Preparation of albumin nanospheres loaded with gemcitabine and their cytotoxicity against BXPC-3 cells in vitro
Aim: To optimize formulation methods for loading gemcitabine (GEM), the main drug against pancreatic cancer, into albumin nanoparticles for extended blood circulation and improved efficacy. Methods: GEM was loaded into two sizes of disolvation-crosslinked bovine serum albumin nanoparticles, with a m...
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creator | Li, Jin-ming Chen, Wei Wang, Hao Jin, Chen Yu, Xian-jun Lu, Wei-yue Cui, Long Fu, De-liang Ni, Quan-xing Hou, Hui-min |
description | Aim: To optimize formulation methods for loading gemcitabine (GEM), the main drug against pancreatic cancer, into albumin nanoparticles for extended blood circulation and improved efficacy. Methods: GEM was loaded into two sizes of disolvation-crosslinked bovine serum albumin nanoparticles, with a mean diameter of 109.7 nm and 405.6 nm, respectively, by corecipitation (the direct method) and follow-up adsorption (the indirect method). The antitumor activities of the two nanoparticulate formulations, were evaluated according to their anti-proliferative effects on the human pan- creatic cell line BXPC-3, which were assessed using the MTT assay. Results: The two nanoparticulate formulations, created by direct co-precipitation and indirect adsorption, possessed smooth surfaces and high drug loading efficiencies, 83% and 93% at 11% and 13% drug loading, respectively. The two formulations released GEM for 8 and 12 h, respectively, and significantly improved anti-BXPC-3 proliferation effects, as compared with the GEM solution and the drugfree albumin particles. Conclusion: Co-precipitating and adsorbing GEM into albumin particles resulted in sustained-release nanoparticulate formulations with improved antitumor cytotoxicity. The result suggests that this is a useful formulation strategy for improving the antitumor efficacy of GEM. |
doi_str_mv | 10.1038/aps.2009.125 |
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Methods: GEM was loaded into two sizes of disolvation-crosslinked bovine serum albumin nanoparticles, with a mean diameter of 109.7 nm and 405.6 nm, respectively, by corecipitation (the direct method) and follow-up adsorption (the indirect method). The antitumor activities of the two nanoparticulate formulations, were evaluated according to their anti-proliferative effects on the human pan- creatic cell line BXPC-3, which were assessed using the MTT assay. Results: The two nanoparticulate formulations, created by direct co-precipitation and indirect adsorption, possessed smooth surfaces and high drug loading efficiencies, 83% and 93% at 11% and 13% drug loading, respectively. The two formulations released GEM for 8 and 12 h, respectively, and significantly improved anti-BXPC-3 proliferation effects, as compared with the GEM solution and the drugfree albumin particles. Conclusion: Co-precipitating and adsorbing GEM into albumin particles resulted in sustained-release nanoparticulate formulations with improved antitumor cytotoxicity. The result suggests that this is a useful formulation strategy for improving the antitumor efficacy of GEM.</description><identifier>ISSN: 1671-4083</identifier><identifier>EISSN: 1745-7254</identifier><identifier>DOI: 10.1038/aps.2009.125</identifier><identifier>PMID: 19730429</identifier><language>eng</language><publisher>London: Nature Publishing Group UK</publisher><subject>Antimetabolites, Antineoplastic - administration & dosage ; Antimetabolites, Antineoplastic - therapeutic use ; Biomedical and Life Sciences ; Biomedicine ; Deoxycytidine - administration & dosage ; Deoxycytidine - analogs & derivatives ; Deoxycytidine - therapeutic use ; Drug Carriers - therapeutic use ; Humans ; Immunology ; Internal Medicine ; Medical Microbiology ; Nanocapsules - therapeutic use ; Nanospheres - therapeutic use ; Original ; original-article ; Pancreatic Neoplasms - drug therapy ; Pharmacology/Toxicology ; Serum Albumin, Bovine - metabolism ; Tumor Cells, Cultured ; Vaccine ; 抗肿瘤活性 ; 牛血清白蛋白 ; 纳米球 ; 纳米粒子 ; 细胞株 ; 胰腺癌</subject><ispartof>Acta pharmacologica Sinica, 2009-09, Vol.30 (9), p.1337-1343</ispartof><rights>CPS and SIMM 2009</rights><rights>Copyright Nature Publishing Group Sep 2009</rights><rights>Copyright © 2009 CPS and SIMM 2009 CPS and SIMM</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c475t-7cfc9f4b31e39b28ceeb876805e6ad985519ab2eb664d776bd488c2a364f8fed3</citedby><cites>FETCH-LOGICAL-c475t-7cfc9f4b31e39b28ceeb876805e6ad985519ab2eb664d776bd488c2a364f8fed3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Uhttp://image.cqvip.com/vip1000/qk/95561A/95561A.jpg</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4007180/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4007180/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,723,776,780,881,27901,27902,53766,53768</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19730429$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Li, Jin-ming</creatorcontrib><creatorcontrib>Chen, Wei</creatorcontrib><creatorcontrib>Wang, Hao</creatorcontrib><creatorcontrib>Jin, Chen</creatorcontrib><creatorcontrib>Yu, Xian-jun</creatorcontrib><creatorcontrib>Lu, Wei-yue</creatorcontrib><creatorcontrib>Cui, Long</creatorcontrib><creatorcontrib>Fu, De-liang</creatorcontrib><creatorcontrib>Ni, Quan-xing</creatorcontrib><creatorcontrib>Hou, Hui-min</creatorcontrib><title>Preparation of albumin nanospheres loaded with gemcitabine and their cytotoxicity against BXPC-3 cells in vitro</title><title>Acta pharmacologica Sinica</title><addtitle>Acta Pharmacol Sin</addtitle><addtitle>Acta Pharmacologica Sinica</addtitle><description>Aim: To optimize formulation methods for loading gemcitabine (GEM), the main drug against pancreatic cancer, into albumin nanoparticles for extended blood circulation and improved efficacy. Methods: GEM was loaded into two sizes of disolvation-crosslinked bovine serum albumin nanoparticles, with a mean diameter of 109.7 nm and 405.6 nm, respectively, by corecipitation (the direct method) and follow-up adsorption (the indirect method). The antitumor activities of the two nanoparticulate formulations, were evaluated according to their anti-proliferative effects on the human pan- creatic cell line BXPC-3, which were assessed using the MTT assay. Results: The two nanoparticulate formulations, created by direct co-precipitation and indirect adsorption, possessed smooth surfaces and high drug loading efficiencies, 83% and 93% at 11% and 13% drug loading, respectively. The two formulations released GEM for 8 and 12 h, respectively, and significantly improved anti-BXPC-3 proliferation effects, as compared with the GEM solution and the drugfree albumin particles. Conclusion: Co-precipitating and adsorbing GEM into albumin particles resulted in sustained-release nanoparticulate formulations with improved antitumor cytotoxicity. The result suggests that this is a useful formulation strategy for improving the antitumor efficacy of GEM.</description><subject>Antimetabolites, Antineoplastic - administration & dosage</subject><subject>Antimetabolites, Antineoplastic - therapeutic use</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Deoxycytidine - administration & dosage</subject><subject>Deoxycytidine - analogs & derivatives</subject><subject>Deoxycytidine - therapeutic use</subject><subject>Drug Carriers - therapeutic use</subject><subject>Humans</subject><subject>Immunology</subject><subject>Internal Medicine</subject><subject>Medical Microbiology</subject><subject>Nanocapsules - therapeutic use</subject><subject>Nanospheres - therapeutic use</subject><subject>Original</subject><subject>original-article</subject><subject>Pancreatic Neoplasms - drug therapy</subject><subject>Pharmacology/Toxicology</subject><subject>Serum Albumin, Bovine - metabolism</subject><subject>Tumor Cells, Cultured</subject><subject>Vaccine</subject><subject>抗肿瘤活性</subject><subject>牛血清白蛋白</subject><subject>纳米球</subject><subject>纳米粒子</subject><subject>细胞株</subject><subject>胰腺癌</subject><issn>1671-4083</issn><issn>1745-7254</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>BENPR</sourceid><recordid>eNp1kc2LFDEQxRtR3HX15lmCZ3vMZyd9EXRwVVhwDwreQpKu7s7ak8wmmdX57zfDDK4ePFXB-9WrB69pXhK8Ipipt2abVxTjfkWoeNScE8lFK6ngj-veSdJyrNhZ8yznG4wZZaR_2pyRXjLMaX_exOsEW5NM8TGgOCKz2N3GBxRMiHk7Q4KMlmgGGNAvX2Y0wcb5YqwPgEwYUJnBJ-T2JZb421dpj8xkfMgFffhxvW4ZcrAsGVXLO19SfN48Gc2S4cVpXjTfLz9-W39ur75--rJ-f9U6LkVppRtdP3LLCLDeUuUArJKdwgI6M_RKCNIbS8F2HR-k7OzAlXLUsI6PaoSBXTTvjr7bnd3A4CCUZBa9TX5j0l5H4_W_SvCznuKd5hhLonA1eH0ySPF2B7nom7hLoWbWlDBMOyEO0Jsj5FLMOcH45wHB-tCOru3oQzu6tlPxV3-HeoBPdVSgPQK5SmGC9PD0P4ankG6OYbqtJ9oa93P0C2hGBFFcdeweahSoQw</recordid><startdate>20090901</startdate><enddate>20090901</enddate><creator>Li, 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of albumin nanospheres loaded with gemcitabine and their cytotoxicity against BXPC-3 cells in vitro</title><author>Li, Jin-ming ; Chen, Wei ; Wang, Hao ; Jin, Chen ; Yu, Xian-jun ; Lu, Wei-yue ; Cui, Long ; Fu, De-liang ; Ni, Quan-xing ; Hou, Hui-min</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c475t-7cfc9f4b31e39b28ceeb876805e6ad985519ab2eb664d776bd488c2a364f8fed3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Antimetabolites, Antineoplastic - administration & dosage</topic><topic>Antimetabolites, Antineoplastic - therapeutic use</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Deoxycytidine - administration & dosage</topic><topic>Deoxycytidine - analogs & derivatives</topic><topic>Deoxycytidine - therapeutic use</topic><topic>Drug Carriers - therapeutic use</topic><topic>Humans</topic><topic>Immunology</topic><topic>Internal Medicine</topic><topic>Medical Microbiology</topic><topic>Nanocapsules - therapeutic use</topic><topic>Nanospheres - therapeutic use</topic><topic>Original</topic><topic>original-article</topic><topic>Pancreatic Neoplasms - drug therapy</topic><topic>Pharmacology/Toxicology</topic><topic>Serum Albumin, Bovine - metabolism</topic><topic>Tumor Cells, Cultured</topic><topic>Vaccine</topic><topic>抗肿瘤活性</topic><topic>牛血清白蛋白</topic><topic>纳米球</topic><topic>纳米粒子</topic><topic>细胞株</topic><topic>胰腺癌</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Li, Jin-ming</creatorcontrib><creatorcontrib>Chen, Wei</creatorcontrib><creatorcontrib>Wang, Hao</creatorcontrib><creatorcontrib>Jin, Chen</creatorcontrib><creatorcontrib>Yu, Xian-jun</creatorcontrib><creatorcontrib>Lu, Wei-yue</creatorcontrib><creatorcontrib>Cui, Long</creatorcontrib><creatorcontrib>Fu, De-liang</creatorcontrib><creatorcontrib>Ni, Quan-xing</creatorcontrib><creatorcontrib>Hou, 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Sinica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Li, Jin-ming</au><au>Chen, Wei</au><au>Wang, Hao</au><au>Jin, Chen</au><au>Yu, Xian-jun</au><au>Lu, Wei-yue</au><au>Cui, Long</au><au>Fu, De-liang</au><au>Ni, Quan-xing</au><au>Hou, Hui-min</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Preparation of albumin nanospheres loaded with gemcitabine and their cytotoxicity against BXPC-3 cells in vitro</atitle><jtitle>Acta pharmacologica Sinica</jtitle><stitle>Acta Pharmacol Sin</stitle><addtitle>Acta Pharmacologica Sinica</addtitle><date>2009-09-01</date><risdate>2009</risdate><volume>30</volume><issue>9</issue><spage>1337</spage><epage>1343</epage><pages>1337-1343</pages><issn>1671-4083</issn><eissn>1745-7254</eissn><abstract>Aim: To optimize formulation methods for loading gemcitabine (GEM), the main drug against pancreatic cancer, into albumin nanoparticles for extended blood circulation and improved efficacy. Methods: GEM was loaded into two sizes of disolvation-crosslinked bovine serum albumin nanoparticles, with a mean diameter of 109.7 nm and 405.6 nm, respectively, by corecipitation (the direct method) and follow-up adsorption (the indirect method). The antitumor activities of the two nanoparticulate formulations, were evaluated according to their anti-proliferative effects on the human pan- creatic cell line BXPC-3, which were assessed using the MTT assay. Results: The two nanoparticulate formulations, created by direct co-precipitation and indirect adsorption, possessed smooth surfaces and high drug loading efficiencies, 83% and 93% at 11% and 13% drug loading, respectively. The two formulations released GEM for 8 and 12 h, respectively, and significantly improved anti-BXPC-3 proliferation effects, as compared with the GEM solution and the drugfree albumin particles. Conclusion: Co-precipitating and adsorbing GEM into albumin particles resulted in sustained-release nanoparticulate formulations with improved antitumor cytotoxicity. The result suggests that this is a useful formulation strategy for improving the antitumor efficacy of GEM.</abstract><cop>London</cop><pub>Nature Publishing Group UK</pub><pmid>19730429</pmid><doi>10.1038/aps.2009.125</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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subjects | Antimetabolites, Antineoplastic - administration & dosage Antimetabolites, Antineoplastic - therapeutic use Biomedical and Life Sciences Biomedicine Deoxycytidine - administration & dosage Deoxycytidine - analogs & derivatives Deoxycytidine - therapeutic use Drug Carriers - therapeutic use Humans Immunology Internal Medicine Medical Microbiology Nanocapsules - therapeutic use Nanospheres - therapeutic use Original original-article Pancreatic Neoplasms - drug therapy Pharmacology/Toxicology Serum Albumin, Bovine - metabolism Tumor Cells, Cultured Vaccine 抗肿瘤活性 牛血清白蛋白 纳米球 纳米粒子 细胞株 胰腺癌 |
title | Preparation of albumin nanospheres loaded with gemcitabine and their cytotoxicity against BXPC-3 cells in vitro |
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