Evaluation of the clearance characteristics of bioadhesive systems in humans
This paper describes the characterisation, radiolabelling and clearance characteristics of three bioadhesive nasal delivery systems; starch microspheres, chitosan microspheres and chitosan solution. The time taken for 50% of these bioadhesive materials and a control to be cleared from the nasal cavi...
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| Veröffentlicht in: | International journal of pharmaceutics 1999-02, Vol.178 (1), p.55-65 |
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| container_title | International journal of pharmaceutics |
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| creator | Soane, R.J Frier, M Perkins, A.C Jones, N.S Davis, S.S Illum, L |
| description | This paper describes the characterisation, radiolabelling and clearance characteristics of three bioadhesive nasal delivery systems; starch microspheres, chitosan microspheres and chitosan solution. The time taken for 50% of these bioadhesive materials and a control to be cleared from the nasal cavity, after nasal administration to human volunteers, was evaluated using gamma scintigraphy. The data show that the control was cleared rapidly, with a half life of 21 min, whereas the bioadhesive delivery systems had much longer half lives. The clearance of the chitosan solution almost doubled to 41 min, whilst the half life of clearance for the starch microspheres more than tripled to 68 min and for the chitosan microspheres the half life of clearance quadrupled to 84 min. From the results reported in this study it is possible to determine that both chitosan systems and the starch microspheres have good bioadhesive characteristics. The results have supported the hypothesis that chitosan delivery systems can reduce the rate of clearance from the nasal cavity, thereby increasing the contact time of the delivery system with the nasal mucosa, providing the potential for increasing the bioavailability of drugs incorporated into these systems. |
| doi_str_mv | 10.1016/S0378-5173(98)00367-6 |
| format | Article |
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The time taken for 50% of these bioadhesive materials and a control to be cleared from the nasal cavity, after nasal administration to human volunteers, was evaluated using gamma scintigraphy. The data show that the control was cleared rapidly, with a half life of 21 min, whereas the bioadhesive delivery systems had much longer half lives. The clearance of the chitosan solution almost doubled to 41 min, whilst the half life of clearance for the starch microspheres more than tripled to 68 min and for the chitosan microspheres the half life of clearance quadrupled to 84 min. From the results reported in this study it is possible to determine that both chitosan systems and the starch microspheres have good bioadhesive characteristics. The results have supported the hypothesis that chitosan delivery systems can reduce the rate of clearance from the nasal cavity, thereby increasing the contact time of the delivery system with the nasal mucosa, providing the potential for increasing the bioavailability of drugs incorporated into these systems.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/S0378-5173(98)00367-6</identifier><identifier>PMID: 10205625</identifier><identifier>CODEN: IJPHDE</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Adhesiveness ; Administration, Intranasal ; Administration, Topical ; Adolescent ; Adult ; Bioadhesive polymers ; Biological and medical sciences ; Chitin - analogs & derivatives ; Chitin - pharmacokinetics ; Chitosan ; Delayed-Action Preparations - pharmacokinetics ; Female ; General pharmacology ; Humans ; Male ; Medical sciences ; Microspheres ; Mucoadhesion and gamma scintigraphy ; Nasal drug delivery ; Nasal Mucosa - physiology ; Particle Size ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Radionuclide Imaging ; Starch ; Starch - pharmacokinetics ; Viscosity</subject><ispartof>International journal of pharmaceutics, 1999-02, Vol.178 (1), p.55-65</ispartof><rights>1999 Elsevier Science B.V.</rights><rights>1999 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c390t-90afa923afa9cee37d4e59620689338741663fa43022e1079d03d051495d7b393</citedby><cites>FETCH-LOGICAL-c390t-90afa923afa9cee37d4e59620689338741663fa43022e1079d03d051495d7b393</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0378-5173(98)00367-6$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,781,785,3551,27929,27930,46000</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1693862$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10205625$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Soane, R.J</creatorcontrib><creatorcontrib>Frier, M</creatorcontrib><creatorcontrib>Perkins, A.C</creatorcontrib><creatorcontrib>Jones, N.S</creatorcontrib><creatorcontrib>Davis, S.S</creatorcontrib><creatorcontrib>Illum, L</creatorcontrib><title>Evaluation of the clearance characteristics of bioadhesive systems in humans</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>This paper describes the characterisation, radiolabelling and clearance characteristics of three bioadhesive nasal delivery systems; starch microspheres, chitosan microspheres and chitosan solution. The time taken for 50% of these bioadhesive materials and a control to be cleared from the nasal cavity, after nasal administration to human volunteers, was evaluated using gamma scintigraphy. The data show that the control was cleared rapidly, with a half life of 21 min, whereas the bioadhesive delivery systems had much longer half lives. The clearance of the chitosan solution almost doubled to 41 min, whilst the half life of clearance for the starch microspheres more than tripled to 68 min and for the chitosan microspheres the half life of clearance quadrupled to 84 min. From the results reported in this study it is possible to determine that both chitosan systems and the starch microspheres have good bioadhesive characteristics. The results have supported the hypothesis that chitosan delivery systems can reduce the rate of clearance from the nasal cavity, thereby increasing the contact time of the delivery system with the nasal mucosa, providing the potential for increasing the bioavailability of drugs incorporated into these systems.</description><subject>Adhesiveness</subject><subject>Administration, Intranasal</subject><subject>Administration, Topical</subject><subject>Adolescent</subject><subject>Adult</subject><subject>Bioadhesive polymers</subject><subject>Biological and medical sciences</subject><subject>Chitin - analogs & derivatives</subject><subject>Chitin - pharmacokinetics</subject><subject>Chitosan</subject><subject>Delayed-Action Preparations - pharmacokinetics</subject><subject>Female</subject><subject>General pharmacology</subject><subject>Humans</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Microspheres</subject><subject>Mucoadhesion and gamma scintigraphy</subject><subject>Nasal drug delivery</subject><subject>Nasal Mucosa - physiology</subject><subject>Particle Size</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Radionuclide Imaging</subject><subject>Starch</subject><subject>Starch - pharmacokinetics</subject><subject>Viscosity</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1v2zAMhoWhQ5O1_QkrfCiK7uCWMm3JOg1D0X0AAXpoexYUmUY0-KMT7QD597WTYN1tF5KH5yWJR4jPEm4lSHX3BKjLtJAab0z5BQCVTtUHsZSlxhRzrU7E8i-yEJ-YfwOAyiSeioWEDAqVFUuxeti6ZnRD6Lukr5NhQ4lvyEXX-WnaTIMfKAYegucZWIfeVRvisKWEdzxQy0noks3Yuo7PxcfaNUwXx34mXr4_PN__TFePP37df1ulHg0MqQFXO5PhXD0R6iqnwqgMVGkQS51LpbB2OUKWkQRtKsAKCpmbotJrNHgmrg97X2P_ZyQebBvYU9O4jvqRrTLKYKnKCSwOoI89c6TavsbQurizEuys0e412tmRNaXda7Rqyl0eD4zrlqp_UgdvE3B1BBx719Szr8Dv3P5-NmFfDxhNNraBomUfaFJbhUh-sFUf_vPJG8-Vjfk</recordid><startdate>19990201</startdate><enddate>19990201</enddate><creator>Soane, R.J</creator><creator>Frier, M</creator><creator>Perkins, A.C</creator><creator>Jones, N.S</creator><creator>Davis, S.S</creator><creator>Illum, L</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>19990201</creationdate><title>Evaluation of the clearance characteristics of bioadhesive systems in humans</title><author>Soane, R.J ; Frier, M ; Perkins, A.C ; Jones, N.S ; Davis, S.S ; Illum, L</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c390t-90afa923afa9cee37d4e59620689338741663fa43022e1079d03d051495d7b393</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>Adhesiveness</topic><topic>Administration, Intranasal</topic><topic>Administration, Topical</topic><topic>Adolescent</topic><topic>Adult</topic><topic>Bioadhesive polymers</topic><topic>Biological and medical sciences</topic><topic>Chitin - analogs & derivatives</topic><topic>Chitin - pharmacokinetics</topic><topic>Chitosan</topic><topic>Delayed-Action Preparations - pharmacokinetics</topic><topic>Female</topic><topic>General pharmacology</topic><topic>Humans</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Microspheres</topic><topic>Mucoadhesion and gamma scintigraphy</topic><topic>Nasal drug delivery</topic><topic>Nasal Mucosa - physiology</topic><topic>Particle Size</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Radionuclide Imaging</topic><topic>Starch</topic><topic>Starch - pharmacokinetics</topic><topic>Viscosity</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Soane, R.J</creatorcontrib><creatorcontrib>Frier, M</creatorcontrib><creatorcontrib>Perkins, A.C</creatorcontrib><creatorcontrib>Jones, N.S</creatorcontrib><creatorcontrib>Davis, S.S</creatorcontrib><creatorcontrib>Illum, L</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>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Soane, R.J</au><au>Frier, M</au><au>Perkins, A.C</au><au>Jones, N.S</au><au>Davis, S.S</au><au>Illum, L</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Evaluation of the clearance characteristics of bioadhesive systems in humans</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>1999-02-01</date><risdate>1999</risdate><volume>178</volume><issue>1</issue><spage>55</spage><epage>65</epage><pages>55-65</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>This paper describes the characterisation, radiolabelling and clearance characteristics of three bioadhesive nasal delivery systems; starch microspheres, chitosan microspheres and chitosan solution. The time taken for 50% of these bioadhesive materials and a control to be cleared from the nasal cavity, after nasal administration to human volunteers, was evaluated using gamma scintigraphy. The data show that the control was cleared rapidly, with a half life of 21 min, whereas the bioadhesive delivery systems had much longer half lives. The clearance of the chitosan solution almost doubled to 41 min, whilst the half life of clearance for the starch microspheres more than tripled to 68 min and for the chitosan microspheres the half life of clearance quadrupled to 84 min. From the results reported in this study it is possible to determine that both chitosan systems and the starch microspheres have good bioadhesive characteristics. The results have supported the hypothesis that chitosan delivery systems can reduce the rate of clearance from the nasal cavity, thereby increasing the contact time of the delivery system with the nasal mucosa, providing the potential for increasing the bioavailability of drugs incorporated into these systems.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>10205625</pmid><doi>10.1016/S0378-5173(98)00367-6</doi><tpages>11</tpages></addata></record> |
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| subjects | Adhesiveness Administration, Intranasal Administration, Topical Adolescent Adult Bioadhesive polymers Biological and medical sciences Chitin - analogs & derivatives Chitin - pharmacokinetics Chitosan Delayed-Action Preparations - pharmacokinetics Female General pharmacology Humans Male Medical sciences Microspheres Mucoadhesion and gamma scintigraphy Nasal drug delivery Nasal Mucosa - physiology Particle Size Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Radionuclide Imaging Starch Starch - pharmacokinetics Viscosity |
| title | Evaluation of the clearance characteristics of bioadhesive systems in humans |
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