinensis]. Yao Xue Xue Bao. 2002; 33(10):755-8. View

Chang L, Wu C, Liu C, Chuo W, Li P, Tsai T . Preparation, characterization and cytotoxicity evaluation of tanshinone IIA nanoemulsions. J Biomed Nanotechnol. 2011; 7(4):558-67. DOI: 10.1166/jbn.2011.1315. View

Ferrer P, Asensi M, Segarra R, Ortega A, Benlloch M, Obrador E . Association between pterostilbene and quercetin inhibits metastatic activity of B16 melanoma. Neoplasia. 2005; 7(1):37-47. PMC: 1490314. DOI: 10.1593/neo.04337. View

Wang L, Dong J, Chen J, Eastoe J, Li X . Design and optimization of a new self-nanoemulsifying drug delivery system. J Colloid Interface Sci. 2008; 330(2):443-8. DOI: 10.1016/j.jcis.2008.10.077. View

Schneider J, Alosi J, McDonald D, McFadden D . Pterostilbene inhibits lung cancer through induction of apoptosis. J Surg Res. 2009; 161(1):18-22. DOI: 10.1016/j.jss.2009.06.027. View

10.

Liu Y, Zhang D, Zou D, Wang Y, Duan C, Jia L . Development and in vitro characterizations of bifendate nanosuspensions. J Biomed Nanotechnol. 2011; 7(5):621-31. DOI: 10.1166/jbn.2011.1330. View

11.

Hougee S, Faber J, Sanders A, de Jong R, van den Berg W, Garssen J . Selective COX-2 inhibition by a Pterocarpus marsupium extract characterized by pterostilbene, and its activity in healthy human volunteers. Planta Med. 2005; 71(5):387-92. DOI: 10.1055/s-2005-864130. View

12.

Perecko T, Drabikova K, Rackova L, ciz M, Podborska M, Lojek A . Molecular targets of the natural antioxidant pterostilbene: effect on protein kinase C, caspase-3 and apoptosis in human neutrophils in vitro. Neuro Endocrinol Lett. 2010; 31 Suppl 2:84-90. View

13.

Gong Y, Wu Y, Zheng C, Fan L, Xiong F, Zhu J . An excellent delivery system for improving the oral bioavailability of natural vitamin E in rats. AAPS PharmSciTech. 2012; 13(3):961-6. PMC: 3429676. DOI: 10.1208/s12249-012-9819-y. View

14.

Vandamme T, Anton N . Low-energy nanoemulsification to design veterinary controlled drug delivery devices. Int J Nanomedicine. 2010; 5:867-73. PMC: 2963933. DOI: 10.2147/IJN.S13273. View

15.

Pons R, Carrera I, Caelles J, Rouch J, Panizza P . Formation and properties of mini-emulsions formed by microemulsions dilution. Adv Colloid Interface Sci. 2003; 106:129-46. DOI: 10.1016/s0001-8686(03)00108-8. View

16.

Szebeni J, Alving C, Savay S, Barenholz Y, Priev A, Danino D . Formation of complement-activating particles in aqueous solutions of Taxol: possible role in hypersensitivity reactions. Int Immunopharmacol. 2001; 1(4):721-35. DOI: 10.1016/s1567-5769(01)00006-6. View

17.

Paul B, Masih I, Deopujari J, Charpentier C . Occurrence of resveratrol and pterostilbene in age-old darakchasava, an ayurvedic medicine from India. J Ethnopharmacol. 2000; 68(1-3):71-6. DOI: 10.1016/s0378-8741(99)00044-6. View

18.

Chiou Y, Tsai M, Nagabhushanam K, Wang Y, Wu C, Ho C . 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(6):2725-33. DOI: 10.1021/jf2000103. View

19.

Tolomeo M, Grimaudo S, Di Cristina A, Roberti M, Pizzirani D, Meli M . Pterostilbene and 3'-hydroxypterostilbene are effective apoptosis-inducing agents in MDR and BCR-ABL-expressing leukemia cells. Int J Biochem Cell Biol. 2005; 37(8):1709-26. DOI: 10.1016/j.biocel.2005.03.004. View

20.

Warisnoicharoen W, Lansley A, Lawrence M . Nonionic oil-in-water microemulsions: the effect of oil type on phase behaviour. Int J Pharm. 2000; 198(1):7-27. DOI: 10.1016/s0378-5173(99)00406-8. View