{"id":7522,"date":"2020-12-01T17:47:12","date_gmt":"2020-12-01T20:47:12","guid":{"rendered":"https:\/\/cendhy.cl\/?post_type=project&#038;p=7522"},"modified":"2020-12-01T17:47:22","modified_gmt":"2020-12-01T20:47:22","slug":"poloxamer-188-coated-ammonium-methacrylate-copolymer-nanocarriers-enhance-loperamide-permeability-across-pgp-expressing-epithelia","status":"publish","type":"project","link":"https:\/\/cendhy.cl\/en\/project\/poloxamer-188-coated-ammonium-methacrylate-copolymer-nanocarriers-enhance-loperamide-permeability-across-pgp-expressing-epithelia\/","title":{"rendered":"Poloxamer 188-Coated Ammonium Methacrylate Copolymer Nanocarriers Enhance Loperamide Permeability across Pgp-Expressing Epithelia"},"content":{"rendered":"<p>[et_pb_section fb_built=&#8221;1&#8243; _builder_version=&#8221;4.4.7&#8243; custom_padding=&#8221;0px||||false|false&#8221;][et_pb_row _builder_version=&#8221;4.4.7&#8243;][et_pb_column type=&#8221;4_4&#8243; _builder_version=&#8221;4.4.7&#8243;][et_pb_text _builder_version=&#8221;4.7.4&#8243; hover_enabled=&#8221;0&#8243; sticky_enabled=&#8221;0&#8243;]<\/p>\n<p><strong>Autores:\u00a0<\/strong><span><span class=\"hlFld-ContribAuthor\">Johanna Catalan-Figueroa,\u00a0<\/span><\/span><span><span class=\"hlFld-ContribAuthor\">Mauricio A. Garc\u00eda,\u00a0<\/span><\/span><span><span class=\"hlFld-ContribAuthor\">Pilar Contreras,\u00a0<\/span><\/span><span><span class=\"hlFld-ContribAuthor\">Constanza B. Boisset,\u00a0<\/span><\/span><span><span class=\"hlFld-ContribAuthor\">Pablo M. Gonzalez,\u00a0<\/span><\/span>Jenny L. Fiedler, Mariela F. P\u00e9rez, Javier O. Morales.<\/p>\n<p>[\/et_pb_text][et_pb_text _builder_version=&#8221;4.7.4&#8243; hover_enabled=&#8221;0&#8243; sticky_enabled=&#8221;0&#8243;]<\/p>\n<p class=\"p1\"><span>Loperamida es un agonista \u03bc-opioide con baja absorci\u00f3n gastrointestinal, principalmente por su modesta solubilidad acuosa y por ser un sustrato de eflujo de P-glicoproteina (Pgp). A\u00fan as\u00ed, estudios sobre efectos terap\u00e9uticos sugieren fuertemente que loperamida tiene potenciales ventajas farmacol\u00f3gicas sobre agonistas \u03bc-opioides tradicionales com\u00fanmente utilizados para analgesia.\u00a0 <\/span><\/p>\n<p class=\"p1\"><span>Entonces, en este art\u00edculo, evaluamos en l\u00edneas celulares MDCK-hMDR1 los efectos sobre el consumo de loperamida y radio de eflujo, al ser cargada en nanotransportadores Eudragit RS (ERS) cubiertos con poloxamer 188 (P188). Se escogieron ERS ya que potencia la dispersabilidad acuosa de loperamida y P188 como un potencial modulador negativo de Pgp modulator. En ensayos de consumo, se observ\u00f3 que Pgp limita la acumulaci\u00f3n de loperamida dentro de las c\u00e9lulas y que la preincubaci\u00f3n con P188, pero no la coincubaci\u00f3n, conduce a un incremento en el consumo de loperamida a un nivel similar a la inhibici\u00f3n farmacol\u00f3gica de Pgp. <\/span><\/p>\n<p class=\"p1\"><span>Por otra parte, el radio de eflujo no se ve alterado cuando se inhibe farmacol\u00f3gicamente a Pgp, mientras que los nanotransportadores ERS\/P188 potencian efectivamente el consumo de loperamida y el transporte transepitelial. Esto sugiere que el transporte de loperamida a trav\u00e9s de las c\u00e9lulas es influenciado significativamente por la presencia de la capa de agua sin agitar, que podr\u00eda obstaculizar la visualizaci\u00f3n de los efectos del eflujo de Pgp durante los ensayos de transporte.<\/span><\/p>\n<p class=\"p1\"><span>Los resultados en este trabajo dstacan que la formulaci\u00f3n de loperamida en estos nanotransportadores potencia su consumo y permeabilidad de transporte.<\/span><\/p>\n<p>[\/et_pb_text][et_pb_divider _builder_version=&#8221;4.4.7&#8243; width=&#8221;30%&#8221; custom_margin=&#8221;30px||0px||false|false&#8221;][\/et_pb_divider][et_pb_text _builder_version=&#8221;4.7.4&#8243; hover_enabled=&#8221;0&#8243; sticky_enabled=&#8221;0&#8243;]<\/p>\n<p><a href=\"https:\/\/doi.org\/10.1021\/acs.molpharmaceut.0c00623\">DOI: https:\/\/doi.org\/10.1021\/acs.molpharmaceut.0c00623<\/a><\/p>\n<p>[\/et_pb_text][\/et_pb_column][\/et_pb_row][\/et_pb_section]<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Autores:\u00a0Johanna Catalan-Figueroa,\u00a0Mauricio A. Garc\u00eda,\u00a0Pilar Contreras,\u00a0Constanza B. Boisset,\u00a0Pablo M. Gonzalez,\u00a0Jenny L. Fiedler, Mariela F. P\u00e9rez, Javier O. Morales. Loperamida es un agonista \u03bc-opioide con baja absorci\u00f3n gastrointestinal, principalmente por su modesta [&hellip;]<\/p>\n","protected":false},"author":2,"featured_media":7523,"comment_status":"open","ping_status":"closed","template":"","meta":{"_et_pb_use_builder":"on","_et_pb_old_content":"","_et_gb_content_width":"","footnotes":""},"project_category":[33,32],"project_tag":[],"class_list":["post-7522","project","type-project","status-publish","has-post-thumbnail","hentry","project_category-2020-en","project_category-publications"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v27.4 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>Poloxamer 188-Coated Ammonium Methacrylate Copolymer Nanocarriers Enhance Loperamide Permeability across Pgp-Expressing Epithelia - Cendhy, centro de nuevos f\u00e1rmacos para hipertensi\u00f3n e insuficiencia card\u00edaca<\/title>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/cendhy.cl\/en\/project\/poloxamer-188-coated-ammonium-methacrylate-copolymer-nanocarriers-enhance-loperamide-permeability-across-pgp-expressing-epithelia\/\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Poloxamer 188-Coated Ammonium Methacrylate Copolymer Nanocarriers Enhance Loperamide Permeability across Pgp-Expressing Epithelia - Cendhy, centro de nuevos f\u00e1rmacos para hipertensi\u00f3n e insuficiencia card\u00edaca\" \/>\n<meta property=\"og:description\" content=\"Autores:\u00a0Johanna Catalan-Figueroa,\u00a0Mauricio A. 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