Exploring Orodispersible Films Containing the Proteolysis Targeting Chimera ARV-110 in Hot Melt Extrusion and Solvent Casting Using Polyvinyl Alcohol
Background/Objectives: This project aims to provide valuable insights into the formulation of orodispersible films (ODFs) for the delivery of PROTAC ARV-110. The primary objective of this drug delivery formulation is to enhance the solubility of PROTAC ARV-110, which faces significant challenges due...
Gespeichert in:
| Veröffentlicht in: | Pharmaceutics 2024-11, Vol.16 (12), p.1499 |
|---|---|
| Hauptverfasser: | , , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | |
|---|---|
| container_issue | 12 |
| container_start_page | 1499 |
| container_title | Pharmaceutics |
| container_volume | 16 |
| creator | Meloni, Valentina Halstenberg, Laura Mareczek, Lena Lu, Jankin Liang, Bonnie Gottschalk, Nadine Mueller, Lena K. |
| description | Background/Objectives: This project aims to provide valuable insights into the formulation of orodispersible films (ODFs) for the delivery of PROTAC ARV-110. The primary objective of this drug delivery formulation is to enhance the solubility of PROTAC ARV-110, which faces significant challenges due to the low solubility of this active pharmaceutical ingredient, as it belongs to a molecular class that is considered to exceed the “Rule of Five”. Methods: We employed the concept of developing a rapidly disintegrating ODF to enhance the solubility of PROTAC ARV-110, utilizing polyvinyl alcohol as the polymer of choice. Given the high thermal stability of ARV-110, the PROTAC was subjected to two primary ODF manufacturing techniques: Hot melt extrusion (HME) and solvent casting. To establish the HME method, pre-screening through vacuum compression molding was performed. The films were characterized based on their disintegration in artificial saliva, drug release in a physiological environment, and mechanical strength. Results: All formulations demonstrated enhanced solubility of ARV-110, achieving exceptional results in terms of disintegration times and resistance to applied stress. Conclusions: The findings from the experiments outlined herein establish a solid foundation for the successful production of orodispersible films for the delivery of PROTACs. |
| doi_str_mv | 10.3390/pharmaceutics16121499 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_doaj_</sourceid><recordid>TN_cdi_proquest_journals_3149749974</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><doaj_id>oai_doaj_org_article_62147911434847e08f9d6e432ea22644</doaj_id><sourcerecordid>3149749974</sourcerecordid><originalsourceid>FETCH-LOGICAL-c1879-7b6f8ef1b48c26a67eec78bdcfe5d065d126d092209efebf4997e1d01a47aeac3</originalsourceid><addsrcrecordid>eNptUdtq3DAQNaWBhjSfUBDk2a1kaSXrcTGbJpCSkEtfhSyNd7VoJVfShuyH5H9rZ0PpQ-ZhZpjLmeGcqvpG8HdKJf4xbnTaaQP74kwmnDSESfmpOiVSyprJhn7-L_9Snee8xZNRSloqT6vX1cvoY3JhjW5TtC6PkLLrPaBL53cZdTEU7cLcLxtAdykWiP6QXUaPOq2hzJ1u43aQNFre_64JwcgFdBUL-gW-oNVLSfvsYkA6WPQQ_TOEgjqd3zaf8uzvJsRnFw4eLb2Jm-i_VieD9hnO3-NZ9XS5euyu6pvbn9fd8qY2pBWyFj0fWhhIz1rTcM0FgBFtb80AC4v5wpKGWyybBksYoB8mZgQQi4lmQoM29Ky6PuLaqLdqTG6n00FF7dRbIaa10mki1oPiE7FCEsIoa5kA3A7ScmC0Ad00nLEJ6-KINab4Zw-5qG3cpzC9r-ikiZiPz1OL45RJMecEw7-rBKtZUPWhoPQvIz-ZWA</addsrcrecordid><sourcetype>Open Website</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>3149749974</pqid></control><display><type>article</type><title>Exploring Orodispersible Films Containing the Proteolysis Targeting Chimera ARV-110 in Hot Melt Extrusion and Solvent Casting Using Polyvinyl Alcohol</title><source>DOAJ Directory of Open Access Journals</source><source>PubMed Central Open Access</source><source>MDPI - Multidisciplinary Digital Publishing Institute</source><source>EZB-FREE-00999 freely available EZB journals</source><source>PubMed Central</source><source>Free Full-Text Journals in Chemistry</source><creator>Meloni, Valentina ; Halstenberg, Laura ; Mareczek, Lena ; Lu, Jankin ; Liang, Bonnie ; Gottschalk, Nadine ; Mueller, Lena K.</creator><creatorcontrib>Meloni, Valentina ; Halstenberg, Laura ; Mareczek, Lena ; Lu, Jankin ; Liang, Bonnie ; Gottschalk, Nadine ; Mueller, Lena K.</creatorcontrib><description>Background/Objectives: This project aims to provide valuable insights into the formulation of orodispersible films (ODFs) for the delivery of PROTAC ARV-110. The primary objective of this drug delivery formulation is to enhance the solubility of PROTAC ARV-110, which faces significant challenges due to the low solubility of this active pharmaceutical ingredient, as it belongs to a molecular class that is considered to exceed the “Rule of Five”. Methods: We employed the concept of developing a rapidly disintegrating ODF to enhance the solubility of PROTAC ARV-110, utilizing polyvinyl alcohol as the polymer of choice. Given the high thermal stability of ARV-110, the PROTAC was subjected to two primary ODF manufacturing techniques: Hot melt extrusion (HME) and solvent casting. To establish the HME method, pre-screening through vacuum compression molding was performed. The films were characterized based on their disintegration in artificial saliva, drug release in a physiological environment, and mechanical strength. Results: All formulations demonstrated enhanced solubility of ARV-110, achieving exceptional results in terms of disintegration times and resistance to applied stress. Conclusions: The findings from the experiments outlined herein establish a solid foundation for the successful production of orodispersible films for the delivery of PROTACs.</description><identifier>ISSN: 1999-4923</identifier><identifier>EISSN: 1999-4923</identifier><identifier>DOI: 10.3390/pharmaceutics16121499</identifier><language>eng</language><publisher>Basel: MDPI AG</publisher><subject>Acids ; amorphous solid dispersions ; ASD ; Bioavailability ; Drug delivery systems ; Drug dosages ; Ligands ; ODF ; Orodispersible films ; Pharmaceuticals ; Polymers ; Polyvinyl alcohol ; PROTACs ; PVA ; Solvents ; Surfactants ; Temperature</subject><ispartof>Pharmaceutics, 2024-11, Vol.16 (12), p.1499</ispartof><rights>2024 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><cites>FETCH-LOGICAL-c1879-7b6f8ef1b48c26a67eec78bdcfe5d065d126d092209efebf4997e1d01a47aeac3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,864,2102,27924,27925</link.rule.ids></links><search><creatorcontrib>Meloni, Valentina</creatorcontrib><creatorcontrib>Halstenberg, Laura</creatorcontrib><creatorcontrib>Mareczek, Lena</creatorcontrib><creatorcontrib>Lu, Jankin</creatorcontrib><creatorcontrib>Liang, Bonnie</creatorcontrib><creatorcontrib>Gottschalk, Nadine</creatorcontrib><creatorcontrib>Mueller, Lena K.</creatorcontrib><title>Exploring Orodispersible Films Containing the Proteolysis Targeting Chimera ARV-110 in Hot Melt Extrusion and Solvent Casting Using Polyvinyl Alcohol</title><title>Pharmaceutics</title><description>Background/Objectives: This project aims to provide valuable insights into the formulation of orodispersible films (ODFs) for the delivery of PROTAC ARV-110. The primary objective of this drug delivery formulation is to enhance the solubility of PROTAC ARV-110, which faces significant challenges due to the low solubility of this active pharmaceutical ingredient, as it belongs to a molecular class that is considered to exceed the “Rule of Five”. Methods: We employed the concept of developing a rapidly disintegrating ODF to enhance the solubility of PROTAC ARV-110, utilizing polyvinyl alcohol as the polymer of choice. Given the high thermal stability of ARV-110, the PROTAC was subjected to two primary ODF manufacturing techniques: Hot melt extrusion (HME) and solvent casting. To establish the HME method, pre-screening through vacuum compression molding was performed. The films were characterized based on their disintegration in artificial saliva, drug release in a physiological environment, and mechanical strength. Results: All formulations demonstrated enhanced solubility of ARV-110, achieving exceptional results in terms of disintegration times and resistance to applied stress. Conclusions: The findings from the experiments outlined herein establish a solid foundation for the successful production of orodispersible films for the delivery of PROTACs.</description><subject>Acids</subject><subject>amorphous solid dispersions</subject><subject>ASD</subject><subject>Bioavailability</subject><subject>Drug delivery systems</subject><subject>Drug dosages</subject><subject>Ligands</subject><subject>ODF</subject><subject>Orodispersible films</subject><subject>Pharmaceuticals</subject><subject>Polymers</subject><subject>Polyvinyl alcohol</subject><subject>PROTACs</subject><subject>PVA</subject><subject>Solvents</subject><subject>Surfactants</subject><subject>Temperature</subject><issn>1999-4923</issn><issn>1999-4923</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><sourceid>8G5</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><sourceid>GUQSH</sourceid><sourceid>M2O</sourceid><sourceid>DOA</sourceid><recordid>eNptUdtq3DAQNaWBhjSfUBDk2a1kaSXrcTGbJpCSkEtfhSyNd7VoJVfShuyH5H9rZ0PpQ-ZhZpjLmeGcqvpG8HdKJf4xbnTaaQP74kwmnDSESfmpOiVSyprJhn7-L_9Snee8xZNRSloqT6vX1cvoY3JhjW5TtC6PkLLrPaBL53cZdTEU7cLcLxtAdykWiP6QXUaPOq2hzJ1u43aQNFre_64JwcgFdBUL-gW-oNVLSfvsYkA6WPQQ_TOEgjqd3zaf8uzvJsRnFw4eLb2Jm-i_VieD9hnO3-NZ9XS5euyu6pvbn9fd8qY2pBWyFj0fWhhIz1rTcM0FgBFtb80AC4v5wpKGWyybBksYoB8mZgQQi4lmQoM29Ky6PuLaqLdqTG6n00FF7dRbIaa10mki1oPiE7FCEsIoa5kA3A7ScmC0Ad00nLEJ6-KINab4Zw-5qG3cpzC9r-ikiZiPz1OL45RJMecEw7-rBKtZUPWhoPQvIz-ZWA</recordid><startdate>20241122</startdate><enddate>20241122</enddate><creator>Meloni, Valentina</creator><creator>Halstenberg, Laura</creator><creator>Mareczek, Lena</creator><creator>Lu, Jankin</creator><creator>Liang, Bonnie</creator><creator>Gottschalk, Nadine</creator><creator>Mueller, Lena K.</creator><general>MDPI AG</general><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7XB</scope><scope>8FK</scope><scope>8G5</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>GNUQQ</scope><scope>GUQSH</scope><scope>M2O</scope><scope>MBDVC</scope><scope>PIMPY</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>Q9U</scope><scope>DOA</scope></search><sort><creationdate>20241122</creationdate><title>Exploring Orodispersible Films Containing the Proteolysis Targeting Chimera ARV-110 in Hot Melt Extrusion and Solvent Casting Using Polyvinyl Alcohol</title><author>Meloni, Valentina ; Halstenberg, Laura ; Mareczek, Lena ; Lu, Jankin ; Liang, Bonnie ; Gottschalk, Nadine ; Mueller, Lena K.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c1879-7b6f8ef1b48c26a67eec78bdcfe5d065d126d092209efebf4997e1d01a47aeac3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><topic>Acids</topic><topic>amorphous solid dispersions</topic><topic>ASD</topic><topic>Bioavailability</topic><topic>Drug delivery systems</topic><topic>Drug dosages</topic><topic>Ligands</topic><topic>ODF</topic><topic>Orodispersible films</topic><topic>Pharmaceuticals</topic><topic>Polymers</topic><topic>Polyvinyl alcohol</topic><topic>PROTACs</topic><topic>PVA</topic><topic>Solvents</topic><topic>Surfactants</topic><topic>Temperature</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Meloni, Valentina</creatorcontrib><creatorcontrib>Halstenberg, Laura</creatorcontrib><creatorcontrib>Mareczek, Lena</creatorcontrib><creatorcontrib>Lu, Jankin</creatorcontrib><creatorcontrib>Liang, Bonnie</creatorcontrib><creatorcontrib>Gottschalk, Nadine</creatorcontrib><creatorcontrib>Mueller, Lena K.</creatorcontrib><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>Research Library (Alumni Edition)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>ProQuest Central</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>ProQuest Central Student</collection><collection>Research Library Prep</collection><collection>Research Library</collection><collection>Research Library (Corporate)</collection><collection>Publicly Available Content Database</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>ProQuest Central Basic</collection><collection>DOAJ Directory of Open Access Journals</collection><jtitle>Pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Meloni, Valentina</au><au>Halstenberg, Laura</au><au>Mareczek, Lena</au><au>Lu, Jankin</au><au>Liang, Bonnie</au><au>Gottschalk, Nadine</au><au>Mueller, Lena K.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Exploring Orodispersible Films Containing the Proteolysis Targeting Chimera ARV-110 in Hot Melt Extrusion and Solvent Casting Using Polyvinyl Alcohol</atitle><jtitle>Pharmaceutics</jtitle><date>2024-11-22</date><risdate>2024</risdate><volume>16</volume><issue>12</issue><spage>1499</spage><pages>1499-</pages><issn>1999-4923</issn><eissn>1999-4923</eissn><abstract>Background/Objectives: This project aims to provide valuable insights into the formulation of orodispersible films (ODFs) for the delivery of PROTAC ARV-110. The primary objective of this drug delivery formulation is to enhance the solubility of PROTAC ARV-110, which faces significant challenges due to the low solubility of this active pharmaceutical ingredient, as it belongs to a molecular class that is considered to exceed the “Rule of Five”. Methods: We employed the concept of developing a rapidly disintegrating ODF to enhance the solubility of PROTAC ARV-110, utilizing polyvinyl alcohol as the polymer of choice. Given the high thermal stability of ARV-110, the PROTAC was subjected to two primary ODF manufacturing techniques: Hot melt extrusion (HME) and solvent casting. To establish the HME method, pre-screening through vacuum compression molding was performed. The films were characterized based on their disintegration in artificial saliva, drug release in a physiological environment, and mechanical strength. Results: All formulations demonstrated enhanced solubility of ARV-110, achieving exceptional results in terms of disintegration times and resistance to applied stress. Conclusions: The findings from the experiments outlined herein establish a solid foundation for the successful production of orodispersible films for the delivery of PROTACs.</abstract><cop>Basel</cop><pub>MDPI AG</pub><doi>10.3390/pharmaceutics16121499</doi><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 1999-4923 |
| ispartof | Pharmaceutics, 2024-11, Vol.16 (12), p.1499 |
| issn | 1999-4923 1999-4923 |
| language | eng |
| recordid | cdi_proquest_journals_3149749974 |
| source | DOAJ Directory of Open Access Journals; PubMed Central Open Access; MDPI - Multidisciplinary Digital Publishing Institute; EZB-FREE-00999 freely available EZB journals; PubMed Central; Free Full-Text Journals in Chemistry |
| subjects | Acids amorphous solid dispersions ASD Bioavailability Drug delivery systems Drug dosages Ligands ODF Orodispersible films Pharmaceuticals Polymers Polyvinyl alcohol PROTACs PVA Solvents Surfactants Temperature |
| title | Exploring Orodispersible Films Containing the Proteolysis Targeting Chimera ARV-110 in Hot Melt Extrusion and Solvent Casting Using Polyvinyl Alcohol |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-06T22%3A28%3A15IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_doaj_&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Exploring%20Orodispersible%20Films%20Containing%20the%20Proteolysis%20Targeting%20Chimera%20ARV-110%20in%20Hot%20Melt%20Extrusion%20and%20Solvent%20Casting%20Using%20Polyvinyl%20Alcohol&rft.jtitle=Pharmaceutics&rft.au=Meloni,%20Valentina&rft.date=2024-11-22&rft.volume=16&rft.issue=12&rft.spage=1499&rft.pages=1499-&rft.issn=1999-4923&rft.eissn=1999-4923&rft_id=info:doi/10.3390/pharmaceutics16121499&rft_dat=%3Cproquest_doaj_%3E3149749974%3C/proquest_doaj_%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=3149749974&rft_id=info:pmid/&rft_doaj_id=oai_doaj_org_article_62147911434847e08f9d6e432ea22644&rfr_iscdi=true |