کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2486333 | 1114381 | 2011 | 14 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Secretory phospholipase A2 responsive liposomes
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
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چکیده انگلیسی
Secretory phospholipase A2 (sPLA2) expression is increased in several cancers and has been shown to trigger release from some lipid carriers. This study used electrospray ionization mass spectrometry (ESIâMS) and release of 6âcarboxyfluorescein (6âCF) to determine the effects of sPLA2 on various liposome formulations. Different combinations of zwitterionic [1,2âdipalmitoylâsnâglyceroâ3âphosphatidylcholine, 1,2âdistearoylâsnâglyceroâ3âphosphatidylcholine, and 1,2â distearoylâsnâglyceroâ3âphosphatidylethanolamine (DSPE)] and anionic [1,2âdistearoylâsnâglyceroâ3âphosphatidic acid, 1,2âdistearoylâsnâglyceroâ3âphosphatidylglycerol (DSPG), 1,2âdistearoylâsnâglyceroâ3âphosphatidylserine, and 1,2âdistearoylâsnâglyceroâ3âphosphoethanolamine-Nâpoly(ethylene glycol) 2000 (DSPE-PEG)] phospholipids were examined. DSPG and DSPE were most susceptible to sPLA2âmediated degradation compared with other phospholipids. Increased 6âCF release was observed after inclusion of 10Â mol % DSPE and anionic lipids into different liposome formulations. Group IIa sPLA2âmediated 6âCF release was less than Group III and relatively insensitive to cholesterol (Chol), whereas Chol reduced sPLA2âmediated release. Inclusion of DSPE-PEG increased sPLA2âmediated 6âCF release, whereas serum reduced lipid degradation and 6âCF release significantly. These data demonstrate that ESIâMS and 6âCF release were useful in determining the selectivity of sPLA2 and release from liposomes, that differences in the activity of different sPLA2 isoforms exist, and that DSPE-PEG enhanced sPLA2âmediated release of liposomal constituents. These findings will aid in the selection of lipids and optimization of the kinetics of drug release for the treatment of cancers and diseases of inflammation in which sPLA2 expression is increased. © 2011 WileyâLiss, Inc. and the American Pharmacists Association J Pharm Sci 100:3146-3159, 2011
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 100, Issue 8, August 2011, Pages 3146-3159
Journal: Journal of Pharmaceutical Sciences - Volume 100, Issue 8, August 2011, Pages 3146-3159
نویسندگان
Guodong Zhu, Jason N. Mock, Ibrahim Aljuffali, Brian S. Cummings, Robert D. Arnold,