Abstract:
:In our previously studies, we confirmed that ergosterol could ameliorate diabetic nephropathy by suppressing the proliferation of mesangial cells and the accumulation of extracellular matrix (ECM). However, the therapeutic application of ergosterol may be confined due to poor aqueous solubility and low oral bioavailability. We aim to prepare ergosterol-loaded nanostructured lipid carriers (ERG-NLCs) to enhance the solubility and oral bioavailability of ergosterol. ERG-NLCs were prepared using glyceryl monostearate and decanoyl/octanoyl-glycerides by hot emulsification-ultrasonication method and characterized by dynamic light scattering (DLS), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) analysis, entrapment efficiency (EE), and drug loading (DL) capacity studies. The prepared ERG-NLCs were spherical, with particle size of 81.39 nm and negative zeta potential of 30.77 mV. Ergosterol was successfully encapsulated in NLCs with a high EE of 92.95% and a DL capacity of 6.51%. In pharmacokinetic study, Cmax and AUC0-∞ of ergosterol in ERG-NLCs were obviously enhanced, and the relative oral bioavailability of ERG-NLCs was 277.56% higher than that of raw ergosterol. Moreover, the in vitro pharmacodynamic study indicated that ERG-NLCs inhibited high-glucose-stimulated mesangial cells over proliferation and ECM accumulation more effectively compared to raw ergosterol. In conclusion, the validated ERG-NLCs showed that NLCs mediated delivery could be used as potential vehicle to enhance solubility, oral bioavailability and therapeutic efficacy of ergosterol.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Dong Z,Iqbal S,Zhao Zdoi
10.1208/s12249-019-1597-3subject
Has Abstractpub_date
2020-01-13 00:00:00pages
64issue
2issn
1530-9932pii
10.1208/s12249-019-1597-3journal_volume
21pub_type
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journal_title:AAPS PharmSciTech
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journal_title:AAPS PharmSciTech
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journal_title:AAPS PharmSciTech
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journal_title:AAPS PharmSciTech
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journal_title:AAPS PharmSciTech
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journal_title:AAPS PharmSciTech
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
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更新日期:2007-12-14 00:00:00
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt0804119
更新日期:2007-12-28 00:00:00
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
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journal_title:AAPS PharmSciTech
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journal_title:AAPS PharmSciTech
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-013-9950-4
更新日期:2013-06-01 00:00:00
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-013-0050-2
更新日期:2014-02-01 00:00:00
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journal_title:AAPS PharmSciTech
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doi:10.1208/s12249-012-9773-8
更新日期:2012-06-01 00:00:00
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
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journal_title:AAPS PharmSciTech
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
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更新日期:2017-04-01 00:00:00
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journal_title:AAPS PharmSciTech
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更新日期:2018-04-01 00:00:00
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journal_title:AAPS PharmSciTech
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journal_title:AAPS PharmSciTech
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更新日期:2012-03-01 00:00:00
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journal_title:AAPS PharmSciTech
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt070129
更新日期:2006-03-24 00:00:00
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journal_title:AAPS PharmSciTech
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