Formulation optimization of Docetaxel loaded self-emulsifying drug delivery system to enhance bioavailability and anti-tumor activity
Poor bioavailability of Docetaxel (DCT) arising due to its low aqueous solubility and permeability limits its clinical utility. The aim of the present study was to develop DCT loaded self-emulsified drug delivery systems (D-SEDDS) and evaluate its potential ability to improve the oral bioavailabilit...
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| Veröffentlicht in: | Scientific reports 2016-05, Vol.6 (1), p.26895-26895, Article 26895 |
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| creator | Valicherla, Guru R. Dave, Kandarp M. Syed, Anees A. Riyazuddin, Mohammed Gupta, Anand P. Singh, Akhilesh Wahajuddin Mitra, Kalyan Datta, Dipak Gayen, Jiaur R. |
| description | Poor bioavailability of Docetaxel (DCT) arising due to its low aqueous solubility and permeability limits its clinical utility. The aim of the present study was to develop DCT loaded self-emulsified drug delivery systems (D-SEDDS) and evaluate its potential ability to improve the oral bioavailability and therapeutic efficacy of DCT. D-SEDDS were characterized for their
in vitro
antitumor activity,
in situ
single pass intestinal perfusion (SPIP), bioavailability, chylomicron flow blocking study and bio-distribution profile. The D-SEDDS were prepared using Capryol 90, Vitamin E TPGS, Gelucire 44/14 and Transcutol HP with a ratio of 32.7/29.4/8.3/29.6 using D-Optimal Mixture Design. The solubility of DCT was improved upto 50 mg/mL. The oral bioavailability of the D-SEDDS in rats (21.84 ± 3.12%) was increased by 3.19 fold than orally administered Taxotere (6.85 ± 1.82%). The enhanced bioavailability was probably due to increase in solubility and permeability. In SPIP, effective permeability of D-SEDDS was significantly higher than Taxotere. D-SEDDS showed 25 fold more
in vitro
cytotoxic activity compared to free DCT. Chylomicron flow blocking study and tissue distribution demonstrated the intestinal lymphatic transport of D-SEDDS and higher retention in tumor than Taxotere. The data suggests that D-SEDDS showed desired stability, enhanced oral bioavailability and
in vitro
antitumor efficacy. |
| doi_str_mv | 10.1038/srep26895 |
| format | Article |
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in vitro
antitumor activity,
in situ
single pass intestinal perfusion (SPIP), bioavailability, chylomicron flow blocking study and bio-distribution profile. The D-SEDDS were prepared using Capryol 90, Vitamin E TPGS, Gelucire 44/14 and Transcutol HP with a ratio of 32.7/29.4/8.3/29.6 using D-Optimal Mixture Design. The solubility of DCT was improved upto 50 mg/mL. The oral bioavailability of the D-SEDDS in rats (21.84 ± 3.12%) was increased by 3.19 fold than orally administered Taxotere (6.85 ± 1.82%). The enhanced bioavailability was probably due to increase in solubility and permeability. In SPIP, effective permeability of D-SEDDS was significantly higher than Taxotere. D-SEDDS showed 25 fold more
in vitro
cytotoxic activity compared to free DCT. Chylomicron flow blocking study and tissue distribution demonstrated the intestinal lymphatic transport of D-SEDDS and higher retention in tumor than Taxotere. The data suggests that D-SEDDS showed desired stability, enhanced oral bioavailability and
in vitro
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in vitro
antitumor activity,
in situ
single pass intestinal perfusion (SPIP), bioavailability, chylomicron flow blocking study and bio-distribution profile. The D-SEDDS were prepared using Capryol 90, Vitamin E TPGS, Gelucire 44/14 and Transcutol HP with a ratio of 32.7/29.4/8.3/29.6 using D-Optimal Mixture Design. The solubility of DCT was improved upto 50 mg/mL. The oral bioavailability of the D-SEDDS in rats (21.84 ± 3.12%) was increased by 3.19 fold than orally administered Taxotere (6.85 ± 1.82%). The enhanced bioavailability was probably due to increase in solubility and permeability. In SPIP, effective permeability of D-SEDDS was significantly higher than Taxotere. D-SEDDS showed 25 fold more
in vitro
cytotoxic activity compared to free DCT. Chylomicron flow blocking study and tissue distribution demonstrated the intestinal lymphatic transport of D-SEDDS and higher retention in tumor than Taxotere. The data suggests that D-SEDDS showed desired stability, enhanced oral bioavailability and
in vitro
antitumor efficacy.</description><subject>101/58</subject><subject>13</subject><subject>13/106</subject><subject>Humanities and Social Sciences</subject><subject>multidisciplinary</subject><subject>Science</subject><issn>2045-2322</issn><issn>2045-2322</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>C6C</sourceid><recordid>eNptkVFLHDEQx0OpVFEf-gVKHtvC6iabvey-FORarSD4os9hdjN7RrLJNckebt_93o3c9VAwkMwk8-M_Sf6EfGblGSur5jwGXPNF09YfyBEvRV3wivOPr_JDchrjY5lHzVvB2k_kkEsuWCPlEXm-9GGcLCTjHfXrZEbzd7cZ6E_fY4IntNR60KhpRDsUmPlohtm4FdVhygtas8Ew0zjHhCNNnqJ7ANcj7YyHDRgLnbEmzRSczjOZIk2jDxT6ZDb5_IQcDGAjnu7iMbm__HW3_F3c3F5dLy9uil7IRSqAI3bVwKSWGoG1XHTQ6bZERF13pRSQ3zSIGhuJmtWDQNaIXgLyBeuqCqtj8mOru566EXWPLgWwah3MCGFWHox6W3HmQa38RommWfC6zQJfdwLB_5kwJjWa2KO14NBPUTHZVpwJ2YqMftuiffAxmzTs27BSvTin9s5l9svre-3J_z5l4PsWiLnkVhjUo5-Cy3_1jto_pGqotw</recordid><startdate>20160531</startdate><enddate>20160531</enddate><creator>Valicherla, Guru R.</creator><creator>Dave, Kandarp M.</creator><creator>Syed, Anees A.</creator><creator>Riyazuddin, Mohammed</creator><creator>Gupta, Anand P.</creator><creator>Singh, Akhilesh</creator><creator>Wahajuddin</creator><creator>Mitra, Kalyan</creator><creator>Datta, Dipak</creator><creator>Gayen, Jiaur R.</creator><general>Nature Publishing Group UK</general><general>Nature Publishing Group</general><scope>C6C</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>20160531</creationdate><title>Formulation optimization of Docetaxel loaded self-emulsifying drug delivery system to enhance bioavailability and anti-tumor activity</title><author>Valicherla, Guru R. ; Dave, Kandarp M. ; Syed, Anees A. ; Riyazuddin, Mohammed ; Gupta, Anand P. ; Singh, Akhilesh ; Wahajuddin ; Mitra, Kalyan ; Datta, Dipak ; Gayen, Jiaur R.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c476t-a2eeb3f17d7dea1924babd90eeed5b074a877f45e87ed15f4e184c7ae261b33e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>101/58</topic><topic>13</topic><topic>13/106</topic><topic>Humanities and Social Sciences</topic><topic>multidisciplinary</topic><topic>Science</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Valicherla, Guru R.</creatorcontrib><creatorcontrib>Dave, Kandarp M.</creatorcontrib><creatorcontrib>Syed, Anees A.</creatorcontrib><creatorcontrib>Riyazuddin, Mohammed</creatorcontrib><creatorcontrib>Gupta, Anand P.</creatorcontrib><creatorcontrib>Singh, Akhilesh</creatorcontrib><creatorcontrib>Wahajuddin</creatorcontrib><creatorcontrib>Mitra, Kalyan</creatorcontrib><creatorcontrib>Datta, Dipak</creatorcontrib><creatorcontrib>Gayen, Jiaur R.</creatorcontrib><collection>Springer Nature OA Free Journals</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Scientific reports</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Valicherla, Guru R.</au><au>Dave, Kandarp M.</au><au>Syed, Anees A.</au><au>Riyazuddin, Mohammed</au><au>Gupta, Anand P.</au><au>Singh, Akhilesh</au><au>Wahajuddin</au><au>Mitra, Kalyan</au><au>Datta, Dipak</au><au>Gayen, Jiaur R.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Formulation optimization of Docetaxel loaded self-emulsifying drug delivery system to enhance bioavailability and anti-tumor activity</atitle><jtitle>Scientific reports</jtitle><stitle>Sci Rep</stitle><addtitle>Sci Rep</addtitle><date>2016-05-31</date><risdate>2016</risdate><volume>6</volume><issue>1</issue><spage>26895</spage><epage>26895</epage><pages>26895-26895</pages><artnum>26895</artnum><issn>2045-2322</issn><eissn>2045-2322</eissn><abstract>Poor bioavailability of Docetaxel (DCT) arising due to its low aqueous solubility and permeability limits its clinical utility. The aim of the present study was to develop DCT loaded self-emulsified drug delivery systems (D-SEDDS) and evaluate its potential ability to improve the oral bioavailability and therapeutic efficacy of DCT. D-SEDDS were characterized for their
in vitro
antitumor activity,
in situ
single pass intestinal perfusion (SPIP), bioavailability, chylomicron flow blocking study and bio-distribution profile. The D-SEDDS were prepared using Capryol 90, Vitamin E TPGS, Gelucire 44/14 and Transcutol HP with a ratio of 32.7/29.4/8.3/29.6 using D-Optimal Mixture Design. The solubility of DCT was improved upto 50 mg/mL. The oral bioavailability of the D-SEDDS in rats (21.84 ± 3.12%) was increased by 3.19 fold than orally administered Taxotere (6.85 ± 1.82%). The enhanced bioavailability was probably due to increase in solubility and permeability. In SPIP, effective permeability of D-SEDDS was significantly higher than Taxotere. D-SEDDS showed 25 fold more
in vitro
cytotoxic activity compared to free DCT. Chylomicron flow blocking study and tissue distribution demonstrated the intestinal lymphatic transport of D-SEDDS and higher retention in tumor than Taxotere. The data suggests that D-SEDDS showed desired stability, enhanced oral bioavailability and
in vitro
antitumor efficacy.</abstract><cop>London</cop><pub>Nature Publishing Group UK</pub><pmid>27241877</pmid><doi>10.1038/srep26895</doi><tpages>1</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | 101/58 13 13/106 Humanities and Social Sciences multidisciplinary Science |
| title | Formulation optimization of Docetaxel loaded self-emulsifying drug delivery system to enhance bioavailability and anti-tumor activity |
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