A comparison of dissolving microneedles and transdermal film with solid microneedles for iloperidone in vivo: a proof of concept
Iloperidone (ILO) is a poorly soluble and bioavailable WHO-approved schizophrenia drug. Microneedles are a revolutionary delivery technology that overcomes many of the issues associated with traditional drug administration. The current research aimed to compare the antipsychotic activity and pharmac...
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| Veröffentlicht in: | Naunyn-Schmiedeberg's archives of pharmacology 2023-02, Vol.396 (2), p.239-246 |
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| creator | Bhadale, Rupali S. Londhe, Vaishali Y. |
| description | Iloperidone (ILO) is a poorly soluble and bioavailable WHO-approved schizophrenia drug. Microneedles are a revolutionary delivery technology that overcomes many of the issues associated with traditional drug administration. The current research aimed to compare the antipsychotic activity and pharmacokinetics of ILO-loaded dissolving microneedles (DMNs) and transdermal film with a solid microneedle (STF). The DMNs were fabricated using the micromolding process, while the transdermal film was created using the solvent casting approach. Furthermore, an in vivo pharmacokinetic, pharmacodynamic, and skin irritation study was performed on Wistar rats. Studies were compared with transdermal film (TF) on untreated skin as a passive control. STF and DMNs had considerably greater AUC and
C
max
(
p
≤ 0.001) than transdermal film. In pharmacodynamic tests, STF and DMNs demonstrated significant (
p
≤ 0.001) forelimb retraction time (FRT) and hindlimb retraction time (HRT) delay responses as compared to control and TF. In the skin irritation test, no adverse effects such as erythema or edema were observed at the end of the 48 h. Thus, antipsychotic activity (paw test) and pharmacokinetics studies revealed sustained action of DMN and STF. This research revealed that improved efficacy of DMN and STF for antipsychotic drug delivery may be an alternative to the existing dosage form. |
| doi_str_mv | 10.1007/s00210-022-02309-0 |
| format | Article |
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C
max
(
p
≤ 0.001) than transdermal film. In pharmacodynamic tests, STF and DMNs demonstrated significant (
p
≤ 0.001) forelimb retraction time (FRT) and hindlimb retraction time (HRT) delay responses as compared to control and TF. In the skin irritation test, no adverse effects such as erythema or edema were observed at the end of the 48 h. Thus, antipsychotic activity (paw test) and pharmacokinetics studies revealed sustained action of DMN and STF. This research revealed that improved efficacy of DMN and STF for antipsychotic drug delivery may be an alternative to the existing dosage form.</description><identifier>ISSN: 0028-1298</identifier><identifier>EISSN: 1432-1912</identifier><identifier>DOI: 10.1007/s00210-022-02309-0</identifier><identifier>PMID: 36271937</identifier><language>eng</language><publisher>Berlin/Heidelberg: Springer Berlin Heidelberg</publisher><subject>Administration, Cutaneous ; Animals ; Antipsychotic Agents ; Antipsychotics ; Biomedical and Life Sciences ; Biomedicine ; Drug delivery ; Drug Delivery Systems ; Edema ; Erythema ; Irritation ; Limbs ; Mental disorders ; Neurosciences ; Pharmacodynamics ; Pharmacokinetics ; Pharmacology/Toxicology ; Psychotropic drugs ; Rats ; Rats, Wistar ; Schizophrenia ; Skin tests</subject><ispartof>Naunyn-Schmiedeberg's archives of pharmacology, 2023-02, Vol.396 (2), p.239-246</ispartof><rights>The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature 2022. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law.</rights><rights>2022. The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c305t-a0ae97c3a4ec09911973de00ccd18c4dfdcc4a99df42c3bda942ce49bc0ccfa73</citedby><cites>FETCH-LOGICAL-c305t-a0ae97c3a4ec09911973de00ccd18c4dfdcc4a99df42c3bda942ce49bc0ccfa73</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s00210-022-02309-0$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s00210-022-02309-0$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,780,784,27924,27925,41488,42557,51319</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/36271937$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Bhadale, Rupali S.</creatorcontrib><creatorcontrib>Londhe, Vaishali Y.</creatorcontrib><title>A comparison of dissolving microneedles and transdermal film with solid microneedles for iloperidone in vivo: a proof of concept</title><title>Naunyn-Schmiedeberg's archives of pharmacology</title><addtitle>Naunyn-Schmiedeberg's Arch Pharmacol</addtitle><addtitle>Naunyn Schmiedebergs Arch Pharmacol</addtitle><description>Iloperidone (ILO) is a poorly soluble and bioavailable WHO-approved schizophrenia drug. Microneedles are a revolutionary delivery technology that overcomes many of the issues associated with traditional drug administration. The current research aimed to compare the antipsychotic activity and pharmacokinetics of ILO-loaded dissolving microneedles (DMNs) and transdermal film with a solid microneedle (STF). The DMNs were fabricated using the micromolding process, while the transdermal film was created using the solvent casting approach. Furthermore, an in vivo pharmacokinetic, pharmacodynamic, and skin irritation study was performed on Wistar rats. Studies were compared with transdermal film (TF) on untreated skin as a passive control. STF and DMNs had considerably greater AUC and
C
max
(
p
≤ 0.001) than transdermal film. In pharmacodynamic tests, STF and DMNs demonstrated significant (
p
≤ 0.001) forelimb retraction time (FRT) and hindlimb retraction time (HRT) delay responses as compared to control and TF. In the skin irritation test, no adverse effects such as erythema or edema were observed at the end of the 48 h. Thus, antipsychotic activity (paw test) and pharmacokinetics studies revealed sustained action of DMN and STF. This research revealed that improved efficacy of DMN and STF for antipsychotic drug delivery may be an alternative to the existing dosage form.</description><subject>Administration, Cutaneous</subject><subject>Animals</subject><subject>Antipsychotic Agents</subject><subject>Antipsychotics</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Drug delivery</subject><subject>Drug Delivery Systems</subject><subject>Edema</subject><subject>Erythema</subject><subject>Irritation</subject><subject>Limbs</subject><subject>Mental disorders</subject><subject>Neurosciences</subject><subject>Pharmacodynamics</subject><subject>Pharmacokinetics</subject><subject>Pharmacology/Toxicology</subject><subject>Psychotropic drugs</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Schizophrenia</subject><subject>Skin tests</subject><issn>0028-1298</issn><issn>1432-1912</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2023</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><recordid>eNp9kEtLAzEUhYMotlb_gAsJuB69SaYzjbtSfIHgRtchzaOmzCRjMq2486eb2qq4ERIu3Pvdc5KD0CmBCwJQXyYASqAASvNlwAvYQ0NSMloQTug-Gub5pCCUTwboKKUlAFRkPD5EA1bRmnBWD9HHFKvQdjK6FDwOFmuXUmjWzi9w61QM3hjdmISl17iP0idtYisbbF3T4jfXv-CMO_0XtiFi14TORKdzEzuP124drrDEXQzZJR8VvDJdf4wOrGySOdnVEXq-uX6a3RUPj7f3s-lDoRiM-0KCNLxWTJZGAeeE8JppA6CUJhNVaquVKiXn2pZUsbmWPFdT8rnKiJU1G6HzrW5-wOvKpF4swyr6bCloXTFSEVpBpuiWyp9JKRoruuhaGd8FAbEJXWxDFzl08RW62Cyd7aRX89bon5XvlDPAtkDKI78w8df7H9lPiVWQAw</recordid><startdate>20230201</startdate><enddate>20230201</enddate><creator>Bhadale, Rupali S.</creator><creator>Londhe, Vaishali Y.</creator><general>Springer Berlin Heidelberg</general><general>Springer Nature 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>3V.</scope><scope>7QP</scope><scope>7TK</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>K9.</scope><scope>M0S</scope><scope>M1P</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope></search><sort><creationdate>20230201</creationdate><title>A comparison of dissolving microneedles and transdermal film with solid microneedles for iloperidone in vivo: a proof of concept</title><author>Bhadale, Rupali S. ; Londhe, Vaishali Y.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c305t-a0ae97c3a4ec09911973de00ccd18c4dfdcc4a99df42c3bda942ce49bc0ccfa73</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2023</creationdate><topic>Administration, Cutaneous</topic><topic>Animals</topic><topic>Antipsychotic Agents</topic><topic>Antipsychotics</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Drug delivery</topic><topic>Drug Delivery Systems</topic><topic>Edema</topic><topic>Erythema</topic><topic>Irritation</topic><topic>Limbs</topic><topic>Mental disorders</topic><topic>Neurosciences</topic><topic>Pharmacodynamics</topic><topic>Pharmacokinetics</topic><topic>Pharmacology/Toxicology</topic><topic>Psychotropic drugs</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Schizophrenia</topic><topic>Skin tests</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Bhadale, Rupali S.</creatorcontrib><creatorcontrib>Londhe, Vaishali Y.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni)</collection><collection>ProQuest Central</collection><collection>ProQuest Central</collection><collection>ProQuest One Community College</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><jtitle>Naunyn-Schmiedeberg's archives of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Bhadale, Rupali S.</au><au>Londhe, Vaishali Y.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>A comparison of dissolving microneedles and transdermal film with solid microneedles for iloperidone in vivo: a proof of concept</atitle><jtitle>Naunyn-Schmiedeberg's archives of pharmacology</jtitle><stitle>Naunyn-Schmiedeberg's Arch Pharmacol</stitle><addtitle>Naunyn Schmiedebergs Arch Pharmacol</addtitle><date>2023-02-01</date><risdate>2023</risdate><volume>396</volume><issue>2</issue><spage>239</spage><epage>246</epage><pages>239-246</pages><issn>0028-1298</issn><eissn>1432-1912</eissn><abstract>Iloperidone (ILO) is a poorly soluble and bioavailable WHO-approved schizophrenia drug. Microneedles are a revolutionary delivery technology that overcomes many of the issues associated with traditional drug administration. The current research aimed to compare the antipsychotic activity and pharmacokinetics of ILO-loaded dissolving microneedles (DMNs) and transdermal film with a solid microneedle (STF). The DMNs were fabricated using the micromolding process, while the transdermal film was created using the solvent casting approach. Furthermore, an in vivo pharmacokinetic, pharmacodynamic, and skin irritation study was performed on Wistar rats. Studies were compared with transdermal film (TF) on untreated skin as a passive control. STF and DMNs had considerably greater AUC and
C
max
(
p
≤ 0.001) than transdermal film. In pharmacodynamic tests, STF and DMNs demonstrated significant (
p
≤ 0.001) forelimb retraction time (FRT) and hindlimb retraction time (HRT) delay responses as compared to control and TF. In the skin irritation test, no adverse effects such as erythema or edema were observed at the end of the 48 h. Thus, antipsychotic activity (paw test) and pharmacokinetics studies revealed sustained action of DMN and STF. This research revealed that improved efficacy of DMN and STF for antipsychotic drug delivery may be an alternative to the existing dosage form.</abstract><cop>Berlin/Heidelberg</cop><pub>Springer Berlin Heidelberg</pub><pmid>36271937</pmid><doi>10.1007/s00210-022-02309-0</doi><tpages>8</tpages></addata></record> |
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| source | MEDLINE; SpringerNature Complete Journals |
| subjects | Administration, Cutaneous Animals Antipsychotic Agents Antipsychotics Biomedical and Life Sciences Biomedicine Drug delivery Drug Delivery Systems Edema Erythema Irritation Limbs Mental disorders Neurosciences Pharmacodynamics Pharmacokinetics Pharmacology/Toxicology Psychotropic drugs Rats Rats, Wistar Schizophrenia Skin tests |
| title | A comparison of dissolving microneedles and transdermal film with solid microneedles for iloperidone in vivo: a proof of concept |
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