Abstract：
:Oral administration is the most convenient way of all the drug delivery routes. Orally administered bioactive compounds must resist the harsh acidic fluids or enzyme digestion in stomach, to reach their absorbed destination in small intestine. This is the case for silibinin, a drug used to protect liver cells against toxins that has also been demonstrated in vitro to possess anti-cancer effects. However, as many other drugs, silibinin can degrade in the stomach due to the action of the gastric fluid. The use of pH-sensitive self-nanoemulsifying drug delivery systems (pH-SNEDDS) could overcome the drawback due to degradation of the drug in the stomach while enhancing its solubility and dissolution rate. In this paper we have investigated pH-sensitive self-nanoemulsifying formulations containing silibinin as model drug. Pseudo-ternary phase diagrams have been constructed in order to identify the self-emulsification regions under different pH. Solubility of silibinin in selected formulations has been assessed and stability of the pure drug and of the silibinin loaded pH-SNEDDS formulations in simulated gastric fluid had been compared. Droplet size of the optimized pH-SNEDDS has been correlated to pH, volume of dilution medium and silibinin loading amount. TEM (transmission electron microscopy) studies have shown that emulsion droplets had spherical shape and narrow size distribution. In vitro drug release studies of the optimal pH-SNEDDS indicated substantial increase of the drug release and release rate in comparison to pure silibinin and to the commercial silibinin tablet. The results indicated that pH-SNEDDS have potential to improve the biopharmaceutics properties of acid-labile lipophilic drugs.
journal_name
Chem Phys Lipidsjournal_title
Chemistry and physics of lipidsauthors
Zhao T,Maniglio D,Chen J,Chen B,Migliaresi Cdoi
10.1016/j.chemphyslip.2016.02.008subject
Has Abstractpub_date
2016-03-01 00:00:00pages
81-8eissn
0009-3084issn
1873-2941pii
S0009-3084(16)30030-5journal_volume
196pub_type
杂志文章abstract：:A series of polyprenyl phosphates with modified structure of polyprenyl residue was prepared through phosphorylation of polyprenyl trichloroacetimidates with phosphoric acid. Interaction of polyprenols with tetra-n-butylammonium dihydrogen phosphate and trichloroacetonitrile was found to represent a very efficient, si...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(89)90006-6
更新日期：1989-11-01 00:00:00
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journal_title：Chemistry and physics of lipids
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doi：10.1016/s0009-3084(97)02664-9
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journal_title：Chemistry and physics of lipids
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doi：10.1016/j.chemphyslip.2005.03.006
更新日期：2005-07-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2007.05.005
更新日期：2007-09-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/s0009-3084(02)00195-0
更新日期：2003-04-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2008.03.001
更新日期：2008-06-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2010.11.007
更新日期：2011-02-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2005.07.007
更新日期：2005-12-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(75)90054-7
更新日期：1975-04-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2016.02.006
更新日期：2016-03-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(89)90047-9
更新日期：1989-10-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(78)90040-3
更新日期：1978-09-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2011.11.008
更新日期：2012-01-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(86)90116-7
更新日期：1986-03-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/s0009-3084(01)00130-x
更新日期：2001-05-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(85)90028-3
更新日期：1985-11-01 00:00:00
abstract：:Monolactone (NeuAc1-9NeuAc linkage) formation of a ganglioside, GD1b, was observed at 20 degrees C on solutions ranging in concentration from 0.008 to 1.7 mM and in pH from 2 to 8.1, by following the change of ellipicity at 235 nm, where lactonized gangliosides showed a strong Cotton effect. The lactonization was foun...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(94)90051-5
更新日期：1994-03-31 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2017.02.003
更新日期：2017-04-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2018.03.008
更新日期：2018-07-01 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章,评审
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更新日期：1986-12-15 00:00:00
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journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(88)90092-8
更新日期：1988-10-01 00:00:00
abstract：:Previously unknown 4,5-epoxy-N-acetyl-sphingosine (1) was synthesized by epoxidation of N-acetyl-sphingosine with 1,1-dimethyldioxirane. A by-product generated by HPLC purification is the tetrahydrofuryl derivative of acetamide (2). Mainly allylic oxidation was observed when natural ceramides were reacted with dimethy...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/s0009-3084(00)00208-5
更新日期：2001-02-01 00:00:00
abstract：:(Z)-tetracos-5-enoic acid and racemic cis-4-(2-octadecylcyclopropane-1-yl)-butanoic acid have been prepared from 1-eicosene by a new facile route. Periodic acid cleavage of the epoxide of 1-eicosene gave nonadecanal which was condensed with 4-carboxybutyltriphenylphosphonium bromide to give predominately (Z)-tetracos-...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/s0009-3084(03)00092-6
更新日期：2003-11-01 00:00:00
abstract：:A complex mixture of monoacylglycerols, identified as (C30--C36) corynomycoloylglycerols was isolated from the diethyl ether/acetone-soluble lipids of Corynebacterium pseudotuberculosis. ...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(79)90055-0
更新日期：1979-09-01 00:00:00
abstract：:This article reviews the use of fluorescent lipids and free probes in the studies of lipid regular distribution in model membranes. The first part of this article summarizes the evidence and physical properties for lipid regular distribution in pyrene-labeled phosphatidylcholine (PC)/unlabeled PC binary mixtures as re...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章,评审
doi：10.1016/s0009-3084(02)00025-7
更新日期：2002-06-01 00:00:00
abstract：:For the design of new synthetic substrates for the assay of pancreatic lipases activity, acyl dialkylglycerols of variable chain length were prepared. Titrimetric assay of these substrates showed the highest lipolytic activity of porcine pancreas lipase (pPL) with butanoyl dibutylglycerol. The activity is lower but co...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/s0009-3084(01)00143-8
更新日期：2001-06-01 00:00:00
abstract：:Low-temperature molecular mobility and packing in biological tissues are important for their survival upon cryopreservation. Electron paramagnetic resonance (EPR) in its pulsed version of electron spin echo (ESE) allows studying stochastic librations of spin-labeled molecules, the type of motion which dominates at low...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2019.104817
更新日期：2020-01-01 00:00:00
abstract：:Monitoring bile acids as signal molecules in combination with a bile acid synthesis marker and the FXR regulator fibroblast growth factor 19 (FGF19), this study addresses significant postprandial changes. The efficacy of the different pathways to regulate bile acid synthesis through short heterodimer partner (SHP) dep...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2011.05.003
更新日期：2011-09-01 00:00:00
abstract：:The apparent Mn2+ binding constant for L-alpha-dipalmitoylphosphatidylcholine (DPPC) bilayers dispersed in monovalent salt and MnCl2 dispersions was determined as a function temperature using electron paramagnetic resonance (ERP). Reproducibility in the data sets requires the use of a standard salt solution and dual c...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/0009-3084(88)90023-0
更新日期：1988-03-01 00:00:00
abstract：:In cell biology (and in many biophysical) studies there is a natural tendency to consider ceramide as a highly condensed, solid-type lipid conferring rigidity and close packing to biomembranes. In the present work we advanced the understanding of the phase behavior of palmitoyl-ceramide restricted to a planar interfac...
journal_title：Chemistry and physics of lipids
pub_type： 杂志文章
doi：10.1016/j.chemphyslip.2010.04.008
更新日期：2010-06-01 00:00:00
