Preactivated thiomers: permeation enhancing properties.
Preactivated thiomers: permeation enhancing properties.
复制标题
预活化硫聚物：渗透增强特性
DOI：
10.1016/j.ijpharm.2012.08.045
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发表时间：
2012-11-15
影响因子：
5.8
通讯作者：
Bernkop-Schnuerch, Andreas
中科院分区：
文献类型：
--
作者：
Wang, Xueqing;Iqbal, Javed;Rahmat, Deni;Bernkop-Schnuerch, Andreas
本研究旨在制备一系列聚丙烯酸-半胱氨酸-2-巯基烟酸缀合物（预活化硫代聚合物），并评价分子量或2-巯基烟酸（2 MNA）预活化程度对其渗透增强性能的影响。合成了具有不同分子量和不同预活化程度的预活化的硫代聚物，并基于它们的分子量和预活化程度将其分类为PAA 100-Cys-2 MNA（h）、PAA 250-Cys-2 MNA（h）、PAA 450-Cys-2 MNA（h）、PAA 450-Cys-2 MNA（m）和PAA 450-Cys-2 MNA（l）。在体外透皮实验中，预活化硫代聚物对Caco-2细胞单层和大鼠肠粘膜的促渗能力均为PAA 450-Cys-2 MNA（h）> PAA 250-Cys-2 MNA（h）> PAA 100-Cys-2 MNA（h）。在Caco-2细胞上，PAA 450-Cys-2 MNA（h）> PAA 450-Cys-2 MNA（m）> PAA 450-Cys-2 MNA（l）;在肠粘膜上，PAA 450-Cys-2 MNA（m）> PAA 450-Cys-2 MNA（h）> PAA 450-Cys-2 MNA（l）。与仅缓冲液中的荧光素钠相比，PAA 450-Cys-2 MNA（h）在Caco-2细胞单层上的荧光素钠Papp提高了5.08倍，PAA 450-Cys-2 MNA（m）在肠粘膜上的荧光素钠Papp提高了2.46倍。这些结果表明，预活化的硫代聚物可以被认为是一个有前途的大分子渗透促进聚合物的非侵入性给药。
The study was aimed to prepare a series of poly(acrylic acid)-cysteine-2-mercaptonicotinic acid conjugates (preactivated thiomers) and to evaluate the influence of molecular mass or degree of preactivation with 2-mercaptonicotinic acid (2MNA) on their permeation enhancing properties. Preactivated thiomers with different molecular mass and different degree of preactivation were synthesized and categorized on the basis of their molecular mass and degree of preactivation as PAA100-Cys-2MNA (h), PAA250-Cys-2MNA (h), PAA450-Cys-2MNA (h), PAA450-Cys-2MNA (m) and PAA450-Cys-2MNA (l). In vitro permeation studies, the permeation enhancement ability for preactivated thiomers was ranked as PAA450-Cys-2MNA (h) > PAA250-Cys-2MNA (h) > PAA100-Cys-2MNA (h) on both Caco-2 cell monolayers and rat intestinal mucosa. Comparing the influence of degree of preactivation with 2MNA on permeation enhancement, the following order PAA450-Cys-2MNA (h) > PAA450-Cys-2MNA (m) ≈ PAA450-Cys-2MNA (l) on Caco-2 cell monolayers and PAA450-Cys-2MNA (m) > PAA450-Cys-2MNA (h) > PAA450-Cys-2MNA (l) on intestinal mucosa was observed. The Papp of sodium fluorescein was 5.08-fold improved on Caco-2 cell monolayers for PAA450-Cys-2MNA (h) and 2.46-fold improved on intestinal mucosa for PAA450-Cys-2MNA (m), respectively, in comparison to sodium fluorescein in buffer only. These results indicated that preactivated thiomers could be considered as a promising macromolecular permeation enhancing polymer for non-invasive drug administration.
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影响因子：
5.8
作者：
Bernkop-Schnürch, A;Steininger, S
通讯作者：
Steininger, S
影响因子：
14
作者：
Kast, CE;Bernkop-Schnürch, A
通讯作者：
Bernkop-Schnürch, A
影响因子：
4.6
作者：
Meaney, C;O'Driscoll, C
通讯作者：
O'Driscoll, C
DOI：
10.1016/j.ejpb.2009.03.008
发表时间：
2009-08-01
影响因子：
4.9
作者：
Greindl, Melanie;Foeger, Florian;Bernkop-Schnuerch, Andreas
通讯作者：
Bernkop-Schnuerch, Andreas
影响因子：
4.6
作者：
Leitner, VM;Marschütz, MK;Bernkop-Schnürch, A
通讯作者：
Bernkop-Schnürch, A