<?xml version="1.0" encoding="utf-8"?>
<TEI xmlns="http://www.tei-c.org/ns/1.0" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" xmlns:hal="http://hal.archives-ouvertes.fr/" xmlns:gml="http://www.opengis.net/gml/3.3/" xmlns:gmlce="http://www.opengis.net/gml/3.3/ce" version="1.1" xsi:schemaLocation="http://www.tei-c.org/ns/1.0 http://api.archives-ouvertes.fr/documents/aofr-sword.xsd">
  <teiHeader>
    <fileDesc>
      <titleStmt>
        <title>HAL TEI export of hal-03117366</title>
      </titleStmt>
      <publicationStmt>
        <distributor>CCSD</distributor>
        <availability status="restricted">
          <licence target="https://creativecommons.org/publicdomain/zero/1.0/">CC0 1.0 - Universal</licence>
        </availability>
        <date when="2026-05-16T05:16:36+02:00"/>
      </publicationStmt>
      <sourceDesc>
        <p part="N">HAL API Platform</p>
      </sourceDesc>
    </fileDesc>
  </teiHeader>
  <text>
    <body>
      <listBibl>
        <biblFull>
          <titleStmt>
            <title xml:lang="en">Enhanced Antisense Oligonucleotide Delivery Using Cationic Liposomes Grafted with Trastuzumab: A Proof-of-Concept Study in Prostate Cancer</title>
            <author role="aut">
              <persName>
                <forename type="first">Guillaume</forename>
                <surname>Sicard</surname>
              </persName>
              <idno type="halauthorid">584638-0</idno>
              <affiliation ref="#struct-179570"/>
            </author>
            <author role="aut">
              <persName>
                <forename type="first">Clément</forename>
                <surname>Paris</surname>
              </persName>
              <idno type="halauthorid">54853-0</idno>
              <affiliation ref="#struct-179570"/>
            </author>
            <author role="aut">
              <persName>
                <forename type="first">Sarah</forename>
                <surname>Giacometti</surname>
              </persName>
              <idno type="halauthorid">1077810-0</idno>
              <affiliation ref="#struct-179570"/>
            </author>
            <author role="aut">
              <persName>
                <forename type="first">Anne</forename>
                <surname>Rodallec</surname>
              </persName>
              <email type="md5">296e6d1ad58c9cdd0ee9efbf0fb1ffcb</email>
              <email type="domain">univ-amu.fr</email>
              <idno type="idhal" notation="string">anne-rodallec</idno>
              <idno type="idhal" notation="numeric">751465</idno>
              <idno type="halauthorid" notation="string">40682-751465</idno>
              <idno type="ORCID">https://orcid.org/0000-0002-0787-8241</idno>
              <affiliation ref="#struct-179570"/>
            </author>
            <author role="aut">
              <persName>
                <forename type="first">Joseph</forename>
                <surname>Ciccolini</surname>
              </persName>
              <email type="md5">3714cb9f0d63a327527e73a74ca9ec63</email>
              <email type="domain">univmed.fr</email>
              <idno type="idhal" notation="numeric">1211831</idno>
              <idno type="halauthorid" notation="string">518104-1211831</idno>
              <idno type="ORCID">https://orcid.org/0000-0003-1733-3410</idno>
              <idno type="IDREF">https://www.idref.fr/060250402</idno>
              <idno type="VIAF">https://viaf.org/viaf/190557753</idno>
              <idno type="ISNI">http://isni.org/isni/0000000138750155</idno>
              <idno type="GOOGLE SCHOLAR">https://scholar.google.fr/citations?user=1ww58o0AAAAJ</idno>
              <affiliation ref="#struct-179570"/>
            </author>
            <author role="aut">
              <persName>
                <forename type="first">Palma</forename>
                <surname>Rocchi</surname>
              </persName>
              <email type="md5">20dd4d48847853fbdfed3d0eb972449d</email>
              <email type="domain">inserm.fr</email>
              <idno type="idhal" notation="string">palma-rocchi</idno>
              <idno type="idhal" notation="numeric">8380</idno>
              <idno type="halauthorid" notation="string">24180-8380</idno>
              <idno type="ORCID">https://orcid.org/0000-0002-4383-4684</idno>
              <idno type="IDREF">https://www.idref.fr/067276644</idno>
              <affiliation ref="#struct-179570"/>
            </author>
            <author role="aut">
              <persName>
                <forename type="first">Raphaëlle</forename>
                <surname>Fanciullino</surname>
              </persName>
              <email type="md5">7c11f7a6e9cfe09448549b3206173c31</email>
              <email type="domain">univ-amu.fr</email>
              <idno type="idhal" notation="string">raphaelle-fanciullino</idno>
              <idno type="idhal" notation="numeric">751464</idno>
              <idno type="halauthorid" notation="string">48998-751464</idno>
              <idno type="ORCID">https://orcid.org/0000-0001-6750-4658</idno>
              <idno type="IDREF">https://www.idref.fr/10300369X</idno>
              <idno type="VIAF">https://viaf.org/viaf/212011421</idno>
              <idno type="ISNI">http://isni.org/isni/0000000358679370</idno>
              <affiliation ref="#struct-179570"/>
            </author>
            <editor role="depositor">
              <persName>
                <forename>Palma</forename>
                <surname>Rocchi</surname>
              </persName>
              <email type="md5">20dd4d48847853fbdfed3d0eb972449d</email>
              <email type="domain">inserm.fr</email>
            </editor>
          </titleStmt>
          <editionStmt>
            <edition n="v1" type="current">
              <date type="whenSubmitted">2023-07-17 09:23:45</date>
              <date type="whenModified">2024-10-09 09:52:02</date>
              <date type="whenReleased">2023-07-17 09:38:52</date>
              <date type="whenProduced">2020-12</date>
              <date type="whenEndEmbargoed">2023-07-17</date>
              <ref type="file" target="https://hal.science/hal-03117366v1/document">
                <date notBefore="2023-07-17"/>
              </ref>
              <ref type="file" subtype="greenPublisher" n="1" target="https://hal.science/hal-03117366v1/file/pharmaceutics-12-01166.pdf" id="file-4162951-3625132">
                <date notBefore="2023-07-17"/>
              </ref>
              <ref type="externalLink" target="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7761013"/>
            </edition>
            <respStmt>
              <resp>contributor</resp>
              <name key="339229">
                <persName>
                  <forename>Palma</forename>
                  <surname>Rocchi</surname>
                </persName>
                <email type="md5">20dd4d48847853fbdfed3d0eb972449d</email>
                <email type="domain">inserm.fr</email>
              </name>
            </respStmt>
          </editionStmt>
          <publicationStmt>
            <distributor>CCSD</distributor>
            <idno type="halId">hal-03117366</idno>
            <idno type="halUri">https://hal.science/hal-03117366</idno>
            <idno type="halBibtex">sicard:hal-03117366</idno>
            <idno type="halRefHtml">&lt;i&gt;Pharmaceutics&lt;/i&gt;, 2020, 12 (12), pp.1166. &lt;a target="_blank" href="https://dx.doi.org/10.3390/pharmaceutics12121166"&gt;&amp;#x27E8;10.3390/pharmaceutics12121166&amp;#x27E9;&lt;/a&gt;</idno>
            <idno type="halRef">Pharmaceutics, 2020, 12 (12), pp.1166. &amp;#x27E8;10.3390/pharmaceutics12121166&amp;#x27E9;</idno>
            <availability status="restricted">
              <licence target="https://creativecommons.org/licenses/by/4.0/">CC BY 4.0 - Attribution<ref corresp="#file-4162951-3625132"/></licence>
            </availability>
          </publicationStmt>
          <seriesStmt>
            <idno type="stamp" n="INSERM">INSERM - Institut national de la santé et de la recherche médicale</idno>
            <idno type="stamp" n="CNRS">CNRS - Centre national de la recherche scientifique</idno>
            <idno type="stamp" n="UNIV-AMU">Aix Marseille Université</idno>
            <idno type="stamp" n="CRCM">Centre de Recherche en Cancérologie de Marseille</idno>
            <idno type="stamp" n="TEST-HALCNRS">Collection test HAL CNRS</idno>
          </seriesStmt>
          <notesStmt>
            <note type="audience" n="2">International</note>
            <note type="popular" n="0">No</note>
            <note type="peer" n="1">Yes</note>
          </notesStmt>
          <sourceDesc>
            <biblStruct>
              <analytic>
                <title xml:lang="en">Enhanced Antisense Oligonucleotide Delivery Using Cationic Liposomes Grafted with Trastuzumab: A Proof-of-Concept Study in Prostate Cancer</title>
                <author role="aut">
                  <persName>
                    <forename type="first">Guillaume</forename>
                    <surname>Sicard</surname>
                  </persName>
                  <idno type="halauthorid">584638-0</idno>
                  <affiliation ref="#struct-179570"/>
                </author>
                <author role="aut">
                  <persName>
                    <forename type="first">Clément</forename>
                    <surname>Paris</surname>
                  </persName>
                  <idno type="halauthorid">54853-0</idno>
                  <affiliation ref="#struct-179570"/>
                </author>
                <author role="aut">
                  <persName>
                    <forename type="first">Sarah</forename>
                    <surname>Giacometti</surname>
                  </persName>
                  <idno type="halauthorid">1077810-0</idno>
                  <affiliation ref="#struct-179570"/>
                </author>
                <author role="aut">
                  <persName>
                    <forename type="first">Anne</forename>
                    <surname>Rodallec</surname>
                  </persName>
                  <email type="md5">296e6d1ad58c9cdd0ee9efbf0fb1ffcb</email>
                  <email type="domain">univ-amu.fr</email>
                  <idno type="idhal" notation="string">anne-rodallec</idno>
                  <idno type="idhal" notation="numeric">751465</idno>
                  <idno type="halauthorid" notation="string">40682-751465</idno>
                  <idno type="ORCID">https://orcid.org/0000-0002-0787-8241</idno>
                  <affiliation ref="#struct-179570"/>
                </author>
                <author role="aut">
                  <persName>
                    <forename type="first">Joseph</forename>
                    <surname>Ciccolini</surname>
                  </persName>
                  <email type="md5">3714cb9f0d63a327527e73a74ca9ec63</email>
                  <email type="domain">univmed.fr</email>
                  <idno type="idhal" notation="numeric">1211831</idno>
                  <idno type="halauthorid" notation="string">518104-1211831</idno>
                  <idno type="ORCID">https://orcid.org/0000-0003-1733-3410</idno>
                  <idno type="IDREF">https://www.idref.fr/060250402</idno>
                  <idno type="VIAF">https://viaf.org/viaf/190557753</idno>
                  <idno type="ISNI">http://isni.org/isni/0000000138750155</idno>
                  <idno type="GOOGLE SCHOLAR">https://scholar.google.fr/citations?user=1ww58o0AAAAJ</idno>
                  <affiliation ref="#struct-179570"/>
                </author>
                <author role="aut">
                  <persName>
                    <forename type="first">Palma</forename>
                    <surname>Rocchi</surname>
                  </persName>
                  <email type="md5">20dd4d48847853fbdfed3d0eb972449d</email>
                  <email type="domain">inserm.fr</email>
                  <idno type="idhal" notation="string">palma-rocchi</idno>
                  <idno type="idhal" notation="numeric">8380</idno>
                  <idno type="halauthorid" notation="string">24180-8380</idno>
                  <idno type="ORCID">https://orcid.org/0000-0002-4383-4684</idno>
                  <idno type="IDREF">https://www.idref.fr/067276644</idno>
                  <affiliation ref="#struct-179570"/>
                </author>
                <author role="aut">
                  <persName>
                    <forename type="first">Raphaëlle</forename>
                    <surname>Fanciullino</surname>
                  </persName>
                  <email type="md5">7c11f7a6e9cfe09448549b3206173c31</email>
                  <email type="domain">univ-amu.fr</email>
                  <idno type="idhal" notation="string">raphaelle-fanciullino</idno>
                  <idno type="idhal" notation="numeric">751464</idno>
                  <idno type="halauthorid" notation="string">48998-751464</idno>
                  <idno type="ORCID">https://orcid.org/0000-0001-6750-4658</idno>
                  <idno type="IDREF">https://www.idref.fr/10300369X</idno>
                  <idno type="VIAF">https://viaf.org/viaf/212011421</idno>
                  <idno type="ISNI">http://isni.org/isni/0000000358679370</idno>
                  <affiliation ref="#struct-179570"/>
                </author>
              </analytic>
              <monogr>
                <idno type="halJournalId" status="VALID">129631</idno>
                <idno type="issn">1999-4923</idno>
                <title level="j">Pharmaceutics</title>
                <imprint>
                  <publisher>MDPI</publisher>
                  <biblScope unit="volume">12</biblScope>
                  <biblScope unit="issue">12</biblScope>
                  <biblScope unit="pp">1166</biblScope>
                  <date type="datePub">2020-12</date>
                </imprint>
              </monogr>
              <idno type="doi">10.3390/pharmaceutics12121166</idno>
              <idno type="pubmed">33260460</idno>
              <idno type="pubmedcentral">PMC7761013</idno>
            </biblStruct>
          </sourceDesc>
          <profileDesc>
            <langUsage>
              <language ident="en">English</language>
            </langUsage>
            <textClass>
              <keywords scheme="author">
                <term xml:lang="en">antisense oligonucleotides</term>
                <term xml:lang="en">immunoliposomes</term>
                <term xml:lang="en">liposomes</term>
                <term xml:lang="en">prostate cancer</term>
              </keywords>
              <classCode scheme="halDomain" n="chim">Chemical Sciences</classCode>
              <classCode scheme="halTypology" n="ART">Journal articles</classCode>
              <classCode scheme="halOldTypology" n="ART">Journal articles</classCode>
              <classCode scheme="halTreeTypology" n="ART">Journal articles</classCode>
            </textClass>
            <abstract xml:lang="en">
              <p>Prostate cancer (PCa) is the second most common cancer in men worldwide and the fifth leading cause of death by cancer. The overexpression of TCTP protein plays an important role in castration resistance. Over the last decade, antisense technology has emerged as a rising strategy in oncology. Using antisense oligonucleotide (ASO) to silence TCTP protein is a promising therapeutic option-however, the pharmacokinetics of ASO does not always meet the requirements of proper delivery to the tumor site. In this context, developing drug delivery systems is an attractive strategy for improving the efficacy of ASO directed against TCTP. The liposome should protect and deliver ASO at the intracellular level in order to be effective. In addition, because prostate cancer cells express Her2, using an anti-Her2 targeting antibody will increase the affinity of the liposome for the cell and optimize the intratumoral penetration of the ASO, thus improving efficacy. Here, we have designed and developed pegylated liposomes and Her2-targeting immunoliposomes. Mean diameter was below 200 nm, thus ensuring proper enhanced permeation and retention (EPR) effect. Encapsulation rate for ASO was about 40%. Using human PC-3 prostate cancer cells as a canonical model, free ASO and ASO encapsulated into either liposomes or anti-Her2 immunoliposomes were tested for efficacy in vitro using 2D and 3D spheroid models. While the encapsulated forms of ASO were always more effective than free ASO, we observed differences in efficacy of encapsulated ASO. For short exposure times (i.e., 4 h) ASO liposomes (ASO-Li) were more effective than ASO-immunoliposomes (ASO-iLi). Conversely, for longer exposure times, ASO-iLi performed better than ASO-Li. This pilot study demonstrates that it is possible to encapsulate ASO into liposomes and to yield antiproliferative efficacy against PCa. Importantly, despite mild Her2 expression in this PC-3 model, using a surface mAb as targeting agent provides further efficacy, especially when exposure is longer. Overall, the development of third-generation ASO-iLi should help to take advantage of the expression of Her2 by prostate cancer cells in order to allow greater specificity of action in vivo and thus a gain in efficacy.</p>
            </abstract>
          </profileDesc>
        </biblFull>
      </listBibl>
    </body>
    <back>
      <listOrg type="structures">
        <org type="laboratory" xml:id="struct-179570" status="VALID">
          <idno type="RNSR">201220152G</idno>
          <idno type="ROR">0494jpz02</idno>
          <orgName>Centre de Recherche en Cancérologie de Marseille</orgName>
          <orgName type="acronym">CRCM</orgName>
          <date type="start">2012</date>
          <desc>
            <address>
              <addrLine>27 bd Leï Roure, BP 30005913273 Marseille Cedex 09</addrLine>
              <country key="FR"/>
            </address>
            <ref type="url">http://crcm.marseille.inserm.fr/spip.php?article314</ref>
          </desc>
          <listRelation>
            <relation name="UM105" active="#struct-198056" type="direct"/>
            <relation name="UMR7258" active="#struct-301325" type="direct"/>
            <relation active="#struct-301051" type="indirect"/>
            <relation name="U1068" active="#struct-303623" type="direct"/>
            <relation name="UMR7258" active="#struct-441569" type="direct"/>
          </listRelation>
        </org>
        <org type="institution" xml:id="struct-198056" status="VALID">
          <idno type="IdRef">15863621X</idno>
          <idno type="ISNI">0000 0001 2176 4817</idno>
          <idno type="ROR">https://ror.org/035xkbk20</idno>
          <orgName>Aix Marseille Université</orgName>
          <orgName type="acronym">AMU</orgName>
          <date type="start">2012-01-01</date>
          <desc>
            <address>
              <addrLine>Aix-Marseille UniversitéJardins du Pharo58 Boulevard Charles Livon13284 Marseille cedex 7</addrLine>
              <country key="FR"/>
            </address>
            <ref type="url">http://www.univ-amu.fr/</ref>
          </desc>
        </org>
        <org type="institution" xml:id="struct-301325" status="VALID">
          <idno type="ROR">https://ror.org/04s3t1g37</idno>
          <orgName>Institut Paoli-Calmettes</orgName>
          <orgName type="acronym">IPC</orgName>
          <desc>
            <address>
              <addrLine>232 Boulevard de Sainte-Marguerite13009 Marseille</addrLine>
              <country key="FR"/>
            </address>
            <ref type="url">https://www.institutpaolicalmettes.fr/</ref>
          </desc>
          <listRelation>
            <relation active="#struct-301051" type="direct"/>
          </listRelation>
        </org>
        <org type="regroupinstitution" xml:id="struct-301051" status="VALID">
          <orgName>Fédération nationale des Centres de lutte contre le Cancer (FNCLCC)</orgName>
          <desc>
            <address>
              <country key="FR"/>
            </address>
          </desc>
        </org>
        <org type="institution" xml:id="struct-303623" status="VALID">
          <idno type="IdRef">026388278</idno>
          <idno type="ROR">https://ror.org/02vjkv261</idno>
          <orgName>Institut National de la Santé et de la Recherche Médicale</orgName>
          <orgName type="acronym">INSERM</orgName>
          <desc>
            <address>
              <addrLine>101, rue de Tolbiac, 75013 Paris</addrLine>
              <country key="FR"/>
            </address>
            <ref type="url">http://www.inserm.fr</ref>
          </desc>
        </org>
        <org type="regroupinstitution" xml:id="struct-441569" status="VALID">
          <idno type="IdRef">02636817X</idno>
          <idno type="ISNI">0000000122597504</idno>
          <idno type="ROR">https://ror.org/02feahw73</idno>
          <orgName>Centre National de la Recherche Scientifique</orgName>
          <orgName type="acronym">CNRS</orgName>
          <date type="start">1939-10-19</date>
          <desc>
            <address>
              <country key="FR"/>
            </address>
            <ref type="url">https://www.cnrs.fr/</ref>
          </desc>
        </org>
      </listOrg>
    </back>
  </text>
</TEI>