Abstract：
:The purpose of this work was to develop a practical and scalable method to encapsulate the hydrophobic antibiotic thiostrepton (TST) in sterically stabilized micelles (SSM). Using the conventional method of thin-film hydration, we encapsulated up to 5 drug molecules per SSM (diameter ∼ 16 nm). However, since this method is not suitable for large-scale production - a limiting factor for clinical translation - we applied the co-solvent freeze-drying method using tert-butanol (TBA): water co-solvent system. We found that the presence of phosphate-buffered saline (PBS) salts in the lyophilized cake accelerated the reconstitution time and allowed efficient drug encapsulation without the formation of larger drug particles. In addition, TBA proportion of 50% (v/v) was sufficient to maintain both phospholipid and drug in solution prior to the freeze-drying. The increase of drug and phospholipid concentrations in the formulation extended the reconstitution time and led to drug precipitation. Therefore, to increase the strength of the formulation, we prepared lyophilized cakes with lower phospholipid content (5 mM) and reconstituted them in one-third of the fill volume. In conclusion, we found optimum conditions to prepare TST-SSM using the co-solvent freeze-drying method. This scalable production method can facilitate the further clinical development and industrial production of TST-SSM nanomedicine.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Esparza K,Onyuksel Hdoi
10.1016/j.ijpharm.2018.12.001subject
Has Abstractpub_date
2019-02-10 00:00:00pages
21-29eissn
0378-5173issn
1873-3476pii
S0378-5173(18)30893-7journal_volume
556pub_type
杂志文章abstract：:Primary objective of this investigation was to delineate the differential impact of efflux transporters P-glycoprotein (P-gp/Abcb1) and breast cancer resistance protein (Bcrp1/Abcg2) on brain disposition and plasma pharmacokinetics of pazopanib. In addition, this research investigated whether inhibition of these efflu...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.05.038
更新日期：2012-10-15 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.09.055
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journal_title：International journal of pharmaceutics
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doi：10.1016/j.ijpharm.2012.10.012
更新日期：2012-12-15 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.01.012
更新日期：2006-04-26 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00273-2
更新日期：1999-12-01 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.11.022
更新日期：2014-01-30 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.10.025
更新日期：2013-01-30 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.07.025
更新日期：2012-10-15 00:00:00
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pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.04.025
更新日期：2008-08-06 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.05.064
更新日期：2012-09-15 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2011-05-16 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2017-01-10 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.12.026
更新日期：2019-02-10 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00075-7
更新日期：1999-05-10 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.03.044
更新日期：2017-05-15 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.12.038
更新日期：2009-05-08 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.04.004
更新日期：2007-08-16 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.09.050
更新日期：2007-03-06 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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pub_type： 杂志文章
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更新日期：2012-02-14 00:00:00
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pub_type： 杂志文章
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更新日期：2018-10-05 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.06.013
更新日期：2010-08-30 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2020-03-15 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2020-06-30 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.12.042
更新日期：2018-02-15 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.10.035
更新日期：2013-01-30 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.03.049
更新日期：2013-06-05 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2018.12.090
更新日期：2019-03-10 00:00:00
abstract：:The immunostimulation capacity of most vaccines is enhanced through antigen adsorption on aluminum hydroxide (AH) adjuvants. Varying the adsorption conditions, i.e. pH and ionic strength (I), changes the antigen adsorbed amount and therefore the ability of the vaccine to stimulate the immune system. Vaccine formulatio...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.12.019
更新日期：2017-01-30 00:00:00
abstract：:The aim of this study was to develop a self-emulsifying drug delivery system (SEDDS) containing the glycopeptide antibiotic vancomycin (VAN) with improved intestinal mucosa permeating properties in order to increase oral drug absorption. VAN was effectively incorporated into SEDDS increasing the lipophilicity of the d...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.11.010
更新日期：2019-01-10 00:00:00
