Effect of Permeation
Enhancers on the Release Behavior and Permeation
Kinetics of Novel Tramadol Lotions
SNH Shah1,
MATahir2, A Safdar1, R Riaz3,
Y Shahzad1,4, M Rabbani1, S Karim5
and 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: E-mail:
gmdogar356@gmail.com Tel:
0092-314-2082826; Fax: 0092-922-383441
Received: 24 March 20121
Revised accepted: 3 December 2012
Tropical
Journal of Pharmaceutical Research, February 2013;
12(1): 27-32
http://dx.doi.org/10.4314/tjpr.v12i1.5
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.
Keyword:
Tramadol, Transdermal delivery, Permeation, Propylene
glycol, Polyethylene glycol, Rabbit skin.
