Phospholipid based colloidal poloxamer–nanocubic vesicles for brain targeting via the nasal route
[Display omitted] ► New phospholipid based nanocubic vesicular systems were developed. ► The polymeric non-ionic surfactant, poloxamer was incorporated in its lipid bilayer. ► The effect of surfactant concentration on the physicochemical properties of the nanocubic vesicles was investigated. ► The b...
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| Veröffentlicht in: | Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2012-12, Vol.100, p.146-154 |
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| container_title | Colloids and surfaces, B, Biointerfaces |
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| creator | Salama, Hamed A. Mahmoud, Azza A. Kamel, Amany O. Abdel Hady, Mayssa Awad, Gehanne A.S. |
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► New phospholipid based nanocubic vesicular systems were developed. ► The polymeric non-ionic surfactant, poloxamer was incorporated in its lipid bilayer. ► The effect of surfactant concentration on the physicochemical properties of the nanocubic vesicles was investigated. ► The brain targeting efficiency of these vesicles were evaluated after intranasal administration to rats.
In this study, new phospholipid based colloidal nanocubic vesicles encapsulating olanzapine for its brain targeting via the nasal route were developed. The nanocubic vesicles were prepared by incorporating non-ionic copolymers, poloxamer 188 or 407, in the lipid bilayer. The effect of phospholipid:poloxamer molar ratio on the physicochemical properties of the nanocubic vesicles was investigated. The in vivo behavior and brain targeting of these vesicles were evaluated in rats. TEM photographs showed that the vesicles looked spherical before adding poloxamer. However, after poloxamer incorporation, the vesicles showed a predominant cubic shape, except those containing phospholipid:poloxamer in the molar ratio 5:1 which were spherical. DSC study confirmed perturbation of the packing characteristics as well as fluidization of the lipid bilayer by the polymer with consequent formation of the nanocubic structure. The mean diameter of the vesicles was in the range of 363–645nm. All vesicles were elastic and the elasticity was found to depend on both poloxamer type and concentration. The intranasal nanocubic vesicles were significantly more efficient in targeting olanzapine to the brain compared to the liposomal vesicles with drug targeting efficiency values of 100% and 80%, respectively, and absolute bioavailability of 37.9% and 14.9%, respectively. |
| doi_str_mv | 10.1016/j.colsurfb.2012.05.010 |
| format | Article |
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► New phospholipid based nanocubic vesicular systems were developed. ► The polymeric non-ionic surfactant, poloxamer was incorporated in its lipid bilayer. ► The effect of surfactant concentration on the physicochemical properties of the nanocubic vesicles was investigated. ► The brain targeting efficiency of these vesicles were evaluated after intranasal administration to rats.
In this study, new phospholipid based colloidal nanocubic vesicles encapsulating olanzapine for its brain targeting via the nasal route were developed. The nanocubic vesicles were prepared by incorporating non-ionic copolymers, poloxamer 188 or 407, in the lipid bilayer. The effect of phospholipid:poloxamer molar ratio on the physicochemical properties of the nanocubic vesicles was investigated. The in vivo behavior and brain targeting of these vesicles were evaluated in rats. TEM photographs showed that the vesicles looked spherical before adding poloxamer. However, after poloxamer incorporation, the vesicles showed a predominant cubic shape, except those containing phospholipid:poloxamer in the molar ratio 5:1 which were spherical. DSC study confirmed perturbation of the packing characteristics as well as fluidization of the lipid bilayer by the polymer with consequent formation of the nanocubic structure. The mean diameter of the vesicles was in the range of 363–645nm. All vesicles were elastic and the elasticity was found to depend on both poloxamer type and concentration. The intranasal nanocubic vesicles were significantly more efficient in targeting olanzapine to the brain compared to the liposomal vesicles with drug targeting efficiency values of 100% and 80%, respectively, and absolute bioavailability of 37.9% and 14.9%, respectively.</description><identifier>ISSN: 0927-7765</identifier><identifier>EISSN: 1873-4367</identifier><identifier>DOI: 10.1016/j.colsurfb.2012.05.010</identifier><identifier>PMID: 22766291</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Administration, Intranasal ; Administration, Intravenous ; Animals ; Antipsychotic Agents - administration & dosage ; Antipsychotic Agents - chemistry ; Antipsychotic Agents - pharmacokinetics ; Benzodiazepines - administration & dosage ; Benzodiazepines - chemistry ; Benzodiazepines - pharmacokinetics ; Bioavailability ; Biological Availability ; Brain ; Brain Chemistry ; Brain targeting ; Chromatography, Liquid ; Colloids ; Drug Carriers - administration & dosage ; Drug Carriers - chemical synthesis ; Drug Carriers - pharmacokinetics ; Drug Delivery Systems ; Elasticity ; Intranasal ; Lipid Bilayers - chemistry ; Lipids ; Liposomes - chemistry ; Male ; Mass Spectrometry ; Nanocubic ; Nanostructure ; Olanzapine ; Particle Size ; Phospholipids ; Phospholipids - chemistry ; Poloxamer ; Poloxamer - chemistry ; Rats ; Rats, Wistar ; Vesicles</subject><ispartof>Colloids and surfaces, B, Biointerfaces, 2012-12, Vol.100, p.146-154</ispartof><rights>2012 Elsevier B.V.</rights><rights>Copyright © 2012 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c434t-1f15de2c2c1bd0bfe998451745d5c89bb30f0f9f92231a7aad31fc2f994f9ac93</citedby><cites>FETCH-LOGICAL-c434t-1f15de2c2c1bd0bfe998451745d5c89bb30f0f9f92231a7aad31fc2f994f9ac93</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.colsurfb.2012.05.010$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22766291$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Salama, Hamed A.</creatorcontrib><creatorcontrib>Mahmoud, Azza A.</creatorcontrib><creatorcontrib>Kamel, Amany O.</creatorcontrib><creatorcontrib>Abdel Hady, Mayssa</creatorcontrib><creatorcontrib>Awad, Gehanne A.S.</creatorcontrib><title>Phospholipid based colloidal poloxamer–nanocubic vesicles for brain targeting via the nasal route</title><title>Colloids and surfaces, B, Biointerfaces</title><addtitle>Colloids Surf B Biointerfaces</addtitle><description>[Display omitted]
► New phospholipid based nanocubic vesicular systems were developed. ► The polymeric non-ionic surfactant, poloxamer was incorporated in its lipid bilayer. ► The effect of surfactant concentration on the physicochemical properties of the nanocubic vesicles was investigated. ► The brain targeting efficiency of these vesicles were evaluated after intranasal administration to rats.
In this study, new phospholipid based colloidal nanocubic vesicles encapsulating olanzapine for its brain targeting via the nasal route were developed. The nanocubic vesicles were prepared by incorporating non-ionic copolymers, poloxamer 188 or 407, in the lipid bilayer. The effect of phospholipid:poloxamer molar ratio on the physicochemical properties of the nanocubic vesicles was investigated. The in vivo behavior and brain targeting of these vesicles were evaluated in rats. TEM photographs showed that the vesicles looked spherical before adding poloxamer. However, after poloxamer incorporation, the vesicles showed a predominant cubic shape, except those containing phospholipid:poloxamer in the molar ratio 5:1 which were spherical. DSC study confirmed perturbation of the packing characteristics as well as fluidization of the lipid bilayer by the polymer with consequent formation of the nanocubic structure. The mean diameter of the vesicles was in the range of 363–645nm. All vesicles were elastic and the elasticity was found to depend on both poloxamer type and concentration. The intranasal nanocubic vesicles were significantly more efficient in targeting olanzapine to the brain compared to the liposomal vesicles with drug targeting efficiency values of 100% and 80%, respectively, and absolute bioavailability of 37.9% and 14.9%, respectively.</description><subject>Administration, Intranasal</subject><subject>Administration, Intravenous</subject><subject>Animals</subject><subject>Antipsychotic Agents - administration & dosage</subject><subject>Antipsychotic Agents - chemistry</subject><subject>Antipsychotic Agents - pharmacokinetics</subject><subject>Benzodiazepines - administration & dosage</subject><subject>Benzodiazepines - chemistry</subject><subject>Benzodiazepines - pharmacokinetics</subject><subject>Bioavailability</subject><subject>Biological Availability</subject><subject>Brain</subject><subject>Brain Chemistry</subject><subject>Brain targeting</subject><subject>Chromatography, Liquid</subject><subject>Colloids</subject><subject>Drug Carriers - administration & dosage</subject><subject>Drug Carriers - chemical synthesis</subject><subject>Drug Carriers - pharmacokinetics</subject><subject>Drug Delivery Systems</subject><subject>Elasticity</subject><subject>Intranasal</subject><subject>Lipid Bilayers - chemistry</subject><subject>Lipids</subject><subject>Liposomes - chemistry</subject><subject>Male</subject><subject>Mass Spectrometry</subject><subject>Nanocubic</subject><subject>Nanostructure</subject><subject>Olanzapine</subject><subject>Particle Size</subject><subject>Phospholipids</subject><subject>Phospholipids - chemistry</subject><subject>Poloxamer</subject><subject>Poloxamer - chemistry</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Vesicles</subject><issn>0927-7765</issn><issn>1873-4367</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNkc1O3DAUha2qqAzQV0BesknqnySOdyDUQiWkdgFryz_XjEeeOLWTEez6Dn3DPkkzGmBLV3fznXOk-yF0TklNCe2-bGqbYpmzNzUjlNWkrQklH9CK9oJXDe_ER7QikolKiK49RielbAghrKHiEzpmTHQdk3SF7M91KuM6xTAGh40u4PDSHFNwOuIxxfSkt5D__v4z6CHZ2QSLd1CCjVCwTxmbrMOAJ50fYQrDI94Fjac14EGXpSCneYIzdOR1LPD55Z6ih29f769vq7sfN9-vr-4q2_BmqqinrQNmmaXGEeNByr5pqWha19peGsOJJ156yRinWmjtOPWWeSkbL7WV_BRdHHrHnH7NUCa1DcVCjHqANBdFRd_Rnoue_AfatbIRRND3UcJEz5nke7Q7oDanUjJ4Neaw1fl5gdRem9qoV21qr02RVi3aluD5y8ZstuDeYq-eFuDyAMDyv12ArIoNMFhwIYOdlEvhvY1_jlKuuA</recordid><startdate>20121201</startdate><enddate>20121201</enddate><creator>Salama, Hamed A.</creator><creator>Mahmoud, Azza A.</creator><creator>Kamel, Amany O.</creator><creator>Abdel Hady, Mayssa</creator><creator>Awad, Gehanne A.S.</creator><general>Elsevier B.V</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><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7SR</scope><scope>7U5</scope><scope>8BQ</scope><scope>JG9</scope><scope>L7M</scope></search><sort><creationdate>20121201</creationdate><title>Phospholipid based colloidal poloxamer–nanocubic vesicles for brain targeting via the nasal route</title><author>Salama, Hamed A. ; Mahmoud, Azza A. ; Kamel, Amany O. ; Abdel Hady, Mayssa ; Awad, Gehanne A.S.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c434t-1f15de2c2c1bd0bfe998451745d5c89bb30f0f9f92231a7aad31fc2f994f9ac93</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Administration, Intranasal</topic><topic>Administration, Intravenous</topic><topic>Animals</topic><topic>Antipsychotic Agents - administration & dosage</topic><topic>Antipsychotic Agents - chemistry</topic><topic>Antipsychotic Agents - pharmacokinetics</topic><topic>Benzodiazepines - administration & dosage</topic><topic>Benzodiazepines - chemistry</topic><topic>Benzodiazepines - pharmacokinetics</topic><topic>Bioavailability</topic><topic>Biological Availability</topic><topic>Brain</topic><topic>Brain Chemistry</topic><topic>Brain targeting</topic><topic>Chromatography, Liquid</topic><topic>Colloids</topic><topic>Drug Carriers - administration & dosage</topic><topic>Drug Carriers - chemical synthesis</topic><topic>Drug Carriers - pharmacokinetics</topic><topic>Drug Delivery Systems</topic><topic>Elasticity</topic><topic>Intranasal</topic><topic>Lipid Bilayers - chemistry</topic><topic>Lipids</topic><topic>Liposomes - chemistry</topic><topic>Male</topic><topic>Mass Spectrometry</topic><topic>Nanocubic</topic><topic>Nanostructure</topic><topic>Olanzapine</topic><topic>Particle Size</topic><topic>Phospholipids</topic><topic>Phospholipids - chemistry</topic><topic>Poloxamer</topic><topic>Poloxamer - chemistry</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Vesicles</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Salama, Hamed A.</creatorcontrib><creatorcontrib>Mahmoud, Azza A.</creatorcontrib><creatorcontrib>Kamel, Amany O.</creatorcontrib><creatorcontrib>Abdel Hady, Mayssa</creatorcontrib><creatorcontrib>Awad, Gehanne A.S.</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><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Engineered Materials Abstracts</collection><collection>Solid State and Superconductivity Abstracts</collection><collection>METADEX</collection><collection>Materials Research Database</collection><collection>Advanced Technologies Database with Aerospace</collection><jtitle>Colloids and surfaces, B, Biointerfaces</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Salama, Hamed A.</au><au>Mahmoud, Azza A.</au><au>Kamel, Amany O.</au><au>Abdel Hady, Mayssa</au><au>Awad, Gehanne A.S.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Phospholipid based colloidal poloxamer–nanocubic vesicles for brain targeting via the nasal route</atitle><jtitle>Colloids and surfaces, B, Biointerfaces</jtitle><addtitle>Colloids Surf B Biointerfaces</addtitle><date>2012-12-01</date><risdate>2012</risdate><volume>100</volume><spage>146</spage><epage>154</epage><pages>146-154</pages><issn>0927-7765</issn><eissn>1873-4367</eissn><abstract>[Display omitted]
► New phospholipid based nanocubic vesicular systems were developed. ► The polymeric non-ionic surfactant, poloxamer was incorporated in its lipid bilayer. ► The effect of surfactant concentration on the physicochemical properties of the nanocubic vesicles was investigated. ► The brain targeting efficiency of these vesicles were evaluated after intranasal administration to rats.
In this study, new phospholipid based colloidal nanocubic vesicles encapsulating olanzapine for its brain targeting via the nasal route were developed. The nanocubic vesicles were prepared by incorporating non-ionic copolymers, poloxamer 188 or 407, in the lipid bilayer. The effect of phospholipid:poloxamer molar ratio on the physicochemical properties of the nanocubic vesicles was investigated. The in vivo behavior and brain targeting of these vesicles were evaluated in rats. TEM photographs showed that the vesicles looked spherical before adding poloxamer. However, after poloxamer incorporation, the vesicles showed a predominant cubic shape, except those containing phospholipid:poloxamer in the molar ratio 5:1 which were spherical. DSC study confirmed perturbation of the packing characteristics as well as fluidization of the lipid bilayer by the polymer with consequent formation of the nanocubic structure. The mean diameter of the vesicles was in the range of 363–645nm. All vesicles were elastic and the elasticity was found to depend on both poloxamer type and concentration. The intranasal nanocubic vesicles were significantly more efficient in targeting olanzapine to the brain compared to the liposomal vesicles with drug targeting efficiency values of 100% and 80%, respectively, and absolute bioavailability of 37.9% and 14.9%, respectively.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>22766291</pmid><doi>10.1016/j.colsurfb.2012.05.010</doi><tpages>9</tpages></addata></record> |
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| identifier | ISSN: 0927-7765 |
| ispartof | Colloids and surfaces, B, Biointerfaces, 2012-12, Vol.100, p.146-154 |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Administration, Intranasal Administration, Intravenous Animals Antipsychotic Agents - administration & dosage Antipsychotic Agents - chemistry Antipsychotic Agents - pharmacokinetics Benzodiazepines - administration & dosage Benzodiazepines - chemistry Benzodiazepines - pharmacokinetics Bioavailability Biological Availability Brain Brain Chemistry Brain targeting Chromatography, Liquid Colloids Drug Carriers - administration & dosage Drug Carriers - chemical synthesis Drug Carriers - pharmacokinetics Drug Delivery Systems Elasticity Intranasal Lipid Bilayers - chemistry Lipids Liposomes - chemistry Male Mass Spectrometry Nanocubic Nanostructure Olanzapine Particle Size Phospholipids Phospholipids - chemistry Poloxamer Poloxamer - chemistry Rats Rats, Wistar Vesicles |
| title | Phospholipid based colloidal poloxamer–nanocubic vesicles for brain targeting via the nasal route |
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