Enhancing the Efficacy of Chemotherapeutic Drugs Via Encapsulation within Nanocomplexes Designed to Cross the Blood-Brain Barrier and Target Tumors
<p id="p1">The blood-brain barrier (BBB) blocks ~98% of drugs, so brain tumors tend to be refractory to chemotherapy. Transferrin receptors (TfRs) are expressed on the endothelial cell that comprise the BBB and mediate the movement of transferrin into the brain <em><italic xmlns:mml="http://www.w3.o...
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| Formato: | Capítulo de libro |
| Lenguaje: | inglés |
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IntechOpen
2024
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| Acceso en línea: | https://www.intechopen.com/chapters/1201034 |
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| _version_ | 1879164864919764992 |
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| author | Harford, Joe B. Kim, Sang-Soo Pirollo, Kathleen F. Rait, Antonina S. Chang, Esther H. |
| author_browse | Chang, Esther H. Harford, Joe B. Kim, Sang-Soo Pirollo, Kathleen F. Rait, Antonina S. |
| author_facet | Harford, Joe B. Kim, Sang-Soo Pirollo, Kathleen F. Rait, Antonina S. Chang, Esther H. |
| author_sort | Harford, Joe B. |
| building | IntechOpen |
| collection | Acceso abierto |
| description | <p id="p1">The blood-brain barrier (BBB) blocks ~98% of drugs, so brain tumors tend to be refractory to chemotherapy. Transferrin receptors (TfRs) are expressed on the endothelial cell that comprise the BBB and mediate the movement of transferrin into the brain <em><italic xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance">via</italic></em> transcytosis. Tumor cells overexpress TfRs, so encapsulating drugs within nanocomplexes that bind to TfRs has the potential to enhance both entry into the brain and delivery to tumor cells. Here, we present data on the use of TfR-targeted platform nanotechnology termed scL (for <underline>s</underline>ingle-<underline>c</underline>hain <underline>L</underline>iposome) to encapsulate five different chemotherapeutic agents. Data are provided showing that scL nanoformulations of these drugs were more effective in killing cancer cells than their unencapsulated counterparts. It is not our intention to study any one of these nanoformulations in detail but rather to highlight the general versatility of this drug delivery system. The scL formulation of TMZ (scL-TMZ) was more effective than unencapsulated TMZ against TMZ-resistant glioblastoma (GBM) and displayed improved efficacy in impeding tumor growth and extending lifespan in mice bearing intracranial GBM tumors. The scL formulation of irinotecan displayed both enhanced potency in killing lung cancer cells in culture and improved <em><italic xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance">in vivo</italic></em> efficacy in a murine lung cancer xenograft model.</p> |
| doi_str_mv | 10.5772/intechopen.1007332 |
| first_indexed | 2026-10-15T21:41:07Z |
| format | Book Chapter |
| fullrecord | <oai_dc:dc xmlns:oai_dc="http://www.openarchives.org/OAI/2.0/oai_dc/" xmlns:dc="http://purl.org/dc/elements/1.1/" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" xsi:schemaLocation="http://www.openarchives.org/OAI/2.0/oai_dc/ http://www.openarchives.org/OAI/2.0/oai_dc.xsd"><identifier>intech-1201034</identifier><datestamp>2024-10-15</datestamp>
<dc:title>Enhancing the Efficacy of Chemotherapeutic Drugs Via Encapsulation within Nanocomplexes Designed to Cross the Blood-Brain Barrier and Target Tumors</dc:title>
<dc:creator>Joe B. Harford</dc:creator>
<dc:creator>Sang-Soo Kim</dc:creator>
<dc:creator>Kathleen F. Pirollo</dc:creator>
<dc:creator>Antonina S. Rait</dc:creator>
<dc:creator>Esther H. Chang</dc:creator>
<dc:subject>Health Sciences</dc:subject>
<dc:description><p id="p1">The blood-brain barrier (BBB) blocks ~98% of drugs, so brain tumors tend to be refractory to chemotherapy. Transferrin receptors (TfRs) are expressed on the endothelial cell that comprise the BBB and mediate the movement of transferrin into the brain <em><italic xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance">via</italic></em> transcytosis. Tumor cells overexpress TfRs, so encapsulating drugs within nanocomplexes that bind to TfRs has the potential to enhance both entry into the brain and delivery to tumor cells. Here, we present data on the use of TfR-targeted platform nanotechnology termed scL (for <underline>s</underline>ingle-<underline>c</underline>hain <underline>L</underline>iposome) to encapsulate five different chemotherapeutic agents. Data are provided showing that scL nanoformulations of these drugs were more effective in killing cancer cells than their unencapsulated counterparts. It is not our intention to study any one of these nanoformulations in detail but rather to highlight the general versatility of this drug delivery system. The scL formulation of TMZ (scL-TMZ) was more effective than unencapsulated TMZ against TMZ-resistant glioblastoma (GBM) and displayed improved efficacy in impeding tumor growth and extending lifespan in mice bearing intracranial GBM tumors. The scL formulation of irinotecan displayed both enhanced potency in killing lung cancer cells in culture and improved <em><italic xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance">in vivo</italic></em> efficacy in a murine lung cancer xenograft model.</p></dc:description>
<dc:publisher>IntechOpen</dc:publisher>
<dc:date>2024-10-15</dc:date>
<dc:type>Chapter, Part Of Book</dc:type>
<dc:identifier>https://www.intechopen.com/chapters/1201034</dc:identifier>
<dc:identifier>doi:10.5772/intechopen.1007332</dc:identifier>
<dc:language>en</dc:language>
<dc:relation>ISBN:978-0-85014-808-4</dc:relation>
<dc:rights>https://creativecommons.org/licenses/by/3.0/</dc:rights>
<dc:source>https://www.intechopen.com/books/1004112 ; Advanced Concepts and Strategies in Central Nervous System Tumors</dc:source>
</oai_dc:dc> |
| id | intech-1201034 |
| institution | IntechOpen |
| isbn | 978-0-85014-808-4 |
| language | English |
| last_indexed | 2026-10-15T21:41:07Z |
| publishDate | 2024 |
| publishDateRange | 2024 |
| publishDateSort | 2024 |
| publisher | IntechOpen |
| publisherStr | IntechOpen |
| record_format | oai_dc |
| spelling | intech-12010342024-10-15 Enhancing the Efficacy of Chemotherapeutic Drugs Via Encapsulation within Nanocomplexes Designed to Cross the Blood-Brain Barrier and Target Tumors Joe B. Harford Sang-Soo Kim Kathleen F. Pirollo Antonina S. Rait Esther H. Chang Health Sciences <p id="p1">The blood-brain barrier (BBB) blocks ~98% of drugs, so brain tumors tend to be refractory to chemotherapy. Transferrin receptors (TfRs) are expressed on the endothelial cell that comprise the BBB and mediate the movement of transferrin into the brain <em><italic xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance">via</italic></em> transcytosis. Tumor cells overexpress TfRs, so encapsulating drugs within nanocomplexes that bind to TfRs has the potential to enhance both entry into the brain and delivery to tumor cells. Here, we present data on the use of TfR-targeted platform nanotechnology termed scL (for <underline>s</underline>ingle-<underline>c</underline>hain <underline>L</underline>iposome) to encapsulate five different chemotherapeutic agents. Data are provided showing that scL nanoformulations of these drugs were more effective in killing cancer cells than their unencapsulated counterparts. It is not our intention to study any one of these nanoformulations in detail but rather to highlight the general versatility of this drug delivery system. The scL formulation of TMZ (scL-TMZ) was more effective than unencapsulated TMZ against TMZ-resistant glioblastoma (GBM) and displayed improved efficacy in impeding tumor growth and extending lifespan in mice bearing intracranial GBM tumors. The scL formulation of irinotecan displayed both enhanced potency in killing lung cancer cells in culture and improved <em><italic xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance">in vivo</italic></em> efficacy in a murine lung cancer xenograft model.</p> IntechOpen 2024-10-15 Chapter, Part Of Book https://www.intechopen.com/chapters/1201034 doi:10.5772/intechopen.1007332 en ISBN:978-0-85014-808-4 https://creativecommons.org/licenses/by/3.0/ https://www.intechopen.com/books/1004112 ; Advanced Concepts and Strategies in Central Nervous System Tumors |
| spellingShingle | Health Sciences Harford, Joe B. Kim, Sang-Soo Pirollo, Kathleen F. Rait, Antonina S. Chang, Esther H. Enhancing the Efficacy of Chemotherapeutic Drugs Via Encapsulation within Nanocomplexes Designed to Cross the Blood-Brain Barrier and Target Tumors |
| title | Enhancing the Efficacy of Chemotherapeutic Drugs Via Encapsulation within Nanocomplexes Designed to Cross the Blood-Brain Barrier and Target Tumors |
| title_full | Enhancing the Efficacy of Chemotherapeutic Drugs Via Encapsulation within Nanocomplexes Designed to Cross the Blood-Brain Barrier and Target Tumors |
| title_fullStr | Enhancing the Efficacy of Chemotherapeutic Drugs Via Encapsulation within Nanocomplexes Designed to Cross the Blood-Brain Barrier and Target Tumors |
| title_full_unstemmed | Enhancing the Efficacy of Chemotherapeutic Drugs Via Encapsulation within Nanocomplexes Designed to Cross the Blood-Brain Barrier and Target Tumors |
| title_short | Enhancing the Efficacy of Chemotherapeutic Drugs Via Encapsulation within Nanocomplexes Designed to Cross the Blood-Brain Barrier and Target Tumors |
| title_sort | enhancing the efficacy of chemotherapeutic drugs via encapsulation within nanocomplexes designed to cross the blood brain barrier and target tumors |
| topic | Health Sciences |
| url | https://www.intechopen.com/chapters/1201034 |
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