Curcumin (CUR) is considered as one of the most bioactive molecules ever discovered from nature due to its proven anti-inflammatory and antioxidant in both preclinical and clinical studies. Despite its proven safety and efficacy, the clinical translation of CUR into a useful therapeutic agent is still limited due to its poor oral bioavailability. To overcome its limitation and enhance oral bioavailability by improving its aqueous solubility, stability, and intestinal permeability, a novel CUR formulation (NCF) was developed using the self-nanomicellizing solid dispersion strategy. From the initial screening of polymers for their potential to improve the solubility and stability, Soluplus (SOL) was selected. The optimized NCF demonstrated over 20,000-fold improvement in aqueous solubility as a result of amorphization, hydrogen bonding interaction, and micellization determined using differential scanning calorimetry, X-ray diffraction, scanning electron microscopy, Fourier transform infrared spectroscopy, nuclear magnetic resonance, dynamic light scattering, and transmission electron microscopy. Moreover, the greater stabilizing effect in alkaline pH and light was observed. Furthermore, significant enhancement of dissolution and permeability of CUR across everted sacs of rat small intestine were noticed. Pharmacokinetic studies demonstrated that the oral bioavailability of CUR was increased 117 and 17-fold in case of NCF and physical mixture of CUR and SOL compared to CUR suspension. These results suggest NCF identified as a promising new approach for repositioning of CUR for pharmaceutical application by enhancing the oral bioavailability of CUR. The findings herein stimulate further in vivo evaluations and clinical tests of NCF.
Biochem Pharmacol. 2008 Feb 15;75(4):787-809
[PMID:
17900536]
Am J Geriatr Psychiatry. 2018 Mar;26(3):266-277
[PMID:
29246725]
AAPS PharmSciTech. 2015 Aug;16(4):824-34
[PMID:
25567525]
Drug Des Devel Ther. 2018 Jul 05;12:2051-2069
[PMID:
30013324]
Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):799-813
[PMID:
24056053]
Int J Pharm. 2016 Dec 30;515(1-2):490-500
[PMID:
27789367]
Tissue Barriers. 2018 Jan 2;6(1):e1425085
[PMID:
29420166]
J Pharm Sci. 2005 Oct;94(10):2166-74
[PMID:
16136578]
Molecules. 2016 Oct 17;21(10):
[PMID:
27763524]
Pharm Dev Technol. 2017 Feb;22(1):2-12
[PMID:
26616399]
Pharm Res. 2016 Aug;33(8):1972-87
[PMID:
27245466]
Int J Pharm. 2004 Mar 1;271(1-2):281-6
[PMID:
15129995]
Mol Pharm. 2015 Jan 5;12(1):162-70
[PMID:
25426538]
Iran J Pharm Res. 2015 Winter;14(1):35-50
[PMID:
25561910]
Int J Pharm. 2014 Dec 30;477(1-2):399-407
[PMID:
25445521]
Mol Pharm. 2016 Jan 4;13(1):287-94
[PMID:
26623947]
Molecules. 2015 Jun 19;20(6):11345-56
[PMID:
26102068]
Curr Alzheimer Res. 2005 Apr;2(2):131-6
[PMID:
15974909]
J Pharm Pharmacol. 2017 May;69(5):544-553
[PMID:
27431770]
Cancer Res Treat. 2014 Jan;46(1):2-18
[PMID:
24520218]
Mol Pharm. 2007 Nov-Dec;4(6):807-18
[PMID:
17999464]
Nanoscale Res Lett. 2014 Dec;9(1):2406
[PMID:
26088982]
Drug Dev Ind Pharm. 2015;41(11):1847-55
[PMID:
25721984]
Adv Drug Deliv Rev. 2016 May 1;100:27-50
[PMID:
26705850]
J Pharm Sci. 2011 May;100(5):1987-95
[PMID:
21374628]
Int J Pharm. 2012 Mar 15;424(1-2):18-25
[PMID:
22226878]
Drug Dev Ind Pharm. 2017 Nov;43(11):1846-1857
[PMID:
28665151]
Int J Pharm. 2015 May 15;485(1-2):215-28
[PMID:
25772420]
Pharm Dev Technol. 2018 Jul;23(6):573-586
[PMID:
27824281]
Biotechnol Adv. 2014 Nov 1;32(6):1053-64
[PMID:
24793420]
Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):1325-36
[PMID:
23954511]
J Psychopharmacol. 2015 May;29(5):642-51
[PMID:
25277322]
Int J Pharm. 2007 Jun 29;338(1-2):27-34
[PMID:
17298869]
Eur J Pharmacol. 2006 Sep 1;545(1):51-64
[PMID:
16904103]
AAPS J. 2006 Jul 07;8(3):E443-9
[PMID:
17025261]
Drug Des Devel Ther. 2018 Jul 09;12:2111-2128
[PMID:
30022810]
Int J Biochem Cell Biol. 2009 Jan;41(1):40-59
[PMID:
18662800]
Food Chem. 2014 Aug 1;156:227-33
[PMID:
24629962]
AAPS J. 2009 Sep;11(3):495-510
[PMID:
19590964]
AAPS J. 2013 Jan;15(1):195-218
[PMID:
23143785]
Genet Mol Biol. 2015 Dec;38(4):490-8
[PMID:
26537603]
Front Neurol. 2014 May 09;5:69
[PMID:
24847308]
Br J Nutr. 2016 Jun;115(12):2106-13
[PMID:
27102361]
Eur J Pharm Biopharm. 2015 Aug;94:322-32
[PMID:
26073546]
Eur J Pharm Biopharm. 2011 Feb;77(2):275-82
[PMID:
21147222]
AAPS PharmSciTech. 2012 Mar;13(1):59-66
[PMID:
22105472]
Drug Deliv. 2017 Nov;24(1):962-978
[PMID:
28633547]
Eur J Pharm Sci. 2014 Oct 1;62:16-22
[PMID:
24836392]
J Pharm Pharmacol. 2018 Feb;70(2):242-249
[PMID:
29148063]
Drug Des Devel Ther. 2015 May 22;9:2745-56
[PMID:
26045660]
Biomaterials. 2010 Sep;31(25):6597-611
[PMID:
20553984]
Mol Nutr Food Res. 2011 Mar;55(3):495-503
[PMID:
20938993]
Drug Des Devel Ther. 2015 Jan 22;9:631-42
[PMID:
25653501]
J Colloid Interface Sci. 2011 Feb 1;354(1):116-23
[PMID:
21044788]
AAPS PharmSciTech. 2016 Apr;17(2):252-61
[PMID:
26040724]
