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

作　　者：Jigar Shah Anroop B.Nair Hiral Shah Shery Jacob Tamer M.Shehata Mohamed Aly Morsy 

机构地区：[1]Institute of Pharmacy,Nirma University,Ahmedabad 382481,India [2]College of Clinical Pharmacy,King Faisal University,Al-Ahsa 31982,Saudi Arabia [3]Arihant School of Pharmacy&BRI,Gandhinagar 382421,India [4]College of Pharmacy,Gulf Medical University,Ajman 4184,United Arab Emirates [5]Faculty of Pharmacy,University of Zagazig,Zagazig 44519,Egypt [6]Faculty of Medicine,Minia University,El-Minia 61511,Egypt

出　　处：《Asian Journal of Pharmaceutical Sciences》2020年第6期786-796,共11页亚洲药物制剂科学（英文）

摘　　要：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.

关 键 词：TRAMADOL Proniosomes Flux EDEMA PHARMACOKINETICS Rats 

分 类 号：R943[医药卫生—药剂学]