Double-responsive hyaluronic acid-based prodrugs for efficient tumour targeting
Hyaluronic acid (HA)-based prodrugs bearing double-responsive (acid pH or oxidation) boronates of catechol-containing drugs were used to treat xenografted human prostate tumours (LNCaP) in SCID mice. The HA prodrugs accumulated significantly only in tumours (impressively, up to 40% of the injected d...
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| Veröffentlicht in: | Materials Science & Engineering C 2021-12, Vol.131, p.112475-112475, Article 112475 |
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| container_title | Materials Science & Engineering C |
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| creator | Quagliariello, Vincenzo Gennari, Arianna Jain, Som Akshay Rosso, Francesco Iaffaioli, Rosario Vincenzo Barbarisi, Alfonso Barbarisi, Manlio Tirelli, Nicola |
| description | Hyaluronic acid (HA)-based prodrugs bearing double-responsive (acid pH or oxidation) boronates of catechol-containing drugs were used to treat xenografted human prostate tumours (LNCaP) in SCID mice. The HA prodrugs accumulated significantly only in tumours (impressively, up to 40% of the injected dose after 24 h) and in liver, with negligible – actually anti-inflammatory - consequences in the latter. A quercetin-HA prodrug significantly slowed down tumour growth, in a dose-dependent fashion and with a much higher efficacy (up to 4 times) than equivalent doses of free quercetin. In short, boronated HA appears to be a very promising platform for targeted chemotherapy.
Hyaluronic acid-based prodrugs bearing side-chain boronic esters show excellent tumour accumulation (targeting) and acid pH- or reactive oxygen species (ROS)-responsive release of polyphenolic drugs such as quercetin. The chemotherapeutic performance of the latter in xenografted mice is dramatically improved upon conjugation with HA. [Display omitted]
•Boronate-linked payloads can be released from hyaluronic acid upon acidification or oxidation.•Boronate-based hyaluronic acid prodrugs accumulate in tumours up to 40–50% of the injected doses.•Boronate-based hyaluronic acid prodrugs efficiently treat human prostate tumours in SCID mice. |
| doi_str_mv | 10.1016/j.msec.2021.112475 |
| format | Article |
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Hyaluronic acid-based prodrugs bearing side-chain boronic esters show excellent tumour accumulation (targeting) and acid pH- or reactive oxygen species (ROS)-responsive release of polyphenolic drugs such as quercetin. The chemotherapeutic performance of the latter in xenografted mice is dramatically improved upon conjugation with HA. [Display omitted]
•Boronate-linked payloads can be released from hyaluronic acid upon acidification or oxidation.•Boronate-based hyaluronic acid prodrugs accumulate in tumours up to 40–50% of the injected doses.•Boronate-based hyaluronic acid prodrugs efficiently treat human prostate tumours in SCID mice.</description><identifier>ISSN: 0928-4931</identifier><identifier>EISSN: 1873-0191</identifier><identifier>DOI: 10.1016/j.msec.2021.112475</identifier><language>eng</language><publisher>Lausanne: Elsevier B.V</publisher><subject>Boronates ; Cancer ; Catechol ; Chemotherapy ; Drugs ; Field flow fractionation ; Hyaluronic acid ; Inflammation ; Materials science ; Oxidation ; Prodrugs ; Prostate ; Quercetin ; Responsive release ; Targeted drug delivery ; Tumors ; Xenografts</subject><ispartof>Materials Science & Engineering C, 2021-12, Vol.131, p.112475-112475, Article 112475</ispartof><rights>2021 The Authors</rights><rights>Copyright Elsevier BV Dec 2021</rights><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c405t-680a333a9323f5073c193e4c0d8772a740a88fbeb2b5c661cabe1156197038cc3</citedby><cites>FETCH-LOGICAL-c405t-680a333a9323f5073c193e4c0d8772a740a88fbeb2b5c661cabe1156197038cc3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.msec.2021.112475$$EHTML$$P50$$Gelsevier$$Hfree_for_read</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,45974</link.rule.ids></links><search><creatorcontrib>Quagliariello, Vincenzo</creatorcontrib><creatorcontrib>Gennari, Arianna</creatorcontrib><creatorcontrib>Jain, Som Akshay</creatorcontrib><creatorcontrib>Rosso, Francesco</creatorcontrib><creatorcontrib>Iaffaioli, Rosario Vincenzo</creatorcontrib><creatorcontrib>Barbarisi, Alfonso</creatorcontrib><creatorcontrib>Barbarisi, Manlio</creatorcontrib><creatorcontrib>Tirelli, Nicola</creatorcontrib><title>Double-responsive hyaluronic acid-based prodrugs for efficient tumour targeting</title><title>Materials Science & Engineering C</title><description>Hyaluronic acid (HA)-based prodrugs bearing double-responsive (acid pH or oxidation) boronates of catechol-containing drugs were used to treat xenografted human prostate tumours (LNCaP) in SCID mice. The HA prodrugs accumulated significantly only in tumours (impressively, up to 40% of the injected dose after 24 h) and in liver, with negligible – actually anti-inflammatory - consequences in the latter. A quercetin-HA prodrug significantly slowed down tumour growth, in a dose-dependent fashion and with a much higher efficacy (up to 4 times) than equivalent doses of free quercetin. In short, boronated HA appears to be a very promising platform for targeted chemotherapy.
Hyaluronic acid-based prodrugs bearing side-chain boronic esters show excellent tumour accumulation (targeting) and acid pH- or reactive oxygen species (ROS)-responsive release of polyphenolic drugs such as quercetin. The chemotherapeutic performance of the latter in xenografted mice is dramatically improved upon conjugation with HA. [Display omitted]
•Boronate-linked payloads can be released from hyaluronic acid upon acidification or oxidation.•Boronate-based hyaluronic acid prodrugs accumulate in tumours up to 40–50% of the injected doses.•Boronate-based hyaluronic acid prodrugs efficiently treat human prostate tumours in SCID mice.</description><subject>Boronates</subject><subject>Cancer</subject><subject>Catechol</subject><subject>Chemotherapy</subject><subject>Drugs</subject><subject>Field flow fractionation</subject><subject>Hyaluronic acid</subject><subject>Inflammation</subject><subject>Materials science</subject><subject>Oxidation</subject><subject>Prodrugs</subject><subject>Prostate</subject><subject>Quercetin</subject><subject>Responsive release</subject><subject>Targeted drug delivery</subject><subject>Tumors</subject><subject>Xenografts</subject><issn>0928-4931</issn><issn>1873-0191</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><recordid>eNp9kD1PwzAQhi0EEqXwB5gisbAk-OwkdiQWVD6lSl1gthznUhylcbGTSvx7HJWJgeF0y_Oe3nsIuQaaAYXyrst2AU3GKIMMgOWiOCELkIKnFCo4JQtaMZnmFYdzchFCR2kpuWALsnl0U91j6jHs3RDsAZPPb91P3g3WJNrYJq11wCbZe9f4aRuS1vkE29Yai8OYjNPOTT4Ztd_iaIftJTlrdR_w6ncvycfz0_vqNV1vXt5WD-vU5LQY01JSzTnXFWe8LajgBiqOuaGNFIJpkVMtZVtjzerClCUYXSNAUUIlKJfG8CW5Pd6Nvb4mDKPa2WCw7_WAbgqKlbSMLzMBEb35g3ax8hDbRQqkpCJOpNiRMt6F4LFVe2932n8roGp2rDo1O1azY3V0HEP3xxDGVw8WvQqzFoON9WhG1Tj7X_wHMAGEiA</recordid><startdate>202112</startdate><enddate>202112</enddate><creator>Quagliariello, Vincenzo</creator><creator>Gennari, Arianna</creator><creator>Jain, Som Akshay</creator><creator>Rosso, Francesco</creator><creator>Iaffaioli, Rosario Vincenzo</creator><creator>Barbarisi, Alfonso</creator><creator>Barbarisi, Manlio</creator><creator>Tirelli, Nicola</creator><general>Elsevier B.V</general><general>Elsevier BV</general><scope>6I.</scope><scope>AAFTH</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QF</scope><scope>7QO</scope><scope>7QQ</scope><scope>7SC</scope><scope>7SE</scope><scope>7SP</scope><scope>7SR</scope><scope>7T7</scope><scope>7TA</scope><scope>7TB</scope><scope>7U5</scope><scope>8BQ</scope><scope>8FD</scope><scope>C1K</scope><scope>F28</scope><scope>FR3</scope><scope>H8D</scope><scope>H8G</scope><scope>JG9</scope><scope>JQ2</scope><scope>KR7</scope><scope>L7M</scope><scope>L~C</scope><scope>L~D</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>202112</creationdate><title>Double-responsive hyaluronic acid-based prodrugs for efficient tumour targeting</title><author>Quagliariello, Vincenzo ; 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The HA prodrugs accumulated significantly only in tumours (impressively, up to 40% of the injected dose after 24 h) and in liver, with negligible – actually anti-inflammatory - consequences in the latter. A quercetin-HA prodrug significantly slowed down tumour growth, in a dose-dependent fashion and with a much higher efficacy (up to 4 times) than equivalent doses of free quercetin. In short, boronated HA appears to be a very promising platform for targeted chemotherapy.
Hyaluronic acid-based prodrugs bearing side-chain boronic esters show excellent tumour accumulation (targeting) and acid pH- or reactive oxygen species (ROS)-responsive release of polyphenolic drugs such as quercetin. The chemotherapeutic performance of the latter in xenografted mice is dramatically improved upon conjugation with HA. [Display omitted]
•Boronate-linked payloads can be released from hyaluronic acid upon acidification or oxidation.•Boronate-based hyaluronic acid prodrugs accumulate in tumours up to 40–50% of the injected doses.•Boronate-based hyaluronic acid prodrugs efficiently treat human prostate tumours in SCID mice.</abstract><cop>Lausanne</cop><pub>Elsevier B.V</pub><doi>10.1016/j.msec.2021.112475</doi><tpages>1</tpages><oa>free_for_read</oa></addata></record> |
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| source | Elsevier ScienceDirect Journals |
| subjects | Boronates Cancer Catechol Chemotherapy Drugs Field flow fractionation Hyaluronic acid Inflammation Materials science Oxidation Prodrugs Prostate Quercetin Responsive release Targeted drug delivery Tumors Xenografts |
| title | Double-responsive hyaluronic acid-based prodrugs for efficient tumour targeting |
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