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THE PHARMA REVIEW
(NOVEMBER - DECEMBER 2011) |
InVitro penetration Study of
Diclofenac Sodium Using the Human Cadaver Skin.
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Rahul M1*,
Swati R2 Ambrish T3
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Abstract: The skin is very effective as a
selective penetration barrier. Percutaneous absorption
involves the passage of the drug molecule from the skin
surface into the stratum corneum under the influence of
a concentration gradient and its subsequent diffusion
through the stratum corneum and underlying epidermis,
through the dermis, and into the blood circulation.
There is currently a great deal of world-wide interest
in the field of transdermal drug delivery and,
consequently, broad classes of drugs are being evaluated
for percutaneous absorption potential. The advantages of
this mode of drug administration are numerous, the
patient convenience and therapeutic optimization of
using patch transdermal systems being major positive
features. The in vitro release test is a measure of in
process control and also as a finished product
specification for example, gels, emugel and spray. An in
vitro diffusion cell experiment was designed to
demonstrate the rate of release of Diclofenac sodium
from three different topical formulations: (i) gels,
(ii) emugel and (iii) spray. In vitro release of
Diclofenac sodium from three different formulations
through the receptor phase through human cadaver skin
was monitored chromatographically. By monitoring and
attempting to explain the numerous possible from the
three formulations, it was a better to understanding of
the complexities of transdermal drug administration.
More over spray topical formulation could be suggested
as a good dosage form for the topical delivery of
Diclofenac sodium, giving higher drug release than the
gel and emugel formulations.
Introduction: The skin is the largest human
organ. It ensures that harmful substances and drugs
released from topically applied formulations cannot
intrude into the organism offhand [1]. Drug delivery
through the skin has been used to target the epidermis,
dermis and deeper tissues and for systemic delivery. The
major barrier for the transport of drugs through the
skin is the stratum corneum, with most transport
occurring through the intercellular region. When taken
orally, many drugs are destroyed by the liver. Drug
administration through the skin often pro-vides a
slower, more controlled alternative route for release
into the blood stream. There is currently a great deal
of world-wide interest in the field of trans-dermal drug
delivery and, consequently, broad classes of drugs are
being evaluated for percutaneous absorption potential.
Another potential ad-vantage of this type of drug
delivery is the optimization of drug concentration at
the desirable sites, reducing the chances of side
effects [2]. Therapeutic efficacy of any topical
formulation depends on its ability to deliver drugs to
their sites of action from the skin surface for either
local or systemic purposes. [3, 4]. Diclofenac sodium
(2-[2-[(2, 6-dichlorophenyl) amino] phenyl] acetic acid)
is a potent member of non-steroidal anti-inflammatory
drugs (NSAIDS) and widely used clinically, because of
its strong analgesic and anti-pyretic effect [5].It has
a short half-life (2 hrs). Diclofenac sodium causes
gastrointestinal disturbances, peptic ulceration with
bleeding, if present in large doses in gastrointestinal
tract [6].It is marketed as injections, oral sustained
release tablets and topical formulations. After oral
administration, it is extensively metabolized in the
liver and because of its short biological half-life, the
drug has to be administered frequently [7]. The topical
application allows for a higher local concentration of
the drug at the site of initiation of the pain and lower
or negligible systemic drug levels producing fewer or
not adverse drug effects [8]. Topical drugs used to
control pain act locally on damaged or dysfunctional
soft tissues or peripheral nerves, and their actions may
be on the inflammatory response itself or on sensory
neurons [2]. A Diclofenac formulation with a high degree
of skin permeation could be useful in the treatment of
not only locally inflamed skin tissues, but also
inflammatory and painful states of supporting structures
of the body bones, ligaments, joints, tendons and
muscles [9, 10]. The present work aims to evaluate that
in vitro release of Diclofenac sodium from the different
formulations.
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