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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...

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Autores principales: Shah, Jigar, Nair, Anroop B., Shah, Hiral, Jacob, Shery, Shehata, Tamer M., Morsy, Mohamed Aly
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shenyang Pharmaceutical University 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7750831/
https://www.ncbi.nlm.nih.gov/pubmed/33363633
http://dx.doi.org/10.1016/j.ajps.2019.05.001
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author Shah, Jigar
Nair, Anroop B.
Shah, Hiral
Jacob, Shery
Shehata, Tamer M.
Morsy, Mohamed Aly
author_facet Shah, Jigar
Nair, Anroop B.
Shah, Hiral
Jacob, Shery
Shehata, Tamer M.
Morsy, Mohamed Aly
author_sort Shah, Jigar
collection PubMed
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 < 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 < 0.005) in mice and edema (P < 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.
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spelling pubmed-77508312020-12-23 Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel Shah, Jigar Nair, Anroop B. Shah, Hiral Jacob, Shery Shehata, Tamer M. Morsy, Mohamed Aly Asian J Pharm Sci Original Research Paper 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 < 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 < 0.005) in mice and edema (P < 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. Shenyang Pharmaceutical University 2020-11 2019-06-19 /pmc/articles/PMC7750831/ /pubmed/33363633 http://dx.doi.org/10.1016/j.ajps.2019.05.001 Text en © 2019 Shenyang Pharmaceutical University. Published by Elsevier B.V. http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Original Research Paper
Shah, Jigar
Nair, Anroop B.
Shah, Hiral
Jacob, Shery
Shehata, Tamer M.
Morsy, Mohamed Aly
Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel
title Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel
title_full Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel
title_fullStr Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel
title_full_unstemmed Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel
title_short Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel
title_sort enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel
topic Original Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7750831/
https://www.ncbi.nlm.nih.gov/pubmed/33363633
http://dx.doi.org/10.1016/j.ajps.2019.05.001
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