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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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
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Summary: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 
ISSN:1818-0876
2221-285X
DOI:10.1016/j.ajps.2019.05.001