Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel

Oral therapy of tramadol, an opiate analgesic, undergoes extensive hepatic metabolism and requires frequent administration. Transdermal therapy by virtue can overcome these issues and can improve the efficacy and reduce abuse liability of tramadol. The aim of this research was to investigate the pos...

Full description

Saved in:
Bibliographic Details
Published in:Asian journal of pharmceutical sciences 2020-11, Vol.15 (6), p.786-796
Main Authors: Shah, Jigar, Nair, Anroop B., Shah, Hiral, Jacob, Shery, Shehata, Tamer M., Morsy, Mohamed Aly
Format: Article
Language:English
Subjects:
Edema
Flux
Original Research Paper
Pharmacokinetics
Proniosomes
Rats
Tramadol
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
cited_by cdi_FETCH-LOGICAL-c521t-4903aad81dcb98c616edcf3ccb22a247b74371361908851645a35d67bc1e8aba3
cites cdi_FETCH-LOGICAL-c521t-4903aad81dcb98c616edcf3ccb22a247b74371361908851645a35d67bc1e8aba3
container_end_page 796
container_issue 6
container_start_page 786
container_title Asian journal of pharmceutical sciences
container_volume 15
creator Shah, Jigar
Nair, Anroop B.
Shah, Hiral
Jacob, Shery
Shehata, Tamer M.
Morsy, Mohamed Aly
description Oral therapy of tramadol, an opiate analgesic, undergoes extensive hepatic metabolism and requires frequent administration. Transdermal therapy by virtue can overcome these issues and can improve the efficacy and reduce abuse liability of tramadol. The aim of this research was to investigate the possibility of transdermal delivery of tramadol by formulating proniosome gel and evaluate its therapeutic potential in vivo. The effect of formulation composition as well as amount of drug on physicochemical characteristics of prepared proniosomes were examined. Best proniosome gel (F4) was selected and evaluated for drug release, stability and transdermal efficacy by ex vivo and in vivo experiments. The vesicles demonstrated optimal properties including spherical shape, nanosize with good entrapment efficiency, adequate zeta potential, higher stability and greater transdermal flux. The amorphization and dispersion of tramadol in the aqueous core of proniosome vesicles was confirmed by differential scanning calorimeter. Release profile of F4 was distinct (P 
doi_str_mv 10.1016/j.ajps.2019.05.001
format article
fullrecord <record><control><sourceid>elsevier_doaj_</sourceid><recordid>TN_cdi_doaj_primary_oai_doaj_org_article_fd693038b64b4f9295872d2e1def16bd</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S1818087618312686</els_id><doaj_id>oai_doaj_org_article_fd693038b64b4f9295872d2e1def16bd</doaj_id><sourcerecordid>S1818087618312686</sourcerecordid><originalsourceid>FETCH-LOGICAL-c521t-4903aad81dcb98c616edcf3ccb22a247b74371361908851645a35d67bc1e8aba3</originalsourceid><addsrcrecordid>eNp9kd2K1DAUgIMo7jDuC3ghfYHWnKRNUhBBllUXFrxR8C7kdzalTYakDszbm-7o4t5ILpKcnPMlOR9CbwF3gIG9nzo1HUtHMIwdHjqM4QXaEUKgJWL4-RLtQIBoseDsCl2XMuGaQTkH0b9GV5RSVgfdIX8bH1Q0bnFxbUJsVFxDTCYYd1zDydW9fYy1IfpZLYtaUz43zntn1tIk36xZLcqmudHnbR2LdXlRc3PMKYZU0uKag5vfoFdezcVd_5n36Mfn2-83X9v7b1_ubj7dt2YgsLb9iKlSVoA1ehSGAXPWeGqMJkSRnmveUw6UwYiFGID1g6KDZVwbcEJpRffo7sK1SU3ymMOi8lkmFeRjIOWDVHkNZnbSWzZSTIVmve79SMZBcGKJA-s8MG0r6-OFdfyll_qO2qGs5mfQ5ycxPMhDOknOBywoVAC5AExOpWTnn2oBy02inOQmUW4SJR7kpmiP3v1761PJX2U14cMlwdU-noLLspjgqkIbcpVSPxr-x_8NRsmw5Q</addsrcrecordid><sourcetype>Open Website</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype></control><display><type>article</type><title>Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel</title><source>ScienceDirect®</source><source>PubMed Central</source><creator>Shah, Jigar ; Nair, Anroop B. ; Shah, Hiral ; Jacob, Shery ; Shehata, Tamer M. ; Morsy, Mohamed Aly</creator><creatorcontrib>Shah, Jigar ; Nair, Anroop B. ; Shah, Hiral ; Jacob, Shery ; Shehata, Tamer M. ; Morsy, Mohamed Aly</creatorcontrib><description>Oral therapy of tramadol, an opiate analgesic, undergoes extensive hepatic metabolism and requires frequent administration. Transdermal therapy by virtue can overcome these issues and can improve the efficacy and reduce abuse liability of tramadol. The aim of this research was to investigate the possibility of transdermal delivery of tramadol by formulating proniosome gel and evaluate its therapeutic potential in vivo. The effect of formulation composition as well as amount of drug on physicochemical characteristics of prepared proniosomes were examined. Best proniosome gel (F4) was selected and evaluated for drug release, stability and transdermal efficacy by ex vivo and in vivo experiments. The vesicles demonstrated optimal properties including spherical shape, nanosize with good entrapment efficiency, adequate zeta potential, higher stability and greater transdermal flux. The amorphization and dispersion of tramadol in the aqueous core of proniosome vesicles was confirmed by differential scanning calorimeter. Release profile of F4 was distinct (P &lt; 0.001) from control and displayed steady and prolonged tramadol release by Fickian diffusion. Transdermal therapy of F4 showed prominent reduction of induced twitches (P &lt; 0.005) in mice and edema (P &lt; 0.05) in rats, as compared to oral tramadol. The improvement in clinical efficacy of tramadol in transdermal therapy is correlated with the pharmacokinetic data observed. In conclusion, the observed improvement in antinociceptive and anti-inflammatory effects from proniosome carriers signifies its potential to be a suitable alternative to oral therapy of tramadol with greater efficacy. [Display omitted]</description><identifier>ISSN: 1818-0876</identifier><identifier>EISSN: 2221-285X</identifier><identifier>DOI: 10.1016/j.ajps.2019.05.001</identifier><identifier>PMID: 33363633</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Edema ; Flux ; Original Research Paper ; Pharmacokinetics ; Proniosomes ; Rats ; Tramadol</subject><ispartof>Asian journal of pharmceutical sciences, 2020-11, Vol.15 (6), p.786-796</ispartof><rights>2019 Shenyang Pharmaceutical University</rights><rights>2019 Shenyang Pharmaceutical University. Published by Elsevier B.V.</rights><rights>2019 Shenyang Pharmaceutical University. Published by Elsevier B.V. 2019 Shenyang Pharmaceutical University</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c521t-4903aad81dcb98c616edcf3ccb22a247b74371361908851645a35d67bc1e8aba3</citedby><cites>FETCH-LOGICAL-c521t-4903aad81dcb98c616edcf3ccb22a247b74371361908851645a35d67bc1e8aba3</cites><orcidid>0000-0003-2850-8669</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC7750831/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S1818087618312686$$EHTML$$P50$$Gelsevier$$Hfree_for_read</linktohtml><link.rule.ids>230,314,727,780,784,885,3549,27924,27925,45780,53791,53793</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/33363633$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Shah, Jigar</creatorcontrib><creatorcontrib>Nair, Anroop B.</creatorcontrib><creatorcontrib>Shah, Hiral</creatorcontrib><creatorcontrib>Jacob, Shery</creatorcontrib><creatorcontrib>Shehata, Tamer M.</creatorcontrib><creatorcontrib>Morsy, Mohamed Aly</creatorcontrib><title>Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel</title><title>Asian journal of pharmceutical sciences</title><addtitle>Asian J Pharm Sci</addtitle><description>Oral therapy of tramadol, an opiate analgesic, undergoes extensive hepatic metabolism and requires frequent administration. Transdermal therapy by virtue can overcome these issues and can improve the efficacy and reduce abuse liability of tramadol. The aim of this research was to investigate the possibility of transdermal delivery of tramadol by formulating proniosome gel and evaluate its therapeutic potential in vivo. The effect of formulation composition as well as amount of drug on physicochemical characteristics of prepared proniosomes were examined. Best proniosome gel (F4) was selected and evaluated for drug release, stability and transdermal efficacy by ex vivo and in vivo experiments. The vesicles demonstrated optimal properties including spherical shape, nanosize with good entrapment efficiency, adequate zeta potential, higher stability and greater transdermal flux. The amorphization and dispersion of tramadol in the aqueous core of proniosome vesicles was confirmed by differential scanning calorimeter. Release profile of F4 was distinct (P &lt; 0.001) from control and displayed steady and prolonged tramadol release by Fickian diffusion. Transdermal therapy of F4 showed prominent reduction of induced twitches (P &lt; 0.005) in mice and edema (P &lt; 0.05) in rats, as compared to oral tramadol. The improvement in clinical efficacy of tramadol in transdermal therapy is correlated with the pharmacokinetic data observed. In conclusion, the observed improvement in antinociceptive and anti-inflammatory effects from proniosome carriers signifies its potential to be a suitable alternative to oral therapy of tramadol with greater efficacy. [Display omitted]</description><subject>Edema</subject><subject>Flux</subject><subject>Original Research Paper</subject><subject>Pharmacokinetics</subject><subject>Proniosomes</subject><subject>Rats</subject><subject>Tramadol</subject><issn>1818-0876</issn><issn>2221-285X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2020</creationdate><recordtype>article</recordtype><sourceid>DOA</sourceid><recordid>eNp9kd2K1DAUgIMo7jDuC3ghfYHWnKRNUhBBllUXFrxR8C7kdzalTYakDszbm-7o4t5ILpKcnPMlOR9CbwF3gIG9nzo1HUtHMIwdHjqM4QXaEUKgJWL4-RLtQIBoseDsCl2XMuGaQTkH0b9GV5RSVgfdIX8bH1Q0bnFxbUJsVFxDTCYYd1zDydW9fYy1IfpZLYtaUz43zntn1tIk36xZLcqmudHnbR2LdXlRc3PMKYZU0uKag5vfoFdezcVd_5n36Mfn2-83X9v7b1_ubj7dt2YgsLb9iKlSVoA1ehSGAXPWeGqMJkSRnmveUw6UwYiFGID1g6KDZVwbcEJpRffo7sK1SU3ymMOi8lkmFeRjIOWDVHkNZnbSWzZSTIVmve79SMZBcGKJA-s8MG0r6-OFdfyll_qO2qGs5mfQ5ycxPMhDOknOBywoVAC5AExOpWTnn2oBy02inOQmUW4SJR7kpmiP3v1761PJX2U14cMlwdU-noLLspjgqkIbcpVSPxr-x_8NRsmw5Q</recordid><startdate>20201101</startdate><enddate>20201101</enddate><creator>Shah, Jigar</creator><creator>Nair, Anroop B.</creator><creator>Shah, Hiral</creator><creator>Jacob, Shery</creator><creator>Shehata, Tamer M.</creator><creator>Morsy, Mohamed Aly</creator><general>Elsevier B.V</general><general>Shenyang Pharmaceutical University</general><general>Elsevier</general><scope>6I.</scope><scope>AAFTH</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>5PM</scope><scope>DOA</scope><orcidid>https://orcid.org/0000-0003-2850-8669</orcidid></search><sort><creationdate>20201101</creationdate><title>Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel</title><author>Shah, Jigar ; Nair, Anroop B. ; Shah, Hiral ; Jacob, Shery ; Shehata, Tamer M. ; Morsy, Mohamed Aly</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c521t-4903aad81dcb98c616edcf3ccb22a247b74371361908851645a35d67bc1e8aba3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2020</creationdate><topic>Edema</topic><topic>Flux</topic><topic>Original Research Paper</topic><topic>Pharmacokinetics</topic><topic>Proniosomes</topic><topic>Rats</topic><topic>Tramadol</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Shah, Jigar</creatorcontrib><creatorcontrib>Nair, Anroop B.</creatorcontrib><creatorcontrib>Shah, Hiral</creatorcontrib><creatorcontrib>Jacob, Shery</creatorcontrib><creatorcontrib>Shehata, Tamer M.</creatorcontrib><creatorcontrib>Morsy, Mohamed Aly</creatorcontrib><collection>ScienceDirect Open Access Titles</collection><collection>Elsevier:ScienceDirect:Open Access</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>PubMed Central (Full Participant titles)</collection><collection>Directory of Open Access Journals</collection><jtitle>Asian journal of pharmceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Shah, Jigar</au><au>Nair, Anroop B.</au><au>Shah, Hiral</au><au>Jacob, Shery</au><au>Shehata, Tamer M.</au><au>Morsy, Mohamed Aly</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel</atitle><jtitle>Asian journal of pharmceutical sciences</jtitle><addtitle>Asian J Pharm Sci</addtitle><date>2020-11-01</date><risdate>2020</risdate><volume>15</volume><issue>6</issue><spage>786</spage><epage>796</epage><pages>786-796</pages><issn>1818-0876</issn><eissn>2221-285X</eissn><abstract>Oral therapy of tramadol, an opiate analgesic, undergoes extensive hepatic metabolism and requires frequent administration. Transdermal therapy by virtue can overcome these issues and can improve the efficacy and reduce abuse liability of tramadol. The aim of this research was to investigate the possibility of transdermal delivery of tramadol by formulating proniosome gel and evaluate its therapeutic potential in vivo. The effect of formulation composition as well as amount of drug on physicochemical characteristics of prepared proniosomes were examined. Best proniosome gel (F4) was selected and evaluated for drug release, stability and transdermal efficacy by ex vivo and in vivo experiments. The vesicles demonstrated optimal properties including spherical shape, nanosize with good entrapment efficiency, adequate zeta potential, higher stability and greater transdermal flux. The amorphization and dispersion of tramadol in the aqueous core of proniosome vesicles was confirmed by differential scanning calorimeter. Release profile of F4 was distinct (P &lt; 0.001) from control and displayed steady and prolonged tramadol release by Fickian diffusion. Transdermal therapy of F4 showed prominent reduction of induced twitches (P &lt; 0.005) in mice and edema (P &lt; 0.05) in rats, as compared to oral tramadol. The improvement in clinical efficacy of tramadol in transdermal therapy is correlated with the pharmacokinetic data observed. In conclusion, the observed improvement in antinociceptive and anti-inflammatory effects from proniosome carriers signifies its potential to be a suitable alternative to oral therapy of tramadol with greater efficacy. [Display omitted]</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>33363633</pmid><doi>10.1016/j.ajps.2019.05.001</doi><tpages>11</tpages><orcidid>https://orcid.org/0000-0003-2850-8669</orcidid><oa>free_for_read</oa></addata></record>
fulltext fulltext
identifier ISSN: 1818-0876
ispartof Asian journal of pharmceutical sciences, 2020-11, Vol.15 (6), p.786-796
issn 1818-0876
2221-285X
language eng
recordid cdi_doaj_primary_oai_doaj_org_article_fd693038b64b4f9295872d2e1def16bd
source ScienceDirect®; PubMed Central
subjects Edema
Flux
Original Research Paper
Pharmacokinetics
Proniosomes
Rats
Tramadol
title Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel
url http://sfxeu10.hosted.exlibrisgroup.com/loughborough?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-01T10%3A25%3A33IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-elsevier_doaj_&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Enhancement%20in%20antinociceptive%20and%20anti-inflammatory%20effects%20of%20tramadol%20by%20transdermal%20proniosome%20gel&rft.jtitle=Asian%20journal%20of%20pharmceutical%20sciences&rft.au=Shah,%20Jigar&rft.date=2020-11-01&rft.volume=15&rft.issue=6&rft.spage=786&rft.epage=796&rft.pages=786-796&rft.issn=1818-0876&rft.eissn=2221-285X&rft_id=info:doi/10.1016/j.ajps.2019.05.001&rft_dat=%3Celsevier_doaj_%3ES1818087618312686%3C/elsevier_doaj_%3E%3Cgrp_id%3Ecdi_FETCH-LOGICAL-c521t-4903aad81dcb98c616edcf3ccb22a247b74371361908851645a35d67bc1e8aba3%3C/grp_id%3E%3Coa%3E%3C/oa%3E%3Curl%3E%3C/url%3E&rft_id=info:oai/&rft_id=info:pmid/33363633&rfr_iscdi=true