Nanosphere based oral insulin delivery
Zinc insulin is successfully encapsulated in various polyester and polyanhydride nanosphere formulations using Phase Inversion Nanoencapsulation (PIN). The encapsulated insulin maintains its biological activity and is released from the nanospheres over a span of approximately 6 h. A specific formula...
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Veröffentlicht in: | Journal of controlled release 2000-03, Vol.65 (1), p.261-269 |
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creator | Carino, Gerardo P Jacob, Jules S Mathiowitz, Edith |
description | Zinc insulin is successfully encapsulated in various polyester and polyanhydride nanosphere formulations using Phase Inversion Nanoencapsulation (PIN). The encapsulated insulin maintains its biological activity and is released from the nanospheres over a span of approximately 6 h. A specific formulation, 1.6% zinc insulin in poly(lactide-co-glycolide) (PLGA) with fumaric anhydride oligimer and iron oxide additives has been shown to be active orally. This formulation is shown to have 11.4% of the efficacy of intraperitoneally delivered zinc insulin and is able to control plasma glucose levels when faced with a simultaneously administered glucose challenge. A number of properties of this formulation, including size, release kinetics, bioadhesiveness and ability to traverse the gastrointestinal epithelium, are likely to contribute to its oral efficacy. |
doi_str_mv | 10.1016/S0168-3659(99)00247-3 |
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The encapsulated insulin maintains its biological activity and is released from the nanospheres over a span of approximately 6 h. A specific formulation, 1.6% zinc insulin in poly(lactide-co-glycolide) (PLGA) with fumaric anhydride oligimer and iron oxide additives has been shown to be active orally. This formulation is shown to have 11.4% of the efficacy of intraperitoneally delivered zinc insulin and is able to control plasma glucose levels when faced with a simultaneously administered glucose challenge. A number of properties of this formulation, including size, release kinetics, bioadhesiveness and ability to traverse the gastrointestinal epithelium, are likely to contribute to its oral efficacy.</description><identifier>ISSN: 0168-3659</identifier><identifier>EISSN: 1873-4995</identifier><identifier>DOI: 10.1016/S0168-3659(99)00247-3</identifier><identifier>PMID: 10699286</identifier><identifier>CODEN: JCREEC</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Administration, Oral ; Animals ; Area Under Curve ; Biological and medical sciences ; Blood Glucose - metabolism ; Cattle ; Diabetes ; Drug Compounding ; Drug Delivery Systems ; General and cellular metabolism. Vitamins ; General pharmacology ; Glucose Tolerance Test ; Hypoglycemic Agents - administration & dosage ; Hypoglycemic Agents - blood ; Hypoglycemic Agents - pharmacology ; Injections, Intraperitoneal ; Insulin ; Insulin - administration & dosage ; Insulin - blood ; Insulin - pharmacology ; Intestinal Absorption ; Medical sciences ; Microscopy, Electron, Scanning ; Microspheres ; Nanosphere ; Oral Delivery ; Particle Size ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. 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The encapsulated insulin maintains its biological activity and is released from the nanospheres over a span of approximately 6 h. A specific formulation, 1.6% zinc insulin in poly(lactide-co-glycolide) (PLGA) with fumaric anhydride oligimer and iron oxide additives has been shown to be active orally. This formulation is shown to have 11.4% of the efficacy of intraperitoneally delivered zinc insulin and is able to control plasma glucose levels when faced with a simultaneously administered glucose challenge. A number of properties of this formulation, including size, release kinetics, bioadhesiveness and ability to traverse the gastrointestinal epithelium, are likely to contribute to its oral efficacy.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Area Under Curve</subject><subject>Biological and medical sciences</subject><subject>Blood Glucose - metabolism</subject><subject>Cattle</subject><subject>Diabetes</subject><subject>Drug Compounding</subject><subject>Drug Delivery Systems</subject><subject>General and cellular metabolism. Vitamins</subject><subject>General pharmacology</subject><subject>Glucose Tolerance Test</subject><subject>Hypoglycemic Agents - administration & dosage</subject><subject>Hypoglycemic Agents - blood</subject><subject>Hypoglycemic Agents - pharmacology</subject><subject>Injections, Intraperitoneal</subject><subject>Insulin</subject><subject>Insulin - administration & dosage</subject><subject>Insulin - blood</subject><subject>Insulin - pharmacology</subject><subject>Intestinal Absorption</subject><subject>Medical sciences</subject><subject>Microscopy, Electron, Scanning</subject><subject>Microspheres</subject><subject>Nanosphere</subject><subject>Oral Delivery</subject><subject>Particle Size</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Polyester</subject><subject>Rats</subject><issn>0168-3659</issn><issn>1873-4995</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkDtPwzAQgC0EoqXwE0AdUAVDwIkdOzchVPGSKhiA2XLsszBKk2I3lfrvSZsK2Fjuhvvu9RFymtKrlKbi-rULRcJEDhcAl5RmXCZsjwzTQrKEA-T7ZPiDDMhRjJ-U0pxxeUgGKRUAWSGGZPKs6yYuPjDguNQR7bgJuhr7OraVr8cWK7_CsD4mB05XEU92eUTe7-_epo_J7OXhaXo7SwwDukwKrVFI4QxImRonKOQOMpuzUmdGFpntKkUGjusCrM55yjgwXXJTOmppJtiITPq5i9B8tRiXau6jwarSNTZtVJICl0IWHZj3oAlNjAGdWgQ_12GtUqo2gtRWkNp8rwDUVpBiXd_ZbkFbztH-6eqNdMD5DtDR6MoFXRsffznGKZObOTc9hp2NlcegovFYG7Q-oFkq2_h_LvkG1MSA_Q</recordid><startdate>20000301</startdate><enddate>20000301</enddate><creator>Carino, Gerardo P</creator><creator>Jacob, Jules S</creator><creator>Mathiowitz, Edith</creator><general>Elsevier B.V</general><general>Elsevier</general><scope>IQODW</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>7X8</scope></search><sort><creationdate>20000301</creationdate><title>Nanosphere based oral insulin delivery</title><author>Carino, Gerardo P ; Jacob, Jules S ; Mathiowitz, Edith</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c390t-8aae676fc9771cf6095f92d53ba2c782dfc9829f4a89da5413493ab4cbf0d0263</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2000</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Area Under Curve</topic><topic>Biological and medical sciences</topic><topic>Blood Glucose - metabolism</topic><topic>Cattle</topic><topic>Diabetes</topic><topic>Drug Compounding</topic><topic>Drug Delivery Systems</topic><topic>General and cellular metabolism. Vitamins</topic><topic>General pharmacology</topic><topic>Glucose Tolerance Test</topic><topic>Hypoglycemic Agents - administration & dosage</topic><topic>Hypoglycemic Agents - blood</topic><topic>Hypoglycemic Agents - pharmacology</topic><topic>Injections, Intraperitoneal</topic><topic>Insulin</topic><topic>Insulin - administration & dosage</topic><topic>Insulin - blood</topic><topic>Insulin - pharmacology</topic><topic>Intestinal Absorption</topic><topic>Medical sciences</topic><topic>Microscopy, Electron, Scanning</topic><topic>Microspheres</topic><topic>Nanosphere</topic><topic>Oral Delivery</topic><topic>Particle Size</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Polyester</topic><topic>Rats</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Carino, Gerardo P</creatorcontrib><creatorcontrib>Jacob, Jules S</creatorcontrib><creatorcontrib>Mathiowitz, Edith</creatorcontrib><collection>Pascal-Francis</collection><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>Journal of controlled release</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Carino, Gerardo P</au><au>Jacob, Jules S</au><au>Mathiowitz, Edith</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Nanosphere based oral insulin delivery</atitle><jtitle>Journal of controlled release</jtitle><addtitle>J Control Release</addtitle><date>2000-03-01</date><risdate>2000</risdate><volume>65</volume><issue>1</issue><spage>261</spage><epage>269</epage><pages>261-269</pages><issn>0168-3659</issn><eissn>1873-4995</eissn><coden>JCREEC</coden><abstract>Zinc insulin is successfully encapsulated in various polyester and polyanhydride nanosphere formulations using Phase Inversion Nanoencapsulation (PIN). The encapsulated insulin maintains its biological activity and is released from the nanospheres over a span of approximately 6 h. A specific formulation, 1.6% zinc insulin in poly(lactide-co-glycolide) (PLGA) with fumaric anhydride oligimer and iron oxide additives has been shown to be active orally. This formulation is shown to have 11.4% of the efficacy of intraperitoneally delivered zinc insulin and is able to control plasma glucose levels when faced with a simultaneously administered glucose challenge. A number of properties of this formulation, including size, release kinetics, bioadhesiveness and ability to traverse the gastrointestinal epithelium, are likely to contribute to its oral efficacy.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>10699286</pmid><doi>10.1016/S0168-3659(99)00247-3</doi><tpages>9</tpages></addata></record> |
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subjects | Administration, Oral Animals Area Under Curve Biological and medical sciences Blood Glucose - metabolism Cattle Diabetes Drug Compounding Drug Delivery Systems General and cellular metabolism. Vitamins General pharmacology Glucose Tolerance Test Hypoglycemic Agents - administration & dosage Hypoglycemic Agents - blood Hypoglycemic Agents - pharmacology Injections, Intraperitoneal Insulin Insulin - administration & dosage Insulin - blood Insulin - pharmacology Intestinal Absorption Medical sciences Microscopy, Electron, Scanning Microspheres Nanosphere Oral Delivery Particle Size Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Polyester Rats |
title | Nanosphere based oral insulin delivery |
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