Novel microspheres based on triterpene saponins from the roots of Physospermum verticillatum (Waldst & Kit) (Apiaceae) for the improvement of gemcitabine release
Objectives This study concerns the preparation and characterization of microspheres based on a mixture of triterpene saponins, from Physospermum verticillatum (Waldst & Kit), as a carrier for the specific release of gemcitabine. Methods Triterpene saponins were derivatized with acrylic acid. The...
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| Veröffentlicht in: | Journal of pharmacy and pharmacology 2016-02, Vol.68 (2), p.275-281 |
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| container_title | Journal of pharmacy and pharmacology |
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| creator | Trombino, Sonia Cassano, Roberta Mellace, Silvia Picci, Nevio Loizzo, Monica R. Menichini, Francesco Tundis, Rosa |
| description | Objectives
This study concerns the preparation and characterization of microspheres based on a mixture of triterpene saponins, from Physospermum verticillatum (Waldst & Kit), as a carrier for the specific release of gemcitabine.
Methods
Triterpene saponins were derivatized with acrylic acid. The obtained polymerizable product was characterized by Fourier transform infrared to confirm the ester linkage. Then, spherical microparticles were prepared by suspension radical copolymerization and impregnated with gemcitabine.
Key findings
Microspheres exhibited a mean diameter of 2.7 μ. The swelling studies showed that particles swell most at pH 6.2, typical of the tumour pathology, than at pH 7.4, miming physiological conditions. The microspheres were loaded with gemcitabine (LE 72.2%). Their release profile showed an initial dot of around 24% and a further release for 24 h.
Conclusions
This carrier could be potentially release the drug in the lung, as a function of different pHs between tumour cells and healthy, reducing the systemic drug toxicity, allowing the reduction of the doses number, increasing the drug half‐life and eliminating the problems related to the fast clearance of gemcitabine administration. |
| doi_str_mv | 10.1111/jphp.12509 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_1765917154</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>3953539821</sourcerecordid><originalsourceid>FETCH-LOGICAL-c3959-81f7a9162a2a32603d306e753ff99a25c799d5b88d80360f1c37b26846ad7a4d3</originalsourceid><addsrcrecordid>eNp9kc1u1DAUhS0EokNhwwMgS0jVtFKKfyZ2smwLTIFRmUVR2VlOcsN4iONgO4V5HN60npm2CxZ4Y1n67vG55yD0mpJTms679bAaTinLSfkETRiZsUzSvHiKJoQwlvFc8gP0IoQ1IUQKIZ6jAyYKzmeMT9DfK3cLHbam9i4MK_AQcKUDNNj1OHoTwQ_QAw56cL3pA269sziuAHvnYsCuxcvVJqRZ8Ha0-BZ8NLXpOh3Ta3qjuyZEfIS_mHiMp2eD0TVoOMat8zsVYwefHFjo41brB9jaRF2Z9KWHDpKTl-hZq7sAr-7vQ_Tt44fri8ts8XX-6eJskdW8zMusoK3UJRVMM82ZILzhRIDMeduWpWZ5LcuyyauiaArCBWlpzWWVcpgJ3Ug9a_ghmu51k6FfI4SorAk1pE16cGNQVIq8pCnZWULf_oOu3ej75G5HMUFTtok62VPbaIOHVg3eWO03ihK1LU5ti1O74hL85l5yrCw0j-hDUwmge-C36WDzHyn1eXm5fBDN9jMmRPjzOKP9TyUkl7m6uZqrxTm5Pv8-l-o9vwMq-rOh</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>1765261423</pqid></control><display><type>article</type><title>Novel microspheres based on triterpene saponins from the roots of Physospermum verticillatum (Waldst & Kit) (Apiaceae) for the improvement of gemcitabine release</title><source>MEDLINE</source><source>Wiley Journals</source><source>Oxford University Press Journals All Titles (1996-Current)</source><creator>Trombino, Sonia ; Cassano, Roberta ; Mellace, Silvia ; Picci, Nevio ; Loizzo, Monica R. ; Menichini, Francesco ; Tundis, Rosa</creator><creatorcontrib>Trombino, Sonia ; Cassano, Roberta ; Mellace, Silvia ; Picci, Nevio ; Loizzo, Monica R. ; Menichini, Francesco ; Tundis, Rosa</creatorcontrib><description>Objectives
This study concerns the preparation and characterization of microspheres based on a mixture of triterpene saponins, from Physospermum verticillatum (Waldst & Kit), as a carrier for the specific release of gemcitabine.
Methods
Triterpene saponins were derivatized with acrylic acid. The obtained polymerizable product was characterized by Fourier transform infrared to confirm the ester linkage. Then, spherical microparticles were prepared by suspension radical copolymerization and impregnated with gemcitabine.
Key findings
Microspheres exhibited a mean diameter of 2.7 μ. The swelling studies showed that particles swell most at pH 6.2, typical of the tumour pathology, than at pH 7.4, miming physiological conditions. The microspheres were loaded with gemcitabine (LE 72.2%). Their release profile showed an initial dot of around 24% and a further release for 24 h.
Conclusions
This carrier could be potentially release the drug in the lung, as a function of different pHs between tumour cells and healthy, reducing the systemic drug toxicity, allowing the reduction of the doses number, increasing the drug half‐life and eliminating the problems related to the fast clearance of gemcitabine administration.</description><identifier>ISSN: 0022-3573</identifier><identifier>EISSN: 2042-7158</identifier><identifier>DOI: 10.1111/jphp.12509</identifier><identifier>PMID: 26833423</identifier><identifier>CODEN: JPPMAB</identifier><language>eng</language><publisher>England: Blackwell Publishing Ltd</publisher><subject><![CDATA[Antimetabolites, Antineoplastic - administration & dosage ; Antimetabolites, Antineoplastic - chemistry ; Apiaceae - chemistry ; Deoxycytidine - administration & dosage ; Deoxycytidine - analogs & derivatives ; Deoxycytidine - chemistry ; Drug Carriers - chemistry ; Drug Carriers - isolation & purification ; Drug Compounding ; Drug Liberation ; gemcitabine ; Hydrogen-Ion Concentration ; lung cancer ; Microspheres ; Plant Roots - chemistry ; release ; Saponins - chemistry ; Saponins - isolation & purification ; Spectroscopy, Fourier Transform Infrared ; Surface Properties ; triterpene saponins ; Triterpenes - chemistry ; Triterpenes - isolation & purification]]></subject><ispartof>Journal of pharmacy and pharmacology, 2016-02, Vol.68 (2), p.275-281</ispartof><rights>2016 Royal Pharmaceutical Society</rights><rights>2016 Royal Pharmaceutical Society.</rights><rights>Copyright © 2016 Royal Pharmaceutical Society</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3959-81f7a9162a2a32603d306e753ff99a25c799d5b88d80360f1c37b26846ad7a4d3</citedby><cites>FETCH-LOGICAL-c3959-81f7a9162a2a32603d306e753ff99a25c799d5b88d80360f1c37b26846ad7a4d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1111%2Fjphp.12509$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1111%2Fjphp.12509$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1417,27924,27925,45574,45575</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/26833423$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Trombino, Sonia</creatorcontrib><creatorcontrib>Cassano, Roberta</creatorcontrib><creatorcontrib>Mellace, Silvia</creatorcontrib><creatorcontrib>Picci, Nevio</creatorcontrib><creatorcontrib>Loizzo, Monica R.</creatorcontrib><creatorcontrib>Menichini, Francesco</creatorcontrib><creatorcontrib>Tundis, Rosa</creatorcontrib><title>Novel microspheres based on triterpene saponins from the roots of Physospermum verticillatum (Waldst & Kit) (Apiaceae) for the improvement of gemcitabine release</title><title>Journal of pharmacy and pharmacology</title><addtitle>J Pharm Pharmacol</addtitle><description>Objectives
This study concerns the preparation and characterization of microspheres based on a mixture of triterpene saponins, from Physospermum verticillatum (Waldst & Kit), as a carrier for the specific release of gemcitabine.
Methods
Triterpene saponins were derivatized with acrylic acid. The obtained polymerizable product was characterized by Fourier transform infrared to confirm the ester linkage. Then, spherical microparticles were prepared by suspension radical copolymerization and impregnated with gemcitabine.
Key findings
Microspheres exhibited a mean diameter of 2.7 μ. The swelling studies showed that particles swell most at pH 6.2, typical of the tumour pathology, than at pH 7.4, miming physiological conditions. The microspheres were loaded with gemcitabine (LE 72.2%). Their release profile showed an initial dot of around 24% and a further release for 24 h.
Conclusions
This carrier could be potentially release the drug in the lung, as a function of different pHs between tumour cells and healthy, reducing the systemic drug toxicity, allowing the reduction of the doses number, increasing the drug half‐life and eliminating the problems related to the fast clearance of gemcitabine administration.</description><subject>Antimetabolites, Antineoplastic - administration & dosage</subject><subject>Antimetabolites, Antineoplastic - chemistry</subject><subject>Apiaceae - chemistry</subject><subject>Deoxycytidine - administration & dosage</subject><subject>Deoxycytidine - analogs & derivatives</subject><subject>Deoxycytidine - chemistry</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Carriers - isolation & purification</subject><subject>Drug Compounding</subject><subject>Drug Liberation</subject><subject>gemcitabine</subject><subject>Hydrogen-Ion Concentration</subject><subject>lung cancer</subject><subject>Microspheres</subject><subject>Plant Roots - chemistry</subject><subject>release</subject><subject>Saponins - chemistry</subject><subject>Saponins - isolation & purification</subject><subject>Spectroscopy, Fourier Transform Infrared</subject><subject>Surface Properties</subject><subject>triterpene saponins</subject><subject>Triterpenes - chemistry</subject><subject>Triterpenes - isolation & purification</subject><issn>0022-3573</issn><issn>2042-7158</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kc1u1DAUhS0EokNhwwMgS0jVtFKKfyZ2smwLTIFRmUVR2VlOcsN4iONgO4V5HN60npm2CxZ4Y1n67vG55yD0mpJTms679bAaTinLSfkETRiZsUzSvHiKJoQwlvFc8gP0IoQ1IUQKIZ6jAyYKzmeMT9DfK3cLHbam9i4MK_AQcKUDNNj1OHoTwQ_QAw56cL3pA269sziuAHvnYsCuxcvVJqRZ8Ha0-BZ8NLXpOh3Ta3qjuyZEfIS_mHiMp2eD0TVoOMat8zsVYwefHFjo41brB9jaRF2Z9KWHDpKTl-hZq7sAr-7vQ_Tt44fri8ts8XX-6eJskdW8zMusoK3UJRVMM82ZILzhRIDMeduWpWZ5LcuyyauiaArCBWlpzWWVcpgJ3Ug9a_ghmu51k6FfI4SorAk1pE16cGNQVIq8pCnZWULf_oOu3ej75G5HMUFTtok62VPbaIOHVg3eWO03ihK1LU5ti1O74hL85l5yrCw0j-hDUwmge-C36WDzHyn1eXm5fBDN9jMmRPjzOKP9TyUkl7m6uZqrxTm5Pv8-l-o9vwMq-rOh</recordid><startdate>201602</startdate><enddate>201602</enddate><creator>Trombino, Sonia</creator><creator>Cassano, Roberta</creator><creator>Mellace, Silvia</creator><creator>Picci, Nevio</creator><creator>Loizzo, Monica R.</creator><creator>Menichini, Francesco</creator><creator>Tundis, Rosa</creator><general>Blackwell Publishing Ltd</general><general>Wiley Subscription Services, Inc</general><scope>BSCLL</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QP</scope><scope>7TK</scope><scope>7U9</scope><scope>H94</scope><scope>K9.</scope><scope>M7N</scope><scope>7X8</scope></search><sort><creationdate>201602</creationdate><title>Novel microspheres based on triterpene saponins from the roots of Physospermum verticillatum (Waldst & Kit) (Apiaceae) for the improvement of gemcitabine release</title><author>Trombino, Sonia ; Cassano, Roberta ; Mellace, Silvia ; Picci, Nevio ; Loizzo, Monica R. ; Menichini, Francesco ; Tundis, Rosa</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3959-81f7a9162a2a32603d306e753ff99a25c799d5b88d80360f1c37b26846ad7a4d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Antimetabolites, Antineoplastic - administration & dosage</topic><topic>Antimetabolites, Antineoplastic - chemistry</topic><topic>Apiaceae - chemistry</topic><topic>Deoxycytidine - administration & dosage</topic><topic>Deoxycytidine - analogs & derivatives</topic><topic>Deoxycytidine - chemistry</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Carriers - isolation & purification</topic><topic>Drug Compounding</topic><topic>Drug Liberation</topic><topic>gemcitabine</topic><topic>Hydrogen-Ion Concentration</topic><topic>lung cancer</topic><topic>Microspheres</topic><topic>Plant Roots - chemistry</topic><topic>release</topic><topic>Saponins - chemistry</topic><topic>Saponins - isolation & purification</topic><topic>Spectroscopy, Fourier Transform Infrared</topic><topic>Surface Properties</topic><topic>triterpene saponins</topic><topic>Triterpenes - chemistry</topic><topic>Triterpenes - isolation & purification</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Trombino, Sonia</creatorcontrib><creatorcontrib>Cassano, Roberta</creatorcontrib><creatorcontrib>Mellace, Silvia</creatorcontrib><creatorcontrib>Picci, Nevio</creatorcontrib><creatorcontrib>Loizzo, Monica R.</creatorcontrib><creatorcontrib>Menichini, Francesco</creatorcontrib><creatorcontrib>Tundis, Rosa</creatorcontrib><collection>Istex</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of pharmacy and pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Trombino, Sonia</au><au>Cassano, Roberta</au><au>Mellace, Silvia</au><au>Picci, Nevio</au><au>Loizzo, Monica R.</au><au>Menichini, Francesco</au><au>Tundis, Rosa</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Novel microspheres based on triterpene saponins from the roots of Physospermum verticillatum (Waldst & Kit) (Apiaceae) for the improvement of gemcitabine release</atitle><jtitle>Journal of pharmacy and pharmacology</jtitle><addtitle>J Pharm Pharmacol</addtitle><date>2016-02</date><risdate>2016</risdate><volume>68</volume><issue>2</issue><spage>275</spage><epage>281</epage><pages>275-281</pages><issn>0022-3573</issn><eissn>2042-7158</eissn><coden>JPPMAB</coden><abstract>Objectives
This study concerns the preparation and characterization of microspheres based on a mixture of triterpene saponins, from Physospermum verticillatum (Waldst & Kit), as a carrier for the specific release of gemcitabine.
Methods
Triterpene saponins were derivatized with acrylic acid. The obtained polymerizable product was characterized by Fourier transform infrared to confirm the ester linkage. Then, spherical microparticles were prepared by suspension radical copolymerization and impregnated with gemcitabine.
Key findings
Microspheres exhibited a mean diameter of 2.7 μ. The swelling studies showed that particles swell most at pH 6.2, typical of the tumour pathology, than at pH 7.4, miming physiological conditions. The microspheres were loaded with gemcitabine (LE 72.2%). Their release profile showed an initial dot of around 24% and a further release for 24 h.
Conclusions
This carrier could be potentially release the drug in the lung, as a function of different pHs between tumour cells and healthy, reducing the systemic drug toxicity, allowing the reduction of the doses number, increasing the drug half‐life and eliminating the problems related to the fast clearance of gemcitabine administration.</abstract><cop>England</cop><pub>Blackwell Publishing Ltd</pub><pmid>26833423</pmid><doi>10.1111/jphp.12509</doi><tpages>7</tpages></addata></record> |
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| ispartof | Journal of pharmacy and pharmacology, 2016-02, Vol.68 (2), p.275-281 |
| issn | 0022-3573 2042-7158 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_1765917154 |
| source | MEDLINE; Wiley Journals; Oxford University Press Journals All Titles (1996-Current) |
| subjects | Antimetabolites, Antineoplastic - administration & dosage Antimetabolites, Antineoplastic - chemistry Apiaceae - chemistry Deoxycytidine - administration & dosage Deoxycytidine - analogs & derivatives Deoxycytidine - chemistry Drug Carriers - chemistry Drug Carriers - isolation & purification Drug Compounding Drug Liberation gemcitabine Hydrogen-Ion Concentration lung cancer Microspheres Plant Roots - chemistry release Saponins - chemistry Saponins - isolation & purification Spectroscopy, Fourier Transform Infrared Surface Properties triterpene saponins Triterpenes - chemistry Triterpenes - isolation & purification |
| title | Novel microspheres based on triterpene saponins from the roots of Physospermum verticillatum (Waldst & Kit) (Apiaceae) for the improvement of gemcitabine release |
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