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

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          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 < 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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          Most cited references 39

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          Nonionic surfactant vesicular systems for effective drug delivery—an overview

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            Permeation enhancer strategies in transdermal drug delivery.

            Today, ∼74% of drugs are taken orally and are not found to be as effective as desired. To improve such characteristics, transdermal drug delivery was brought to existence. This delivery system is capable of transporting the drug or macromolecules painlessly through skin into the blood circulation at fixed rate. Topical administration of therapeutic agents offers many advantages over conventional oral and invasive techniques of drug delivery. Several important advantages of transdermal drug delivery are prevention from hepatic first pass metabolism, enhancement of therapeutic efficiency and maintenance of steady plasma level of the drug. Human skin surface, as a site of drug application for both local and systemic effects, is the most eligible candidate available. New controlled transdermal drug delivery systems (TDDS) technologies (electrically-based, structure-based and velocity-based) have been developed and commercialized for the transdermal delivery of troublesome drugs. This review article covers most of the new active transport technologies involved in enhancing the transdermal permeation via effective drug delivery system.
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              Analgesic and anti-inflammatory activities of [6]-gingerol.

              In the present study, the analgesic and anti-inflammatory effects of [6]-gingerol, which is the pungent constituent of ginger, were performed. Intraperitoneal administration of [6]-gingerol (25 mg/kg-50 mg/kg) produced an inhibition of acetic acid-induced writhing response and formalin-induced licking time in the late phase. [6]-Gingerol (50 mg/kg-100 mg/kg) also produced an inhibition of paw edema induced by carrageenin. These results suggested that [6]-gingerol possessed analgesic and anti-inflammatory activities.
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                Author and article information

                Contributors
                Journal
                Asian J Pharm Sci
                Asian J Pharm Sci
                Asian Journal of Pharmaceutical Sciences
                Shenyang Pharmaceutical University
                1818-0876
                2221-285X
                19 June 2019
                November 2020
                19 June 2019
                : 15
                : 6
                : 786-796
                Affiliations
                [a ]Institute of Pharmacy, Nirma University, Ahmedabad 382481, India
                [b ]College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia
                [c ]Arihant School of Pharmacy & BRI, Gandhinagar 382421, India
                [d ]College of Pharmacy, Gulf Medical University, Ajman 4184, United Arab Emirates
                [e ]Faculty of Pharmacy, University of Zagazig, Zagazig 44519, Egypt
                [f ]Faculty of Medicine, Minia University, El-Minia 61511, Egypt
                Author notes
                [* ]Corresponding author. College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia. Tel: +966 536 219868. anair@ 123456kfu.edu.sa
                Article
                S1818-0876(18)31268-6
                10.1016/j.ajps.2019.05.001
                7750831
                © 2019 Shenyang Pharmaceutical University. Published by Elsevier B.V.

                This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

                Categories
                Original Research Paper

                tramadol, proniosomes, flux, edema, pharmacokinetics, rats

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