Effect of Hydrophobicity of Core on the Anticancer Efficiency of Micelles as Drug Delivery Carriers
Recently, micelles, which are self-assembled by amphiphilic copolymers, have attracted tremendous attention as promising drug delivery systems for cancer treatment. Thus, the hydrophobic core of the micelles, which could efficiently encapsulate small molecular drug, will play a significant role for...
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| Veröffentlicht in: | ACS applied materials & interfaces 2014-12, Vol.6 (24), p.22709-22718 |
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| container_title | ACS applied materials & interfaces |
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| creator | Sun, Chun-Yang Ma, Yin-Chu Cao, Zi-Yang Li, Dong-Dong Fan, Feng Wang, Jun-Xia Tao, Wei Yang, Xian-Zhu |
| description | Recently, micelles, which are self-assembled by amphiphilic copolymers, have attracted tremendous attention as promising drug delivery systems for cancer treatment. Thus, the hydrophobic core of the micelles, which could efficiently encapsulate small molecular drug, will play a significant role for the anticancer efficiency. Unfortunately, the effect of hydrophobicity of micellar core on its anticancer efficiency was rarely reported. Herein, the amphiphilic diblock polymers of poly(ethylene glycol) and polyphosphoester with different side groups (butyl, hexyl, octyl) were synthesized to tune the hydrophobicity of the micellar core. We found that the in vitro cytotoxicity of the DOX-loaded micelles decreased with the increasing hydrophobicity of micellar core due to the drug release rate. However, following systemic delivery, the DOX-loaded micelles with the most hydrophobic core exhibited the most significant inhibition of tumor growth in a MDA-MB-231 tumor model, indicating the importance of hydrophobicity of core on the antitumor efficacy of drug delivery systems. |
| doi_str_mv | 10.1021/am5068723 |
| format | Article |
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Thus, the hydrophobic core of the micelles, which could efficiently encapsulate small molecular drug, will play a significant role for the anticancer efficiency. Unfortunately, the effect of hydrophobicity of micellar core on its anticancer efficiency was rarely reported. Herein, the amphiphilic diblock polymers of poly(ethylene glycol) and polyphosphoester with different side groups (butyl, hexyl, octyl) were synthesized to tune the hydrophobicity of the micellar core. We found that the in vitro cytotoxicity of the DOX-loaded micelles decreased with the increasing hydrophobicity of micellar core due to the drug release rate. However, following systemic delivery, the DOX-loaded micelles with the most hydrophobic core exhibited the most significant inhibition of tumor growth in a MDA-MB-231 tumor model, indicating the importance of hydrophobicity of core on the antitumor efficacy of drug delivery systems.</description><identifier>ISSN: 1944-8244</identifier><identifier>EISSN: 1944-8252</identifier><identifier>DOI: 10.1021/am5068723</identifier><identifier>PMID: 25426800</identifier><language>eng</language><publisher>United States: American Chemical Society</publisher><subject>Animals ; Antibiotics, Antineoplastic - administration & dosage ; Antibiotics, Antineoplastic - chemistry ; Cell Line, Tumor ; Diffusion ; Doxorubicin - administration & dosage ; Doxorubicin - chemistry ; Drug Synergism ; Hydrophobic and Hydrophilic Interactions ; Mice ; Mice, Inbred BALB C ; Mice, Nude ; Micelles ; Nanocapsules - administration & dosage ; Nanocapsules - chemistry ; Nanocapsules - ultrastructure ; Neoplasms, Experimental - drug therapy ; Neoplasms, Experimental - pathology ; Particle Size ; Surface Properties ; Treatment Outcome</subject><ispartof>ACS applied materials & interfaces, 2014-12, Vol.6 (24), p.22709-22718</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-a381t-92ceac1f4ca846619dea31a3e9f339841d9edb2e1bac01e33de46c0ae03727183</citedby><cites>FETCH-LOGICAL-a381t-92ceac1f4ca846619dea31a3e9f339841d9edb2e1bac01e33de46c0ae03727183</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://pubs.acs.org/doi/pdf/10.1021/am5068723$$EPDF$$P50$$Gacs$$H</linktopdf><linktohtml>$$Uhttps://pubs.acs.org/doi/10.1021/am5068723$$EHTML$$P50$$Gacs$$H</linktohtml><link.rule.ids>315,782,786,2769,27085,27933,27934,56747,56797</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/25426800$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Sun, Chun-Yang</creatorcontrib><creatorcontrib>Ma, Yin-Chu</creatorcontrib><creatorcontrib>Cao, Zi-Yang</creatorcontrib><creatorcontrib>Li, Dong-Dong</creatorcontrib><creatorcontrib>Fan, Feng</creatorcontrib><creatorcontrib>Wang, Jun-Xia</creatorcontrib><creatorcontrib>Tao, Wei</creatorcontrib><creatorcontrib>Yang, Xian-Zhu</creatorcontrib><title>Effect of Hydrophobicity of Core on the Anticancer Efficiency of Micelles as Drug Delivery Carriers</title><title>ACS applied materials & interfaces</title><addtitle>ACS Appl. Mater. Interfaces</addtitle><description>Recently, micelles, which are self-assembled by amphiphilic copolymers, have attracted tremendous attention as promising drug delivery systems for cancer treatment. Thus, the hydrophobic core of the micelles, which could efficiently encapsulate small molecular drug, will play a significant role for the anticancer efficiency. Unfortunately, the effect of hydrophobicity of micellar core on its anticancer efficiency was rarely reported. Herein, the amphiphilic diblock polymers of poly(ethylene glycol) and polyphosphoester with different side groups (butyl, hexyl, octyl) were synthesized to tune the hydrophobicity of the micellar core. We found that the in vitro cytotoxicity of the DOX-loaded micelles decreased with the increasing hydrophobicity of micellar core due to the drug release rate. However, following systemic delivery, the DOX-loaded micelles with the most hydrophobic core exhibited the most significant inhibition of tumor growth in a MDA-MB-231 tumor model, indicating the importance of hydrophobicity of core on the antitumor efficacy of drug delivery systems.</description><subject>Animals</subject><subject>Antibiotics, Antineoplastic - administration & dosage</subject><subject>Antibiotics, Antineoplastic - chemistry</subject><subject>Cell Line, Tumor</subject><subject>Diffusion</subject><subject>Doxorubicin - administration & dosage</subject><subject>Doxorubicin - chemistry</subject><subject>Drug Synergism</subject><subject>Hydrophobic and Hydrophilic Interactions</subject><subject>Mice</subject><subject>Mice, Inbred BALB C</subject><subject>Mice, Nude</subject><subject>Micelles</subject><subject>Nanocapsules - administration & dosage</subject><subject>Nanocapsules - chemistry</subject><subject>Nanocapsules - ultrastructure</subject><subject>Neoplasms, Experimental - drug therapy</subject><subject>Neoplasms, Experimental - pathology</subject><subject>Particle Size</subject><subject>Surface Properties</subject><subject>Treatment Outcome</subject><issn>1944-8244</issn><issn>1944-8252</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpt0L1OwzAUBWALgWgpDLwA8oIEQ8B_SZ2xSgtFKmKBOXKca-oqiYudIOXtSWnpxOQr6_PR9UHompIHShh9VHVMEjll_ASNaSpEJFnMTo-zECN0EcKGkIQzEp-jEYsFSyQhY6QXxoBusTN42ZfebdeusNq2_e4mcx6wa3C7BjxrWqtVo8Hj4clAoNG_6NVqqCoIWAU8990nnkNlv8H3OFPeW_DhEp0ZVQW4OpwT9PG0eM-W0ert-SWbrSLFJW2jlGlQmhqhlRRJQtMSFKeKQ2o4T6WgZQplwYAWShMKnJcgEk0UED5lUyr5BN3tc7fefXUQ2ry2YbecasB1IaeJIELyOCUDvd9T7V0IHky-9bZWvs8pyXed5sdOB3tziO2KGsqj_CtxALd7oHTIN67zzfDLf4J-AE0FfN4</recordid><startdate>20141224</startdate><enddate>20141224</enddate><creator>Sun, Chun-Yang</creator><creator>Ma, Yin-Chu</creator><creator>Cao, Zi-Yang</creator><creator>Li, Dong-Dong</creator><creator>Fan, Feng</creator><creator>Wang, Jun-Xia</creator><creator>Tao, Wei</creator><creator>Yang, Xian-Zhu</creator><general>American Chemical Society</general><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>7X8</scope></search><sort><creationdate>20141224</creationdate><title>Effect of Hydrophobicity of Core on the Anticancer Efficiency of Micelles as Drug Delivery Carriers</title><author>Sun, Chun-Yang ; Ma, Yin-Chu ; Cao, Zi-Yang ; Li, Dong-Dong ; Fan, Feng ; Wang, Jun-Xia ; Tao, Wei ; Yang, Xian-Zhu</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-a381t-92ceac1f4ca846619dea31a3e9f339841d9edb2e1bac01e33de46c0ae03727183</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2014</creationdate><topic>Animals</topic><topic>Antibiotics, Antineoplastic - administration & dosage</topic><topic>Antibiotics, Antineoplastic - chemistry</topic><topic>Cell Line, Tumor</topic><topic>Diffusion</topic><topic>Doxorubicin - administration & dosage</topic><topic>Doxorubicin - chemistry</topic><topic>Drug Synergism</topic><topic>Hydrophobic and Hydrophilic Interactions</topic><topic>Mice</topic><topic>Mice, Inbred BALB C</topic><topic>Mice, Nude</topic><topic>Micelles</topic><topic>Nanocapsules - administration & dosage</topic><topic>Nanocapsules - chemistry</topic><topic>Nanocapsules - ultrastructure</topic><topic>Neoplasms, Experimental - drug therapy</topic><topic>Neoplasms, Experimental - pathology</topic><topic>Particle Size</topic><topic>Surface Properties</topic><topic>Treatment Outcome</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Sun, Chun-Yang</creatorcontrib><creatorcontrib>Ma, Yin-Chu</creatorcontrib><creatorcontrib>Cao, Zi-Yang</creatorcontrib><creatorcontrib>Li, Dong-Dong</creatorcontrib><creatorcontrib>Fan, Feng</creatorcontrib><creatorcontrib>Wang, Jun-Xia</creatorcontrib><creatorcontrib>Tao, Wei</creatorcontrib><creatorcontrib>Yang, Xian-Zhu</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>ACS applied materials & interfaces</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Sun, Chun-Yang</au><au>Ma, Yin-Chu</au><au>Cao, Zi-Yang</au><au>Li, Dong-Dong</au><au>Fan, Feng</au><au>Wang, Jun-Xia</au><au>Tao, Wei</au><au>Yang, Xian-Zhu</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of Hydrophobicity of Core on the Anticancer Efficiency of Micelles as Drug Delivery Carriers</atitle><jtitle>ACS applied materials & interfaces</jtitle><addtitle>ACS Appl. Mater. Interfaces</addtitle><date>2014-12-24</date><risdate>2014</risdate><volume>6</volume><issue>24</issue><spage>22709</spage><epage>22718</epage><pages>22709-22718</pages><issn>1944-8244</issn><eissn>1944-8252</eissn><abstract>Recently, micelles, which are self-assembled by amphiphilic copolymers, have attracted tremendous attention as promising drug delivery systems for cancer treatment. Thus, the hydrophobic core of the micelles, which could efficiently encapsulate small molecular drug, will play a significant role for the anticancer efficiency. Unfortunately, the effect of hydrophobicity of micellar core on its anticancer efficiency was rarely reported. Herein, the amphiphilic diblock polymers of poly(ethylene glycol) and polyphosphoester with different side groups (butyl, hexyl, octyl) were synthesized to tune the hydrophobicity of the micellar core. We found that the in vitro cytotoxicity of the DOX-loaded micelles decreased with the increasing hydrophobicity of micellar core due to the drug release rate. However, following systemic delivery, the DOX-loaded micelles with the most hydrophobic core exhibited the most significant inhibition of tumor growth in a MDA-MB-231 tumor model, indicating the importance of hydrophobicity of core on the antitumor efficacy of drug delivery systems.</abstract><cop>United States</cop><pub>American Chemical Society</pub><pmid>25426800</pmid><doi>10.1021/am5068723</doi><tpages>10</tpages></addata></record> |
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| subjects | Animals Antibiotics, Antineoplastic - administration & dosage Antibiotics, Antineoplastic - chemistry Cell Line, Tumor Diffusion Doxorubicin - administration & dosage Doxorubicin - chemistry Drug Synergism Hydrophobic and Hydrophilic Interactions Mice Mice, Inbred BALB C Mice, Nude Micelles Nanocapsules - administration & dosage Nanocapsules - chemistry Nanocapsules - ultrastructure Neoplasms, Experimental - drug therapy Neoplasms, Experimental - pathology Particle Size Surface Properties Treatment Outcome |
| title | Effect of Hydrophobicity of Core on the Anticancer Efficiency of Micelles as Drug Delivery Carriers |
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