Preparation of Chondroitin Sulfate-Glycyl-Prednisolone Conjugate Nanogel and Its Efficacy in Rats with Ulcerative Colitis
A conjugate between chondroitin sulfate (CS) and glycyl-prednisolone (GP), named CS-GP, was produced by carbodiimide coupling at a high GP/CS ratio. CS-GP was not water-soluble and gave a nanogel (NG) in aqueous solution. Two types of nanogels, NG(I) and NG(II), with prednisolone (PD) contents of 5....
Gespeichert in:
| Veröffentlicht in: | Biological & pharmaceutical bulletin 2019/07/01, Vol.42(7), pp.1155-1163 |
|---|---|
| Hauptverfasser: | , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 1163 |
|---|---|
| container_issue | 7 |
| container_start_page | 1155 |
| container_title | Biological & pharmaceutical bulletin |
| container_volume | 42 |
| creator | Onishi, Hiraku Ikeuchi-Takahashi, Yuri Kawano, Kumi Hattori, Yoshiyuki |
| description | A conjugate between chondroitin sulfate (CS) and glycyl-prednisolone (GP), named CS-GP, was produced by carbodiimide coupling at a high GP/CS ratio. CS-GP was not water-soluble and gave a nanogel (NG) in aqueous solution. Two types of nanogels, NG(I) and NG(II), with prednisolone (PD) contents of 5.5 and 21.1% (w/w), respectively, were obtained. They had particle sizes of approximately 280 and 570 nm, respectively, and showed negative ζ-potentials of approximately −40 mV. The PD release rate was slower in the nanogels than in a solution of CS-GP with a PD content of 1.4% (w/w). The PD release rate was slower in NG(II) than in NG(I), and was elevated at pH 7.4 than at pH 6.8. NG(II) was applied in vivo to rats with trinitrobenzene sulfonic acid (TNBS)-induced colitis, and its therapeutic efficacy and pharmacokinetic features were investigated. The therapeutic efficacy of NG(II) was slightly better than that of PD alone. Drug delivery to the lower intestines was enhanced with NG(II). The CS-GP nanogel has potential as a potent DDS for the treatment of ulcerative colitis. |
| doi_str_mv | 10.1248/bpb.b19-00020 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_2250629733</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>2314234653</sourcerecordid><originalsourceid>FETCH-LOGICAL-c510t-d55eb5ac15d0f58961cdb98424190c590347aebc881904f822288cdac0720d9c3</originalsourceid><addsrcrecordid>eNpdkc1vFCEYh4nRtGvbo1dD4sULlY9hhzmaSa1NGjXangkDzC4bFlZgaua_l-nWPXiBwPvw8L75AfCO4GtCG_FpOAzXA-kQxpjiV2BFWNMiTgl_DVa4IwKtCRfn4G3Ou4q0mLIzcM4I5S3t6ArMP5I9qKSKiwHGEfbbGEyKrrgAf01-VMWiWz_r2aNKmuBy9DFY2Mewmza1Cr-pEDfWQxUMvCsZ3oyj00rPsBp-qnrxx5UtfPTaLr88LU991edL8GZUPturl_0CPH65eei_ovvvt3f953ukOcEFGc7twJUm3OCRi25NtBk60dCGdFjzDtd5lR20EPXcjIJSKoQ2SuOWYtNpdgE-Hr2HFH9PNhe5d1lb71WwccqSUo7XtGsZq-iH_9BdnFKo3UnKSENZs-YLhY6UTjHnZEd5SG6v0iwJlksmsmYiaybyOZPKv3-xTsPemhP9L4QK9Edgl4va2BOgUnHa22ddQ2W7LCftqaq3Kkkb2F-NBZ_A</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>2314234653</pqid></control><display><type>article</type><title>Preparation of Chondroitin Sulfate-Glycyl-Prednisolone Conjugate Nanogel and Its Efficacy in Rats with Ulcerative Colitis</title><source>MEDLINE</source><source>J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese</source><source>EZB-FREE-00999 freely available EZB journals</source><source>Free Full-Text Journals in Chemistry</source><creator>Onishi, Hiraku ; Ikeuchi-Takahashi, Yuri ; Kawano, Kumi ; Hattori, Yoshiyuki</creator><creatorcontrib>Onishi, Hiraku ; Ikeuchi-Takahashi, Yuri ; Kawano, Kumi ; Hattori, Yoshiyuki</creatorcontrib><description>A conjugate between chondroitin sulfate (CS) and glycyl-prednisolone (GP), named CS-GP, was produced by carbodiimide coupling at a high GP/CS ratio. CS-GP was not water-soluble and gave a nanogel (NG) in aqueous solution. Two types of nanogels, NG(I) and NG(II), with prednisolone (PD) contents of 5.5 and 21.1% (w/w), respectively, were obtained. They had particle sizes of approximately 280 and 570 nm, respectively, and showed negative ζ-potentials of approximately −40 mV. The PD release rate was slower in the nanogels than in a solution of CS-GP with a PD content of 1.4% (w/w). The PD release rate was slower in NG(II) than in NG(I), and was elevated at pH 7.4 than at pH 6.8. NG(II) was applied in vivo to rats with trinitrobenzene sulfonic acid (TNBS)-induced colitis, and its therapeutic efficacy and pharmacokinetic features were investigated. The therapeutic efficacy of NG(II) was slightly better than that of PD alone. Drug delivery to the lower intestines was enhanced with NG(II). The CS-GP nanogel has potential as a potent DDS for the treatment of ulcerative colitis.</description><identifier>ISSN: 0918-6158</identifier><identifier>EISSN: 1347-5215</identifier><identifier>DOI: 10.1248/bpb.b19-00020</identifier><identifier>PMID: 31257292</identifier><language>eng</language><publisher>Japan: The Pharmaceutical Society of Japan</publisher><subject>Animals ; Anti-Inflammatory Agents - administration & dosage ; Anti-Inflammatory Agents - chemistry ; Anti-Inflammatory Agents - pharmacokinetics ; Carbodiimide ; Chondroitin sulfate ; chondroitin sulfate-glycyl-prednisolone conjugate ; Chondroitin Sulfates - administration & dosage ; Chondroitin Sulfates - chemistry ; Chondroitin Sulfates - pharmacokinetics ; Colitis, Ulcerative - drug therapy ; Colitis, Ulcerative - metabolism ; Colitis, Ulcerative - pathology ; Colon ; Colon - drug effects ; Colon - pathology ; Conjugates ; Drug delivery ; Drug Delivery Systems ; Drug Liberation ; efficacy ; Gels ; in vitro release ; Inflammatory bowel disease ; Intestinal Mucosa - metabolism ; Intestine ; Male ; nanogel ; Nanoparticles - administration & dosage ; Nanoparticles - chemistry ; particle characteristics ; pH effects ; Prednisolone ; Prednisolone - administration & dosage ; Prednisolone - chemistry ; Prednisolone - pharmacokinetics ; Rats, Wistar ; Sulfates ; Sulfonic acid ; Ulcerative colitis</subject><ispartof>Biological and Pharmaceutical Bulletin, 2019/07/01, Vol.42(7), pp.1155-1163</ispartof><rights>2019 The Pharmaceutical Society of Japan</rights><rights>Copyright Japan Science and Technology Agency 2019</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c510t-d55eb5ac15d0f58961cdb98424190c590347aebc881904f822288cdac0720d9c3</citedby><cites>FETCH-LOGICAL-c510t-d55eb5ac15d0f58961cdb98424190c590347aebc881904f822288cdac0720d9c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,1877,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/31257292$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Onishi, Hiraku</creatorcontrib><creatorcontrib>Ikeuchi-Takahashi, Yuri</creatorcontrib><creatorcontrib>Kawano, Kumi</creatorcontrib><creatorcontrib>Hattori, Yoshiyuki</creatorcontrib><title>Preparation of Chondroitin Sulfate-Glycyl-Prednisolone Conjugate Nanogel and Its Efficacy in Rats with Ulcerative Colitis</title><title>Biological & pharmaceutical bulletin</title><addtitle>Biol Pharm Bull</addtitle><description>A conjugate between chondroitin sulfate (CS) and glycyl-prednisolone (GP), named CS-GP, was produced by carbodiimide coupling at a high GP/CS ratio. CS-GP was not water-soluble and gave a nanogel (NG) in aqueous solution. Two types of nanogels, NG(I) and NG(II), with prednisolone (PD) contents of 5.5 and 21.1% (w/w), respectively, were obtained. They had particle sizes of approximately 280 and 570 nm, respectively, and showed negative ζ-potentials of approximately −40 mV. The PD release rate was slower in the nanogels than in a solution of CS-GP with a PD content of 1.4% (w/w). The PD release rate was slower in NG(II) than in NG(I), and was elevated at pH 7.4 than at pH 6.8. NG(II) was applied in vivo to rats with trinitrobenzene sulfonic acid (TNBS)-induced colitis, and its therapeutic efficacy and pharmacokinetic features were investigated. The therapeutic efficacy of NG(II) was slightly better than that of PD alone. Drug delivery to the lower intestines was enhanced with NG(II). The CS-GP nanogel has potential as a potent DDS for the treatment of ulcerative colitis.</description><subject>Animals</subject><subject>Anti-Inflammatory Agents - administration & dosage</subject><subject>Anti-Inflammatory Agents - chemistry</subject><subject>Anti-Inflammatory Agents - pharmacokinetics</subject><subject>Carbodiimide</subject><subject>Chondroitin sulfate</subject><subject>chondroitin sulfate-glycyl-prednisolone conjugate</subject><subject>Chondroitin Sulfates - administration & dosage</subject><subject>Chondroitin Sulfates - chemistry</subject><subject>Chondroitin Sulfates - pharmacokinetics</subject><subject>Colitis, Ulcerative - drug therapy</subject><subject>Colitis, Ulcerative - metabolism</subject><subject>Colitis, Ulcerative - pathology</subject><subject>Colon</subject><subject>Colon - drug effects</subject><subject>Colon - pathology</subject><subject>Conjugates</subject><subject>Drug delivery</subject><subject>Drug Delivery Systems</subject><subject>Drug Liberation</subject><subject>efficacy</subject><subject>Gels</subject><subject>in vitro release</subject><subject>Inflammatory bowel disease</subject><subject>Intestinal Mucosa - metabolism</subject><subject>Intestine</subject><subject>Male</subject><subject>nanogel</subject><subject>Nanoparticles - administration & dosage</subject><subject>Nanoparticles - chemistry</subject><subject>particle characteristics</subject><subject>pH effects</subject><subject>Prednisolone</subject><subject>Prednisolone - administration & dosage</subject><subject>Prednisolone - chemistry</subject><subject>Prednisolone - pharmacokinetics</subject><subject>Rats, Wistar</subject><subject>Sulfates</subject><subject>Sulfonic acid</subject><subject>Ulcerative colitis</subject><issn>0918-6158</issn><issn>1347-5215</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2019</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpdkc1vFCEYh4nRtGvbo1dD4sULlY9hhzmaSa1NGjXangkDzC4bFlZgaua_l-nWPXiBwPvw8L75AfCO4GtCG_FpOAzXA-kQxpjiV2BFWNMiTgl_DVa4IwKtCRfn4G3Ou4q0mLIzcM4I5S3t6ArMP5I9qKSKiwHGEfbbGEyKrrgAf01-VMWiWz_r2aNKmuBy9DFY2Mewmza1Cr-pEDfWQxUMvCsZ3oyj00rPsBp-qnrxx5UtfPTaLr88LU991edL8GZUPturl_0CPH65eei_ovvvt3f953ukOcEFGc7twJUm3OCRi25NtBk60dCGdFjzDtd5lR20EPXcjIJSKoQ2SuOWYtNpdgE-Hr2HFH9PNhe5d1lb71WwccqSUo7XtGsZq-iH_9BdnFKo3UnKSENZs-YLhY6UTjHnZEd5SG6v0iwJlksmsmYiaybyOZPKv3-xTsPemhP9L4QK9Edgl4va2BOgUnHa22ddQ2W7LCftqaq3Kkkb2F-NBZ_A</recordid><startdate>20190701</startdate><enddate>20190701</enddate><creator>Onishi, Hiraku</creator><creator>Ikeuchi-Takahashi, Yuri</creator><creator>Kawano, Kumi</creator><creator>Hattori, Yoshiyuki</creator><general>The Pharmaceutical Society of Japan</general><general>Japan Science and Technology Agency</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>7QP</scope><scope>7QR</scope><scope>7TK</scope><scope>7U9</scope><scope>8FD</scope><scope>FR3</scope><scope>H94</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20190701</creationdate><title>Preparation of Chondroitin Sulfate-Glycyl-Prednisolone Conjugate Nanogel and Its Efficacy in Rats with Ulcerative Colitis</title><author>Onishi, Hiraku ; Ikeuchi-Takahashi, Yuri ; Kawano, Kumi ; Hattori, Yoshiyuki</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c510t-d55eb5ac15d0f58961cdb98424190c590347aebc881904f822288cdac0720d9c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2019</creationdate><topic>Animals</topic><topic>Anti-Inflammatory Agents - administration & dosage</topic><topic>Anti-Inflammatory Agents - chemistry</topic><topic>Anti-Inflammatory Agents - pharmacokinetics</topic><topic>Carbodiimide</topic><topic>Chondroitin sulfate</topic><topic>chondroitin sulfate-glycyl-prednisolone conjugate</topic><topic>Chondroitin Sulfates - administration & dosage</topic><topic>Chondroitin Sulfates - chemistry</topic><topic>Chondroitin Sulfates - pharmacokinetics</topic><topic>Colitis, Ulcerative - drug therapy</topic><topic>Colitis, Ulcerative - metabolism</topic><topic>Colitis, Ulcerative - pathology</topic><topic>Colon</topic><topic>Colon - drug effects</topic><topic>Colon - pathology</topic><topic>Conjugates</topic><topic>Drug delivery</topic><topic>Drug Delivery Systems</topic><topic>Drug Liberation</topic><topic>efficacy</topic><topic>Gels</topic><topic>in vitro release</topic><topic>Inflammatory bowel disease</topic><topic>Intestinal Mucosa - metabolism</topic><topic>Intestine</topic><topic>Male</topic><topic>nanogel</topic><topic>Nanoparticles - administration & dosage</topic><topic>Nanoparticles - chemistry</topic><topic>particle characteristics</topic><topic>pH effects</topic><topic>Prednisolone</topic><topic>Prednisolone - administration & dosage</topic><topic>Prednisolone - chemistry</topic><topic>Prednisolone - pharmacokinetics</topic><topic>Rats, Wistar</topic><topic>Sulfates</topic><topic>Sulfonic acid</topic><topic>Ulcerative colitis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Onishi, Hiraku</creatorcontrib><creatorcontrib>Ikeuchi-Takahashi, Yuri</creatorcontrib><creatorcontrib>Kawano, Kumi</creatorcontrib><creatorcontrib>Hattori, Yoshiyuki</creatorcontrib><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>Chemoreception Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Biological & pharmaceutical bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Onishi, Hiraku</au><au>Ikeuchi-Takahashi, Yuri</au><au>Kawano, Kumi</au><au>Hattori, Yoshiyuki</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Preparation of Chondroitin Sulfate-Glycyl-Prednisolone Conjugate Nanogel and Its Efficacy in Rats with Ulcerative Colitis</atitle><jtitle>Biological & pharmaceutical bulletin</jtitle><addtitle>Biol Pharm Bull</addtitle><date>2019-07-01</date><risdate>2019</risdate><volume>42</volume><issue>7</issue><spage>1155</spage><epage>1163</epage><pages>1155-1163</pages><issn>0918-6158</issn><eissn>1347-5215</eissn><abstract>A conjugate between chondroitin sulfate (CS) and glycyl-prednisolone (GP), named CS-GP, was produced by carbodiimide coupling at a high GP/CS ratio. CS-GP was not water-soluble and gave a nanogel (NG) in aqueous solution. Two types of nanogels, NG(I) and NG(II), with prednisolone (PD) contents of 5.5 and 21.1% (w/w), respectively, were obtained. They had particle sizes of approximately 280 and 570 nm, respectively, and showed negative ζ-potentials of approximately −40 mV. The PD release rate was slower in the nanogels than in a solution of CS-GP with a PD content of 1.4% (w/w). The PD release rate was slower in NG(II) than in NG(I), and was elevated at pH 7.4 than at pH 6.8. NG(II) was applied in vivo to rats with trinitrobenzene sulfonic acid (TNBS)-induced colitis, and its therapeutic efficacy and pharmacokinetic features were investigated. The therapeutic efficacy of NG(II) was slightly better than that of PD alone. Drug delivery to the lower intestines was enhanced with NG(II). The CS-GP nanogel has potential as a potent DDS for the treatment of ulcerative colitis.</abstract><cop>Japan</cop><pub>The Pharmaceutical Society of Japan</pub><pmid>31257292</pmid><doi>10.1248/bpb.b19-00020</doi><tpages>9</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0918-6158 |
| ispartof | Biological and Pharmaceutical Bulletin, 2019/07/01, Vol.42(7), pp.1155-1163 |
| issn | 0918-6158 1347-5215 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_2250629733 |
| source | MEDLINE; J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese; EZB-FREE-00999 freely available EZB journals; Free Full-Text Journals in Chemistry |
| subjects | Animals Anti-Inflammatory Agents - administration & dosage Anti-Inflammatory Agents - chemistry Anti-Inflammatory Agents - pharmacokinetics Carbodiimide Chondroitin sulfate chondroitin sulfate-glycyl-prednisolone conjugate Chondroitin Sulfates - administration & dosage Chondroitin Sulfates - chemistry Chondroitin Sulfates - pharmacokinetics Colitis, Ulcerative - drug therapy Colitis, Ulcerative - metabolism Colitis, Ulcerative - pathology Colon Colon - drug effects Colon - pathology Conjugates Drug delivery Drug Delivery Systems Drug Liberation efficacy Gels in vitro release Inflammatory bowel disease Intestinal Mucosa - metabolism Intestine Male nanogel Nanoparticles - administration & dosage Nanoparticles - chemistry particle characteristics pH effects Prednisolone Prednisolone - administration & dosage Prednisolone - chemistry Prednisolone - pharmacokinetics Rats, Wistar Sulfates Sulfonic acid Ulcerative colitis |
| title | Preparation of Chondroitin Sulfate-Glycyl-Prednisolone Conjugate Nanogel and Its Efficacy in Rats with Ulcerative Colitis |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-02-15T08%3A15%3A15IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Preparation%20of%20Chondroitin%20Sulfate-Glycyl-Prednisolone%20Conjugate%20Nanogel%20and%20Its%20Efficacy%20in%20Rats%20with%20Ulcerative%20Colitis&rft.jtitle=Biological%20&%20pharmaceutical%20bulletin&rft.au=Onishi,%20Hiraku&rft.date=2019-07-01&rft.volume=42&rft.issue=7&rft.spage=1155&rft.epage=1163&rft.pages=1155-1163&rft.issn=0918-6158&rft.eissn=1347-5215&rft_id=info:doi/10.1248/bpb.b19-00020&rft_dat=%3Cproquest_cross%3E2314234653%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=2314234653&rft_id=info:pmid/31257292&rfr_iscdi=true |