Identifying lipidic emulsomes for improved oxcarbazepine brain targeting: In vitro and rat in vivo studies
[Display omitted] Lipid-based nanovectors offer effective carriers for brain delivery by improving drug potency and reducing off-target effects. Emulsomes are nano-triglyceride (TG) carriers formed of lipid cores supported by at least one phospholipid (PC) sheath. Due to their surface active propert...
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| Veröffentlicht in: | International journal of pharmaceutics 2016-04, Vol.503 (1-2), p.127-140 |
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| container_title | International journal of pharmaceutics |
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| creator | El-Zaafarany, Ghada M. Soliman, Mahmoud E. Mansour, Samar Awad, Gehanne A.S. |
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Lipid-based nanovectors offer effective carriers for brain delivery by improving drug potency and reducing off-target effects. Emulsomes are nano-triglyceride (TG) carriers formed of lipid cores supported by at least one phospholipid (PC) sheath. Due to their surface active properties, PC forms bilayers at the aqueous interface, thereby enabling encapsulated drug to benefit from better bioavailability and stability. Emulsomes of oxcarbazepine (OX) were prepared, aimed to offer nanocarriers for nasal delivery for brain targeting. Different TG cores (Compritol®, tripalmitin, tristearin and triolein) and soya phosphatidylcholine in different amounts and ratios were used for emulsomal preparation. Particles were modulated to generate nanocarriers with suitable size, charge, encapsulation efficiency and prolonged release. Cytotoxicity and pharmacokinetic studies were also implemented. Nano-spherical OX-emulsomes with maximal encapsulation of 96.75% were generated. Stability studies showed changes within 30.6% and 11.2% in the size and EE% after 3 months. MTT assay proved a decrease in drug toxicity by its encapsulation in emulsomes. Incorporation of OX into emulsomes resulted in stable nanoformulations. Tailoring emulsomes properties by modulating the surface charge and particle size produced a stable system for the lipophilic drug with a prolonged release profile and mean residence time and proved direct nose-to-brain transport in rats. |
| doi_str_mv | 10.1016/j.ijpharm.2016.02.038 |
| format | Article |
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Lipid-based nanovectors offer effective carriers for brain delivery by improving drug potency and reducing off-target effects. Emulsomes are nano-triglyceride (TG) carriers formed of lipid cores supported by at least one phospholipid (PC) sheath. Due to their surface active properties, PC forms bilayers at the aqueous interface, thereby enabling encapsulated drug to benefit from better bioavailability and stability. Emulsomes of oxcarbazepine (OX) were prepared, aimed to offer nanocarriers for nasal delivery for brain targeting. Different TG cores (Compritol®, tripalmitin, tristearin and triolein) and soya phosphatidylcholine in different amounts and ratios were used for emulsomal preparation. Particles were modulated to generate nanocarriers with suitable size, charge, encapsulation efficiency and prolonged release. Cytotoxicity and pharmacokinetic studies were also implemented. Nano-spherical OX-emulsomes with maximal encapsulation of 96.75% were generated. Stability studies showed changes within 30.6% and 11.2% in the size and EE% after 3 months. MTT assay proved a decrease in drug toxicity by its encapsulation in emulsomes. Incorporation of OX into emulsomes resulted in stable nanoformulations. Tailoring emulsomes properties by modulating the surface charge and particle size produced a stable system for the lipophilic drug with a prolonged release profile and mean residence time and proved direct nose-to-brain transport in rats.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2016.02.038</identifier><identifier>PMID: 26924357</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Administration, Intranasal ; Animals ; Anticonvulsants - administration & dosage ; Anticonvulsants - blood ; Anticonvulsants - chemistry ; Anticonvulsants - pharmacokinetics ; Brain - metabolism ; Carbamazepine - administration & dosage ; Carbamazepine - analogs & derivatives ; Carbamazepine - blood ; Carbamazepine - chemistry ; Carbamazepine - pharmacokinetics ; Cell Line, Tumor ; Cell Survival - drug effects ; Direct nose-to-brain delivery ; Drug Carriers - administration & dosage ; Drug Carriers - chemistry ; Drug Carriers - pharmacokinetics ; Drug Liberation ; Drug targeting efficiency ; Emulsomes ; Humans ; Intranasal ; Lipids - chemistry ; Male ; Nanoparticles - administration & dosage ; Nanoparticles - chemistry ; Nasal Mucosa ; Oxcarbazepine ; Particle Size ; Rats, Wistar ; Surface Properties</subject><ispartof>International journal of pharmaceutics, 2016-04, Vol.503 (1-2), p.127-140</ispartof><rights>2016 Elsevier B.V.</rights><rights>Copyright © 2016 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c398t-ab2e0b4122c8935fbfe122fe68e670d39f773b12d878b6af7c412d53ec65043c3</citedby><cites>FETCH-LOGICAL-c398t-ab2e0b4122c8935fbfe122fe68e670d39f773b12d878b6af7c412d53ec65043c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0378517316301430$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,65309</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/26924357$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>El-Zaafarany, Ghada M.</creatorcontrib><creatorcontrib>Soliman, Mahmoud E.</creatorcontrib><creatorcontrib>Mansour, Samar</creatorcontrib><creatorcontrib>Awad, Gehanne A.S.</creatorcontrib><title>Identifying lipidic emulsomes for improved oxcarbazepine brain targeting: In vitro and rat in vivo studies</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>[Display omitted]
Lipid-based nanovectors offer effective carriers for brain delivery by improving drug potency and reducing off-target effects. Emulsomes are nano-triglyceride (TG) carriers formed of lipid cores supported by at least one phospholipid (PC) sheath. Due to their surface active properties, PC forms bilayers at the aqueous interface, thereby enabling encapsulated drug to benefit from better bioavailability and stability. Emulsomes of oxcarbazepine (OX) were prepared, aimed to offer nanocarriers for nasal delivery for brain targeting. Different TG cores (Compritol®, tripalmitin, tristearin and triolein) and soya phosphatidylcholine in different amounts and ratios were used for emulsomal preparation. Particles were modulated to generate nanocarriers with suitable size, charge, encapsulation efficiency and prolonged release. Cytotoxicity and pharmacokinetic studies were also implemented. Nano-spherical OX-emulsomes with maximal encapsulation of 96.75% were generated. Stability studies showed changes within 30.6% and 11.2% in the size and EE% after 3 months. MTT assay proved a decrease in drug toxicity by its encapsulation in emulsomes. Incorporation of OX into emulsomes resulted in stable nanoformulations. Tailoring emulsomes properties by modulating the surface charge and particle size produced a stable system for the lipophilic drug with a prolonged release profile and mean residence time and proved direct nose-to-brain transport in rats.</description><subject>Administration, Intranasal</subject><subject>Animals</subject><subject>Anticonvulsants - administration & dosage</subject><subject>Anticonvulsants - blood</subject><subject>Anticonvulsants - chemistry</subject><subject>Anticonvulsants - pharmacokinetics</subject><subject>Brain - metabolism</subject><subject>Carbamazepine - administration & dosage</subject><subject>Carbamazepine - analogs & derivatives</subject><subject>Carbamazepine - blood</subject><subject>Carbamazepine - chemistry</subject><subject>Carbamazepine - pharmacokinetics</subject><subject>Cell Line, Tumor</subject><subject>Cell Survival - drug effects</subject><subject>Direct nose-to-brain delivery</subject><subject>Drug Carriers - administration & dosage</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Carriers - pharmacokinetics</subject><subject>Drug Liberation</subject><subject>Drug targeting efficiency</subject><subject>Emulsomes</subject><subject>Humans</subject><subject>Intranasal</subject><subject>Lipids - chemistry</subject><subject>Male</subject><subject>Nanoparticles - administration & dosage</subject><subject>Nanoparticles - chemistry</subject><subject>Nasal Mucosa</subject><subject>Oxcarbazepine</subject><subject>Particle Size</subject><subject>Rats, Wistar</subject><subject>Surface Properties</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE2PFCEQhonRuOPoT9Bw9NItH9NAezFm48ckm3jRM6GhWOl0Ny3Qk11_vUxm9OoJqDwvVfUg9JqSlhIq3o1tGNefJs0tq8-WsJZw9QTtqJK84QcpnqId4VI1HZX8Br3IeSSECEb5c3TDRM8OvJM7NB4dLCX4x7Dc4ymswQWLYd6mHGfI2MeEw7ymeAKH44M1aTC_YQ0L4CGZsOBi0j2UGn6Pjws-hZIiNovDyRQczoVTxLlsLkB-iZ55M2V4dT336MfnT99vvzZ3374cbz_eNZb3qjRmYECGA2XMqp53fvBQ7x6EAiGJ472Xkg-UOSXVIIyXtrKu42BFRw7c8j16e_m3jv1rg1z0HLKFaTILxC1rqkjXEdFXeI-6C2pTzDmB12sKs0mPmhJ91qxHfdWsz5o1Ybpqrrk31xbbMIP7l_rrtQIfLgDURU8Bks42wGLBhQS2aBfDf1r8Aa-AksU</recordid><startdate>20160430</startdate><enddate>20160430</enddate><creator>El-Zaafarany, Ghada M.</creator><creator>Soliman, Mahmoud E.</creator><creator>Mansour, Samar</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>7TK</scope></search><sort><creationdate>20160430</creationdate><title>Identifying lipidic emulsomes for improved oxcarbazepine brain targeting: In vitro and rat in vivo studies</title><author>El-Zaafarany, Ghada M. ; Soliman, Mahmoud E. ; Mansour, Samar ; Awad, Gehanne A.S.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c398t-ab2e0b4122c8935fbfe122fe68e670d39f773b12d878b6af7c412d53ec65043c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Administration, Intranasal</topic><topic>Animals</topic><topic>Anticonvulsants - administration & dosage</topic><topic>Anticonvulsants - blood</topic><topic>Anticonvulsants - chemistry</topic><topic>Anticonvulsants - pharmacokinetics</topic><topic>Brain - metabolism</topic><topic>Carbamazepine - administration & dosage</topic><topic>Carbamazepine - analogs & derivatives</topic><topic>Carbamazepine - blood</topic><topic>Carbamazepine - chemistry</topic><topic>Carbamazepine - pharmacokinetics</topic><topic>Cell Line, Tumor</topic><topic>Cell Survival - drug effects</topic><topic>Direct nose-to-brain delivery</topic><topic>Drug Carriers - administration & dosage</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Carriers - pharmacokinetics</topic><topic>Drug Liberation</topic><topic>Drug targeting efficiency</topic><topic>Emulsomes</topic><topic>Humans</topic><topic>Intranasal</topic><topic>Lipids - chemistry</topic><topic>Male</topic><topic>Nanoparticles - administration & dosage</topic><topic>Nanoparticles - chemistry</topic><topic>Nasal Mucosa</topic><topic>Oxcarbazepine</topic><topic>Particle Size</topic><topic>Rats, Wistar</topic><topic>Surface Properties</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>El-Zaafarany, Ghada M.</creatorcontrib><creatorcontrib>Soliman, Mahmoud E.</creatorcontrib><creatorcontrib>Mansour, Samar</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>Neurosciences Abstracts</collection><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>El-Zaafarany, Ghada M.</au><au>Soliman, Mahmoud E.</au><au>Mansour, Samar</au><au>Awad, Gehanne A.S.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Identifying lipidic emulsomes for improved oxcarbazepine brain targeting: In vitro and rat in vivo studies</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2016-04-30</date><risdate>2016</risdate><volume>503</volume><issue>1-2</issue><spage>127</spage><epage>140</epage><pages>127-140</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><abstract>[Display omitted]
Lipid-based nanovectors offer effective carriers for brain delivery by improving drug potency and reducing off-target effects. Emulsomes are nano-triglyceride (TG) carriers formed of lipid cores supported by at least one phospholipid (PC) sheath. Due to their surface active properties, PC forms bilayers at the aqueous interface, thereby enabling encapsulated drug to benefit from better bioavailability and stability. Emulsomes of oxcarbazepine (OX) were prepared, aimed to offer nanocarriers for nasal delivery for brain targeting. Different TG cores (Compritol®, tripalmitin, tristearin and triolein) and soya phosphatidylcholine in different amounts and ratios were used for emulsomal preparation. Particles were modulated to generate nanocarriers with suitable size, charge, encapsulation efficiency and prolonged release. Cytotoxicity and pharmacokinetic studies were also implemented. Nano-spherical OX-emulsomes with maximal encapsulation of 96.75% were generated. Stability studies showed changes within 30.6% and 11.2% in the size and EE% after 3 months. MTT assay proved a decrease in drug toxicity by its encapsulation in emulsomes. Incorporation of OX into emulsomes resulted in stable nanoformulations. Tailoring emulsomes properties by modulating the surface charge and particle size produced a stable system for the lipophilic drug with a prolonged release profile and mean residence time and proved direct nose-to-brain transport in rats.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>26924357</pmid><doi>10.1016/j.ijpharm.2016.02.038</doi><tpages>14</tpages></addata></record> |
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| subjects | Administration, Intranasal Animals Anticonvulsants - administration & dosage Anticonvulsants - blood Anticonvulsants - chemistry Anticonvulsants - pharmacokinetics Brain - metabolism Carbamazepine - administration & dosage Carbamazepine - analogs & derivatives Carbamazepine - blood Carbamazepine - chemistry Carbamazepine - pharmacokinetics Cell Line, Tumor Cell Survival - drug effects Direct nose-to-brain delivery Drug Carriers - administration & dosage Drug Carriers - chemistry Drug Carriers - pharmacokinetics Drug Liberation Drug targeting efficiency Emulsomes Humans Intranasal Lipids - chemistry Male Nanoparticles - administration & dosage Nanoparticles - chemistry Nasal Mucosa Oxcarbazepine Particle Size Rats, Wistar Surface Properties |
| title | Identifying lipidic emulsomes for improved oxcarbazepine brain targeting: In vitro and rat in vivo studies |
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