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<!doctype html> <html lang="ja"> <head> <title>Molecular-Mediated Difference Action of Poloxham124/188: Abs | 98568</title> <meta name="keywords" content="Xiaoying Lin, Xinxin Zhou, Feng Hao, Lele Li, Yue Cui, Yanfei Zhang, Jiao Guan, Heyun Zhu, Bo Feng, "/> <meta name="description" content="Poloxamers (PLs) are commonly used pharmaceutical excipients. According to the different molecular weight, mainly PL124 and PL188 are observed. PL188 with ..98568"/> <meta name="citation_publisher" content="ロングダム出版SL" /> <meta name="citation_journal_title" content="薬物代謝と毒性学ジャーナル"> <meta name="citation_title" content="Molecular-Mediated Difference Action of Poloxham124/188: Absorption, Efflux and Suborganelle Accumulation in Caco-2 Cells"> <meta name="citation_author" content="Xiaoying Lin" /> <meta name="citation_author" content="Xinxin Zhou" /> <meta name="citation_author" content="Feng Hao" /> <meta name="citation_author" content="Lele Li" /> <meta name="citation_author" content="Yue Cui" /> <meta name="citation_author" content="Yanfei Zhang" /> <meta name="citation_author" content="Jiao Guan" /> <meta name="citation_author" content="Heyun Zhu" /> <meta name="citation_author" content="Bo Feng" /> <meta name="citation_year" content=""> <meta name="citation_volume" content="14"> <meta name="citation_issue" content="1"> <meta name="citation_abstract" content="Poloxamers (PLs) are commonly used pharmaceutical excipients. According to the different molecular weight, mainly PL124 and PL188 are observed. PL188 with the larger weight, hydrophilic and more application in oral exposure drug delivery systems than PL124. However, the absorption and transport mechanisms of PL188 into intestinal epithelial cells are still unclear. In this study, we study the uptake and efflux of PL124/188 in Caco-2 cells, and subcellular accumulation in Caco-2 cells quantitatived by ultra-high-performance liquid chromatography-triple/time-of-flight mass spectrometry (UHPLC-Q-TOF/MS). The results showed that, the uptake in Caco-2 cells are different: Both PL188 and 124 entered Caco-2 cells through active transport, but PL188 uptake into Caco-2 cells relies on pinocytosis pathway, fosselin-mediated endocytosis pathway, and the endocytosis pathway independent of mestin and fosselin-mediated endocytosis. While PL124 uptake by independent of clathrin- and fossa-mediated endocytosis inhibitors pathway; The effects of PL188 on P-gp protein substrate were different: PL188 was stronger than PL124; There are also differences in subcellular accumulations: PL124 reaches the cell membrane at a slower rate compared to PL188, which rapidly enters the cytoplasm and nucleus, with a higher concentration in the cytoplasm. Both PL124 and PL188 remain in the skeleton. This work provides data basis for our subsequent application of PL188 and PL124 as oral preparations. 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According to the different molecular weight, mainly PL124 and PL188 are observed. PL188 with the larger weight, hydrophilic and more application in oral exposure drug delivery systems than PL124. However, the absorption and transport mechanisms of PL188 into intestinal epithelial cells are still unclear. In this study, we study the uptake and efflux of PL124/188 in Caco-2 cells, and subcellular accumulation in Caco-2 cells quantitatived by ultra-high-performance liquid chromatography-triple/time-of-flight mass spectrometry (UHPLC-Q-TOF/MS). The results showed that, the uptake in Caco-2 cells are different: Both PL188 and 124 entered Caco-2 cells through active transport, but PL188 uptake into Caco-2 cells relies on pinocytosis pathway, fosselin-mediated endocytosis pathway, and the endocytosis pathway independent of mestin and fosselin-mediated endocytosis. While PL124 uptake by independent of clathrin- and fossa-mediated endocytosis inhibitors pathway; The effects of PL188 on P-gp protein substrate were different: PL188 was stronger than PL124; There are also differences in subcellular accumulations: PL124 reaches the cell membrane at a slower rate compared to PL188, which rapidly enters the cytoplasm and nucleus, with a higher concentration in the cytoplasm. Both PL124 and PL188 remain in the skeleton. This work provides data basis for our subsequent application of PL188 and PL124 as oral preparations.</p> <div class="alert alert-info text-left"><b>免責事項:</b> この要約は人工知能ツールを使用して翻訳されたものであり、まだレビューまたは検証されていません。</div> <div class="nav social-icons"> <a class="nav-link w-auto">この記事をシェアする</a> <a title="ここをクリック" target="_blank" href="https://www.facebook.com/sharer.php?u=https://japanese.longdom.org/abstract/molecularmediated-difference-action-of-poloxham124188-absorption-efflux-and-suborganelle-accumulation-in-caco2-cells-98568.html" rel="noopener"><i class="fab fa-facebook-f"></i></a> <a class="nav-link" title="ここをクリック" target="_blank" href="https://twitter.com/share?url=https://japanese.longdom.org/abstract/molecularmediated-difference-action-of-poloxham124188-absorption-efflux-and-suborganelle-accumulation-in-caco2-cells-98568.html" rel="noopener"><i class="fab fa-twitter"></i></a> <a class="nav-link" title="ここをクリック" target="_blank" href="https://www.linkedin.com/shareArticle?mini=true&url=https://japanese.longdom.org/abstract/molecularmediated-difference-action-of-poloxham124188-absorption-efflux-and-suborganelle-accumulation-in-caco2-cells-98568.html" rel="noopener"><i class="fab fa-linkedin-in"></i></a> <a class="nav-link" title="ここをクリック" target="_blank" href="https://plus.google.com/share?url=https://japanese.longdom.org/abstract/molecularmediated-difference-action-of-poloxham124188-absorption-efflux-and-suborganelle-accumulation-in-caco2-cells-98568.html" rel="noopener"><i class="fab fa-google-plus-g"></i></a> </div> </div> </div> </div> </section> <footer class="bg-blue-grey-900 py-3"> <div class="container"> <div class="row"> <div class="col-12 col-sm-4"> <h4 class="white font-size-4 fweight-400 border-bottom-1 pb-2">コンテンツリンク</h4> <ul class="list-unstyled footer-links font-size-3"> <li><a class="" href="https://japanese.longdom.org/privacy-policy.html" title="ここをクリック">プライバシーポリシー</a></li> <li><a class="" href="https://japanese.longdom.org/terms-conditions.html" title="ここをクリック">利用規約</a></li> <li><a class="" href="https://japanese.longdom.org/authors-reviewers-editors.html" title="ここをクリック">著者、査読者、編集者</a></li> </ul> </div> <div class="col-12 col-sm-4"> <h4 class="white font-size-4 fweight-400 border-bottom-1 pb-2">ロングダムに連絡する</h4> <p><strong>ロングダムグループ SA</strong><br /> ロジェ・ヴァンデンドリッシュ通り、<br /> 18、1150 ブリュッセル、ベルギー<br /> 電話番号: +442038085340<br /> <strong>メール:</strong> <a class="white" href="mailto:info@longdom.org" title="ここをクリック">info@longdom.org</a></p> </div> <div class="col-12 col-sm-4"> <h4 class="white font-size-4 fweight-400 border-bottom-1 pb-2">接続</h4> <nav class="nav nav-pills social-icons-footer flex-column a-pl-0"> <a href="https://www.facebook.com/longdompublisher" title="ここをクリック" target="_blank" class="nav-link bg-facebook-hover"><i class="fab fa-facebook-f bg-facebook"></i></a> <a href="https://www.linkedin.com/company/longdom-publishing-sl/" title="ここをクリック" target="_blank" class="nav-link bg-linkedin-hover"><i class="fab fa-linkedin-in bg-linkedin"></i></a> <a href="https://twitter.com/LongdomP" title="ここをクリック" target="_blank" class="nav-link bg-twitter-hover"><i class="fab fa-twitter bg-twitter"></i></a> <a href="https://www.instagram.com/longdom_publisher/" title="ここをクリック" target="_blank" class="nav-link bg-instagram-hover"><i class="fab fa-instagram bg-instagram"></i></a> </nav> </div> </div> <div class="row text-center"> <div class="col"> <p>著作権 © 2024 <a href="https://japanese.longdom.org/" title="ここをクリック" class="white">ロングダム出版SL</a>.</p> </div> </div> </div> </footer>  <a href="#0" class="cd-top js-cd-top">Top</a>   <script src="https://code.jquery.com/jquery-3.3.1.min.js"></script> <script src="https://cdnjs.cloudflare.com/ajax/libs/popper.js/1.14.7/umd/popper.min.js"></script> <script src="https://stackpath.bootstrapcdn.com/bootstrap/4.3.1/js/bootstrap.min.js"></script>  <script> jQuery(function($) { $(window).scroll(function fix_element() { $('#target').css( $(window).scrollTop() > 100 ? 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