SNH Shah1,
MA Tahir2,
A Safdar1,
R Riaz3,
Y Shahzad1,4,
M Rabbani1,
S Karim5,
G Murtaza6
1Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan;
2Department of Pharmacy, University of Lahore, Lahore, Pakistan;
3SNS Pharmaceutical Research Laboratory, Multan, Pakistan;
4Division of Pharmacy and Pharmaceutical Sciences, School of Applied Sciences, University of Huddersfield HD1 3DH, UK;
5College of Pharmacy, University of the Punjab, Lahore, Pakistan;
6Department of Pharmaceutical Sciences, COMSATS Institute of Information Technology, Abbottabad-22060, Pakistan.
For correspondence:- G Murtaza
Email: gmdogar356@gmail.com Tel:+00923142082826
Received: 24 March 2012
Accepted: 3 December 2012
Published: 21 February 2013
Citation:
Shah S, Tahir M, Safdar A, Riaz R, Shahzad Y, Rabbani M, et al.
Effect of Permeation Enhancers on the Release Behavior and Permeation Kinetics of Novel Tramadol Lotions. Trop J Pharm Res 2013; 12(1):27-32
doi:
10.4314/tjpr.v12i1.5
© 2013 The authors.
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Abstract
Purpose: The aim of this research work was to formulate, characterize and evaluate the in vitro permeation behavior of tramadol lotion containing propylene glycol (PG) and polyethylene glycol (PEG) as permeation enhancers.
Methods: The permeation experiments were conducted in vitro using full thickness rabbit skin in Franz diffusion cells. The donor compartment was filled with PBS (phosphate buffered saline) at pH 7.4 ± 0.1. The receptor phase was continuously stirred PBS (pH 7.4) at 37 °C ± 0.5. The amount of tramadol permeated into the receptor phase was determined spectrophotometrically at 271 nm. Various permeation parameters such as permeation coefficient (Kp), diffusion coefficient (D), flux (J), input rate, and enhancement ratio were obtained using Fick’s diffusion laws.
Results: Permeation increased with increase in the concentrations of both enhancers tested. Maximum cumulative amount permeated for control lotion (Lc) was 357 µg/cm2/min with input rate 0.574 µg/min and lag time (tlag) of 34.93 min, while for the optimum test lotion (L4, containing 8 % PG/PEG in ratio of 1:1 v/v), it was 926 µg/cm2/min, 1.482 µg/min and 58.36 min, respectively. The significantly (p < 0.05) higher permeability shown by the test lotion L4 can be attributed, in part, to the interaction of PG with intercellular lipids leading to the disruption of their organization and increasing their fluidity, and also partly as a result of solubilization of lipid bilayers by PEG.
Conclusion: A binary system of PG and PEG in lotion can be successfully utilized for the permeation enhancement of tramadol.
Keywords: Tramadol, Transdermal delivery, Permeation, Propylene glycol, Polyethylene glycol, Rabbit skin