title: Formulation design, preparation, and in vitro and in vivo characterizations of β-Elemene-loaded nanostructured lipid carriers.
abstract: In the present study, nanostructured lipid carriers (NLCs) were prepared and optimized for the intravenous delivery of β-Elemene (β-E). Aqueous dispersions of NLCs were successfully prepared by high-pressure homogenization method using glycerol monostearate as the solid lipid and a mixture of Maisine 35-1 and Labrafil M1944 CS as the liquid lipid. The results revealed that the morphology of the NLCs was spheroidal. The particle size, zeta potential, and entrapment efficiency (EE) for the optimized formulation were observed as 138.9 nm, -20.2 mV, and 82.11%, respectively. X-ray diffraction analysis revealed the formation of less ordered structures in the inner core of the NLC particles. Moreover, the β-E-loaded NLCs were also less irritating and less toxic compared to Elemene injection. In addition, β-E-NLCs showed a significantly higher bioavailability and anti-tumor efficacy than Elemene injection. Taken together, our data indicate that the β-E-NLCs described in this study are well-suited for the intravenous delivery of β-E.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.
authors.forename: Feng
authors.initials: F
authors.lastname: Shi
authors.forename: Gang
authors.initials: G
authors.lastname: Yang
authors.forename: Juan
authors.initials: J
authors.lastname: Ren
authors.forename: Teng
authors.initials: T
authors.lastname: Guo
authors.forename: Yan
authors.initials: Y
authors.lastname: Du
authors.forename: Nianping
authors.initials: N
authors.lastname: Feng
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry* / Q000493:pharmacokinetics; D008055:Lipids / Q000737:chemistry*; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry*; D036103:Nanotechnology; D010316:Particle Size; D011312:Pressure; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D012717:Sesquiterpenes / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D014680:Veins / Q000187:drug effects / Q000473:pathology
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008055:Lipids; D012717:Sesquiterpenes; C445979:beta-elemene
keywords: anti-tumor efficacy; high-pressure homogenization; nanostructured lipid carriers; venous irritation; β-Elemene
references.citation: Int J Pharm. 2010 Jul 15;394(1-2):179-85
references.pmid: 20471464
references.citation: Int J Pharm. 2010 May 31;391(1-2):313-21
references.pmid: 20214958
references.citation: Lancet Oncol. 2003 Mar;4(3):177-85
references.pmid: 12623363
references.citation: J Mol Neurosci. 2011 May;44(1):31-40
references.pmid: 21246417
references.citation: Colloids Surf B Biointerfaces. 2013 Feb 1;102:251-6
references.pmid: 23006566
references.citation: Curr Cancer Drug Targets. 2010 Nov;10(7):705-15
references.pmid: 20578985
references.citation: Cell Mol Life Sci. 2005 Apr;62(7-8):881-93
references.pmid: 15868411
references.citation: Int J Pharm. 2012 Jul 1;430(1-2):292-8
references.pmid: 22486962
references.citation: J Control Release. 2009 Sep 1;138(2):103-12
references.pmid: 19433120
references.citation: Zhong Yao Cai. 2006 Feb;29(2):157-60
references.pmid: 16617787
references.citation: Mol Med Rep. 2012 Jul;6(1):185-90
references.pmid: 22552783
references.citation: Bioorg Med Chem. 2009 Feb 1;17(3):1118-24
references.pmid: 19128976
references.citation: Int J Pharm. 2010 Sep 15;397(1-2):155-63
references.pmid: 20599600
references.citation: Int J Pharm. 2011 Aug 30;415(1-2):232-43
references.pmid: 21640809
references.citation: J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Feb 1;877(4):408-14
references.pmid: 19124285
references.citation: Biomaterials. 2010 Jan;31(2):321-9
references.pmid: 19800113
references.citation: Int J Pharm. 2011 Jun 15;411(1-2):188-96
references.pmid: 21421039
references.citation: Colloids Surf B Biointerfaces. 2011 Jul 1;85(2):262-9
references.pmid: 21435845
references.citation: Eur J Pharm Biopharm. 2000 Jul;50(1):161-77
references.pmid: 10840199
references.citation: J Control Release. 2010 Jun 1;144(2):233-41
references.pmid: 20153385
references.citation: Lung Cancer. 2007 Mar;55(3):337-41
references.pmid: 17126951
references.citation: Molecules. 2010 Jul 27;15(8):5093-103
references.pmid: 20714287
references.citation: Eur J Pharm Biopharm. 2007 Aug;67(1):141-8
references.pmid: 17346953
references.citation: Int J Oncol. 2007 Aug;31(2):241-52
references.pmid: 17611679
references.citation: Fitoterapia. 2010 Oct;81(7):680-9
references.pmid: 20471457
references.citation: Int J Pharm. 2008 Feb 4;348(1-2):70-9
references.pmid: 17719191
references.citation: Contemp Clin Trials. 2006 Feb;27(1):70-82
references.pmid: 16243588
references.citation: Int J Nanomedicine. 2012;7:2033-43
references.pmid: 22619540
references.citation: Int J Pharm. 2006 May 11;314(1):83-9
references.pmid: 16563671
references.citation: Pharm Res. 1999 Jun;16(6):930-8
references.pmid: 10397616
references.citation: Int J Pharm. 2008 May 22;356(1-2):282-90
references.pmid: 18289806