Documente Academic
Documente Profesional
Documente Cultură
INT.J.PH.SCI.,SEP-DEC, 2010;2(3):708-716
ISSN 0975-4725
www.ijps.info
SINGH ANISHA*, SHARMA PRAMOD KUMAR, GARG VIPIN KUMAR, GARG GARIMA
Department of Pharmaceutical Technology, Meerut Institute of Engineering & Technology, NH-58, Baghpat
Bypass Crossing, Delhi- Haridwar Highway, Meerut – 250005, U.P., India
*Corresponding author email id: anishapharma24@gmail.com, Mob. no: 09557501533
ABSTRACT
Transdermal route of drug delivery is preferred over the other routes for administration of drugs as it has several additional advantages, to
name a few, it is a non-invasive technique requiring less dosing frequency and abolishes the first pass metabolism. However, the drug is
unable to permeate the skin barriers properly, so penetration enhancers are used to overcome this problem. The present review focuses on
transdermal drug delivery system, the role of penetration enhancers and various techniques which are used to increase the penetration of
drug through the skin.
Key Words: Transdermal, Penetration enhancers, Iontophoresis, Lipid Fluidisation
Penetration enhancement is the most important where Cp-Cr is the difference in permeant concentration
consideration for improving flux. Flux (J) can be defined across the membrane and A is the area of application[7]
as the amount (M) of material flowing through unit area
of cross section (S) of a barrier in unit time (t). Flux can Approaches of penetration enhancement
[6]
be given by : A. Drug vehicle based
J=dM/S.dt 1. Drug selection
Each phase of the membrane can be characterized in 2. Vesicles and particles
terms of diffusional resistance(R), which usually is the 3. Prodrugs and ion pairs
function of thickness (hs) of the phase, the permeant 4. Chemical potential of drug
diffusion coefficient (Ds) within the phase, and the 5. Eutectic systems
partition coefficient (Ks) between the membrane phase 6. Complexes
and external phase.It can be expressed as: B. Physical method
R=hs/Ds.Ks, P=Ds.Ks/hs 1. Iontophoresis
where P is permeability coefficient. The permeability 2. Ultrasound (phonophoresis and sonophoresis)
coefficient is related to membrane flux (J) as given 3. Mechanoporation (Microneedle based devices)
J=APs (Cp-Cr), 4. Electroporation
cyclodextrin concentration is sufficient to complex only region compared to the higher 1MHz energy used in
the drug that is in excess of its solubility, an increase in physiotherapy, across the skin. The ultrasound energy
flux might be expected. However, at higher cyclodextrin pulses have the capability of producing both a physical
concentrations, the excess cyclodextrin would be increase in air pressure above the topical application site
expected to complex free drug and hence reduce and the tissue effects utilised in medical therapy
flux.Complexation with cyclodextrins has been variously applications. However, ultrasound-facilitated
reported to both increase and decrease skin penetration. transdermal delivery has not yet been tried and tested in
Skin penetration enhancement has also been attributed to the clinical field. Therefore, it’s acceptance as a routine
extraction of stratum corneum lipids by cyclodextrins mechanism for topical delivery of macromolecules is
[45].
still hypothetical [46, 47].
increased skin hydration may swell and open the intercalate between stratum corneum ceramides to create
structure of the stratum corneum leading to an increase spatial disruption [51].
in penetration, although it is yet to be demonstrated
experimentally. For example, Scheuplein and Blank CONCLUSION
showed that the diffusion coefficients of alcohols in Successful delivery of transdermal devices requires
hydrated skin were ten times that observed in dry skin. numerous considerations, one of them is the search for
Hydration can be increased by occlusion with plastic the ideal skin penetration enhancer. Over the years there
films, paraffins, oils, waxes as components of ointments has been an efforts to develop a better understanding of
and water-in-oil emulsions that prevent transepidermal the nature of the stratum corneum barrier and the effect
water loss; and oil-in-water emulsions that donate water. of penetration enhancer. So with the help of this article,
Of these, occlusive films of plastic or oily vehicle have we can conclude that the barrier function of skin can be
the most profound effect on hydration and penetration overcome to an extent by the use of above discussed
rate. A commercial example of this is the use of an methods. Still there is need to make efforts to develop
occlusive dressing to enhance skin penetration of such penetration enhancers which exhibit minimum side
lignocaine and prilocane from EMLA cream in order to effects and possible synergistic effect with the drug.
provide sufficient local anaesthesia within about 1 hour
[51]
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