Physical and chemical penetration enhancers in transdermal drug delivery system

Vineet Mathur, Yamini Satrawala, Mithun Singh Rajput

Abstract


There is considerable interest in the skin as a site of drug application for both local and systemic effect. However, the skin, in particular the stratum corneum, possesses a formidable barrier to drug penetration thereby limiting topical and transdermal bioavailability. Skin penetration enhancement techniques have been developed to improve bioavailability and to increase the range of drugs for which topical and transdermal delivery is a viable option. The permeation of drug through skin can be enhanced by both chemical penetration enhancement and physical methods. In this review, we have discussed the physical and chemical penetration enhancement technology for transdermal drug delivery as well as the
probable mechanisms of action.


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References


Barry BW. Dermatological formulation: percutaneous absorption. New

York: Marcel Dekker; 1983. p. 235-6.

Kanikkannan N, Kandimalla K, Lamba SS, Singh M. Structure activity

relationship of chemical penetration enhancers in transdermal drug

delivery. Curr Med Chem 1999;6:593-608.

Shah VP, Flynn GL, Yacobi A, Maibach HI, Bon C, Fleischer NM, et al.

Bioequivalence of topical dermatological dosage forms- methods

of evaluation of bioequivalence. Skin Pharmacol Appl Skin Physiol

;11:117-24.

Smith EW, Maibach HI. Percutaneous Penetration Enhancers. 2nd ed.

New York: CRS Press; 1995.

Hadgraft J. Modulation of the barrier function of the skin. Skin

Pharmacol Appl Skin Physiol 2001;14:72-81.

Henry S, McAllister DV, Allen MG, Prausnitz MR. Microfabricated

microneedles: a novel approach to transdermal drug delivery. J Pharm

Sci 1998;87:922-5.

Machet L, Boucaud A. Phonophoresis: efficiency, mechanisms and skin

tolerance. Int J Pharm 2002;1:247.

Banga AK, Prausnitz MR. Assessing the potential of skin electroporation

for the delivery of protein- and gene-based drugs. Tibtech1998;16:408-12.

Eppstein J, Smith A, Woods T, McRae M, Hatch M, Papp J, et al.

Transdermal insulin infusion via thermal micropores with the MicroPork

universal drug delivery system. CRS Poster Session 2000;3:8025.

Cevc G, Blume G. Lipid vesicles penetrate into intact skin owing to the

transdermal osmotic gradients and hydration force. Biochim Biophys

Acta 1992;1104:226-32.

Cevc G, Scha ̈tzlein A, Blume G. Transdermal drug carriers: basic

properties, optimization and transfer efficiency in the case of

epicutaneously applied peptides. J Control Release 1995;36:9-16.

Christophers E, Schubert C, Goos M. The epidermis. In: Greaves MW,

Shuster S, editors. Pharmacology of the Skin. 1st Vol. Berlin: Springer

publications; 1989. p. 330.

Fartasch M. The nature of the epidermal barrier: structural aspects.

Adv Drug Deliv Rev 1996;18:273-82.

Schurer NY, Plewig G, Elias PM. Stratum corneum lipid function.

Dermatologica 1991;183:77-94.

Scha ̈tzlein A, Cevc G. Non-uniform cellular packing of the stratum

corneum and permeability barrier function of intact skin: a high-

resolution confocal laser scanning microscopy study using highly

deformable vesicles (Transfersomes). Br J Dermatol 1998;138:583-92.

Wertz PW, Downing DT. Stratum corneum: biological and biochemical

considerations. In: Hadgraft J, Guy RH, editors. Transdermal Drug

Delivery: Developmental Issues and Research Initatives. 35th Vol. New

York: Marcel Dekker; 1989. p. 1-22.

Elias PM. Epidermal barrier function: intercellular lamellar lipid

structures, origin, composition and metabolism. J Control Release

;15:199-208.

Hadgraft J, Walters KA, Guy RH. Epidermal lipids and topical drug

delivery. Semin Dermatol 1992;11:139-44.

Sheu HM, Lee JY, Chai CY, Kuo KW. Depletion of stratum corneum

intercellular lipid lamellae and barrier function abnormalities after

long-term topical corticosteroids. Br J Dermatol 1997;136:884-90.

Charalambopoulou GC, Karamertzanis P, Kikkinides ES, Stubos AK,

Kanellopoulos NK, Papaioannou AT. A study on structural and diffusion

properties of porcine stratum corneum based on very small angle

neutron scattering data. Pharm Res 2000;17:1085-91.

Potts RO, Guy RH. Predicting skin permeability. Pharm Res 1992;9:663-9.

Moss GP, Dearden JC, Patel H, Cronin MTD. Quantitative structure-

permeability relationships (QSPRs) for percutaneous absorption. Toxicol

Vitro 2002;16:299-317.

Patel H, Berge WT, Cronin MTD. Quantitative structure – activity

relationships (QSARs) for the prediction of skin permeation of

exogenous chemicals. Chemosphere 2002;48:603-13.

Forslind B. The skin barrier: analysis of physiologically important

elements and trace elements. Acta Dermatovenereol Suppl

;208:46-52.

Schaefer P, Bewick-Sonntag C, Capri MG, Berardesca E. Physiological

changes in skin barrier function. Skin Pharmacol Appl Skin Physiol

;15:7-19.

Hsieh DS. Drug Permeation Enhancement, Theory and Applications.

New York: Marcel Dekker; 1993. p. 19.

Hadgraft J, Pugh WJ. The selection and design of topical and transdermal

agents: a review. J Invest Dermatol 1998;3:131-5.

Mitragotri S. Synergistic effect of enhancers for transdermal drug

delivery. Pharm Res 2000;17:1354-9.

Cevc G. Drug delivery across the skin. Exp Opin Invest Drugs

;6:1887-1937.

Schmook FP, Meingassner JG, Billich A. Comparison of human skin or

epidermis models with human and animal skin in in vitro percutaneous

absorption. Int J Pharm 2001;215:51-6.

Kreuter J. Colloidal Drug Delivery Systems. New York: Marcel Dekker;

p. 353.

Cevc G. Transfersomes, liposomes and other lipid suspensions on the

skin: permeation enhancement, vesicle penetration, and transdermal

drug delivery. Crit Rev Ther Drug Carrier Syst 1996;13:257-388.

Cevc G. Phospholipids Handbook. New York: Marcel Dekker; 1993.

p. 892.

Flynn GL, Bronaugh RL, Maibach HI. Percutaneous absorption. New

York: Marcel Dekker Inc; 1985. p. 17-52.

Kasting GB, Smith RL, Anderson BD. In: Prodrugs: topical and ocular

drug delivery. New York: Marcel Dekker Inc; 1992. p. 117-61.

Potts RO, Guy RH. Predicting skin permeability. Pharm Res 1992;9:663-9.

Scheuplein RJ, Blank IH, Brauner GJ, MacFarlane DJ. Percutaneous

absorption of steroids. J Invest Dermatol 1969;52:63-70.

Scheuplein RJ, Blank IH. Permeability of the skin. Physiol Rev

;51:702-47.

Higuchi WI. Analysis of data on the medicament release from ointments.

J Pharm Sci 1962;51:802-4.

Menon GK. New insights into skin structure: scratching the surface.

Adv Drug Deliv Rev 2002;54:S3-17.

Scheuplein RJ. Transient diffusion and the relative importance of various

routes of skin penetration. J Invest Dermatol 1967;48:79-88.

Anderson RL, Cassidy JM. Variation in physical dimensions and

chemical composition of human stratum corneum. J Invest Dermatol

;61:30-2.

Holbrook KA, Odland GF. Regional differences in the thickness (cell

layers) of the human stratum corneum: an ultrastructural analysis. J

Invest Dermatol 1974;62:415-22.

Wertz PW, Downing DT. In: Transdermal drug delivery: developmental

issues and research iniatives. Hadgraft J, Guy RH, editors. New York:

Marcel Dekker Inc; 1989. p. 1-22.

Elias PM, McNutt NS, Friend DS. Membrane alterations during

cornification of mammalian squamous epithelia: a freeze-fracture,

tracer. Anat Rec 1977;189:577-94.

Michaels AS, Chandrasekaran SK, Shaw JE. Drug permeation through

human skin: theory and in vitro experimemtal measurement. AIChE

;21:985-96.

Elias PM, Brown BE, Fritsch P, Goerke J, Gray GM, White RJ. Localization

and composition of lipids in neonatal mouse stratum granulosum and

stratum corneum. J Invest Dermatol 1979;73:339-48.

Bouwstra JA, Gooris GS, Vander Spek JA, Bras W. Structural investigations

of human stratum corneum by small angle X-ray scattering. J Invest

Dermatol 1991;97:1005-12.

Helmstädter A. The history of electrically assisted transdermal drug

delivery (iontophoresis). Pharmazie 2001;56:583-7.

Bang AK, Bose S, Ghosh TK. Iontophoresis and electroporation:

comparisons and contrasts. Int J Pharm 1999;179:1-19.

Weaver JC, Vaughan TE, Chizmadzhev YA. Theory of electrical creation

of aqueous pathways across skin transport barriers. Adv Drug Deliv

Rev 1999;35:21-39.

Denet AR, Vanbever R, Preat V. Skin electroporation for topical and

transdermal delivery. Adv Drug Deliv Rev 2004;56:659-74.

Wang Y, Allen LV, Li C, Tu Y. Iontophoresis of hydrocortisone across

hairless mouse skin: investigation of skin alteration. J Pharm Sci

;82:1140-4.

Turner NG, Kalia YN, Guy RH. The effect of current on skin barrier

function in vivo: recovery kinetics post iontophoresis. Pharm Res

;14:1252-5.

Banga AK. Electrically assisted transdermal and topical drug delivery.

London: Taylor and Francis; 1998.

Guy RH, Kalia YN, Delgado-Charro MB, Merino, Lopez A, Marro D.

Iontophoresis: electrorepulsion and electroosmosis. J Control Release

;64:129-32.

Subramony JA, Sharma A, Phipps JB. Microprocessor controlled

transdermal drug delivery. Int J Pharm 2006;317:1-6.

Tyle P. Iontophoretic devices for drug delivery. Pharm Res 1986;3:

-26.

Kalia YN, Naik A, Garrison J, Guy RH. Iontophoretic drug delivery. Adv

Drug Del Rev 2004;56:619-58.

Priya B, Rashmi T, Bozena M. Transdermal iontophoresis. Expert Opin

Drug Deliv 2006;3:127-38.

Bommannan DB, Tamada J, Leung L, Potts RO. In vitro Effects of

electroporation on transdermal iontophoretic delivery of luteinizing-

hormone-releasing hormone (LHRH). Pharm Res 1994;11:1809-14.

Chang SL, Hofmann GA, Zhang L, Deftos LJ, Banga AK. The effect of

electroporation on iontophoretic transdermal delivery of calcium

regulating hormones. J Control Release 2000;66:127-33.

Badkar AV, Banga AK. Electrically enhanced transdermal delivery of a

macromolecule. J Pharm Pharmacol 2002;54:907-12.

Kanikkannan N. Iontophoresis based transdermal delivery systems.

Biodrugs 2002;16:339-47.

Mitragotri S, Blankschtein D, Langer R. Transdermal delivery using low

frequency sonophoresis. Pharm Res 1996;13:411-20.

Mitragotri S. Low frequency sonophoresis. Adv Drug Deliv Rev

;56:589-601.

Mitragotri S, Blankschtein D, Langer R. Ultrasound mediated

transdermal protein delivery. Science 1995;269:850-3.

Liu H, Li S, Pan W, Wang Y, Han F, Yao H. Investigation into the potential

of low-frequency ultrasound facilitated topical delivery of Cyclosporin

A. Int J Pharm 2006;326:32-8.

Jacques SL, McAuliffe DJ, Blank IH. Parrish JA. Controlled removal of

human stratum corneum by pulsed laser to enhance percutaneous

transport. US Pat 1988;775:361.

Lee WR, Shen SC, Lai HH, Hu CH, Fang JY. Transdermal drug delivery

enhanced and controlled by erbium: YAG laser: a comparative study

of lipophilic and hydrophilic drugs. J Control Release 2001;75:155-66.

Lee WR, Shen SC, Wang KH, Hu CH, Fang JY. Lasers and microdermabrasion

enhance and control topical delivery of vitamin C. J Invest Dermatol

;121:1118-25.

Lee S, McAuliffe DJ, Flotte TJ, Kollias N, Doukas AG. Photomechanical

transcutaneous delivery of macromolecules. J Invest Dermatol

;111:925-9.

Lee S, Kollias N, McAuliffe DJ, Flotte TJ, Doukas AG. Topical drug

delivery in humans with a single photomechanical wave. Pharm Res

;16:514-8.

Doukas AG, Kollias N. Transdermal delivery with a pressure wave. Adv

Drug Deliv Rev 2004;56:559-79.

Mulholland SE, Lee S, McAuliffe DJ, Doukas AG. Cell loading with

laser generated stress waves: the role of stress gradient. Pharm Res

;16:514-8.

Lee S, McAuliffe DJ, Flotte TJ, Kollias N, Doukas AG. Permeabilization

and recovery of the stratum corneum in vivo: the synergy of

photomechanical waves and sodium lauryl sulphate. Lasers Surg Med

;29:145-50.

Lee S, McAuliffe DJ, Mulholland SE, Doukas AG. Photomechanical

transdermal delivery; the effect of laser confinement. Lasers Surg

Med 2001;28:3447.

Murthy SN. Magnetophoresis: an approach to enhance transdermal

drug diffusion. Pharmazie 1999;54:377-9.

Murthy SN, Hiremath RR. Physical and chemical permeation enhancers

in transdermal delivery of terbutaline sulphate. AAPS Pharm Sci Tech

;2:1-5.

Blank IH, Scheuplein RJ, Macfarlane DJ. Mechanism of percutaneous

absorption: III. The effect of temperature on the transport of non-

electrolytes across the skin. J Invest Dermatol 1967;49:582-9.

Clarys P, Alewaeters K, Jadoul A, Barel A, Mandas OR, Preat V. In vitro

percutaneous penetration through hairless rat skin: influence of

temperature, vehicle and penetration enhancers. Eur J Pharm Biopharm

;46:279-83.

Akomeah F, Nazir T, Martin GP, Brown MB. Effect of heat on the

percutaneous absorption and skin retention of 3 model penetrants.

Eur J Pharm Sci 2004;21:337-45.

Ogiso T, Hirota T, Masahiro I, Hino T, Tadatoshi T. Effect of temperature

on percutaneous absorption of terodiline and relationship between

penetration and fluidity of stratum corneum lipids. Int J Pharm

;176:63-72.

Klemsdal TO, Gjesdal K, Bredesen JE. Heating and cooling of the

nitroglycerin patch application area modify the plasma level of

nitroglycerin. Eur J Clin Pharmacol 1992;43:625-8.

Hull W. Heat enhanced transdermal drug delivery: a survey paper. J

Appl Res Clin Exp Ther 2002;2:1-9.

Shomaker TS, Zhang J, Ashburn MA. A pilot study assessing the impact

of heat on transdermal delivery of testosterone. J Clin Pharmacol

;41:677-82.

Ashburn MA, Ogden LL, Zhan J, Love G, Bastsa SV. Pharmacokinetics

of transdermal fentanyl delivered with and without controlled heat.

J Pain 2003;4:291-7.

Gerstel MS, Place VA. Drug delivery device. US Pat 1976:964482.

Trautman J, Cormier MJ, Kim HL, Zuck MG. Device for enhancing a

transdermal agent flux. US Pat 2000;83:196.

Trautman J, Wong PS, Daddona PE, Kim HL, Zuck MG. Device for

enhancing transdermal agent flux. US Pat 2001:322808.

Yuzhakov VV, Sherman FF, Owens GD, Gartstein V. Apparatus and

method for using an intracutaneous microneedle array. US Pat

:256533.

Giudice EL, Campbell JD. Needle-free vaccine delivery. Adv Drug Deliv

Rev 2006;58:68-89.

Muddle AG, Longridge DJ, Sweeney PA, Burkoth TL, Bellhouse BJ.

Transdermal delivery of testosterone to conscious rabbits using

powderject: a supersonic powder delivery system. Proc Int Symp

Control Release Bioact 1997;24:713.

Longbridge DJ, Sweeney PA, Burkoth TL, Bellhouse BJ. Effects of

particle size and cylinder pressure on dermal powderject delivery of

testosterone to conscious rabbits. Proc Int Symp Control Rel Bioact

;25:964.

Burkoth TL, Bellhouse BJ, Hewson G, Longridge DJ, Muddle AJ, Sarphie

DJ. Transdermal and transmucosal powdered delivery. Crit Rev Ther

Drug Carrier Syst 1999;16:331-84.

Sintov A, Krymbeck I, Daniel D, Hannan T, Sohn Z, Levin G.

Radiofrequency microchanneling as a new way for electrically

assisted transdermal delivery of hydrophilic drugs. J Control Release

;89:311-20.

Bernabei GF. Method and apparatus for skin absorption enhancement

and transdermal drug delivery. US Pat. 7083580.

Svedman P. Transdermal perfusion of fluids. US Pat 1995:441490.

Svedman P, Lundin S, Höglund P, Hammarlund C, Malmros C,

Panzar N. Passive drug diffusion via standardized skin mini-erosion;

methodological aspects and clinical findings with new device. Pharm

Res 1996;13:1354-9.

Mikszta JA, Britingham JM, Alarcon J, Pettis RJ, Dekker JP. Applicator

having abraded surface coated with substance to be applied. Patent

WO. 2001.

Mikszta JA, Britingham JM, Alarcon J, Pettis RJ, Dekker JP. Topical delivery

of vaccines. US Pat 2003;595:1.

Lee WR, Tsai RY, Fang CL, Liu CJ, Hu CH, Fang JY. Microdermabrasion

as a novel tool to enhance drug delivery via the skin: an animal study.

Dermatol Surg 2006;32:1013-22.

Barry BW. Novel mechanisms and devices to enable successful

transdermal drug delivery. Eur J Pharm Sci 2001;14:101-14.

Sage BH, Bock CR. Method and device for abrading skin. US Pat;

;199811.

Sage BH, Bock CR. Device for abrading skin. Patent EP 2003;1086719:1.

Müller RH, Benita S, Böhm B. Emulsions and nanosuspensions for the

formulation of poorly soluble drugs. Stuttgart: Medpharm; 1998. p. 152.

Santos Maia C, Mehnert W, Schaller M, Korting HC, Gysler A, Haberland

A, Schafer-Korting MJ. Drug targeting by solid lipid nanoparticles for

dermal use. Drug Target 2002;10:489-95.

Wissing SA, Muller RH. Cosmetic applications for solid lipid

nanoparticles. Int J Pharm 2003;254:65-8.

Muller RH, Radtke M, Wissing SA. Solid lipid nanoparticles (SLN) and

nanostructured lipid carriers (NLC) in cosmetic and dermatological

preparations. Adv Drug Deliv Rev 2002;54:131-55.

Wissing SA, Muller RH. Solid lipid nanoparticles as carrier for

sunscreens: in vitro release and in vivo skin penetration. J Control Rel

;81:225-33.

Jenning V, Gysler A, Schafer-Korting M, Gohla SH. Vitamin A loaded

solid lipid nanoparticles for topical use: occlusive properties and drug

targeting to the upper skin. Eur J Pharm Biopharm 2000;49:211-8.

Maia CS, Mehnert W, Schafer-Korting M. Solid lipid nanoparticles as

drug carriers for topical glucocorticoids. Int J Pharm 2000;196:165.

Dingler A, Blum RP, Niehus H, Muller RH, Gohla S. Solid lipid

nanoparticles (SLN/Lipopearls)-a pharmaceutical and cosmetic carrier

for the application of vitamin E in dermal products. J Microencapsul

;16:751-67.

Mei Z, Chen H, Weng T, Yang Y, Yang X. Solid lipid nanoparticle and

microemulsion for topical delivery of triptolide. Eur J Pharm Biopharm

;56:189-96.

Wissing SA, Muller RH. The influence of solid lipid nanoparticles on

skin hydration and viscoelasticity – in vivo study. Eur J Pharm Biopharm

;56:67-72.

Tadros TF. Future developments in cosmetic formulations. Int J Cos

Sci 1992;14:93-111.

Kreilgaard M. Influence of microemulsions on cutaneous drug delivery.

Adv Drug Deliv Rev 2002;54:77-98.

Mezei M, Gulasekharam V. Liposomes-a selective drug delivery system

for topical route of administration. Life Sci 1980;26:1473-7.

Touitou E, Junginger HE, Weiner ND, Nagai T, Mezei M. Liposomes

as carriers for topical and transdermal delivery. J Pharm Sci 1994;83:

-203.

Egbaria K, Ramachandran C, Kittayanond D, Weiner N. Topical delivery

of liposomal IFN. Antimicrob Agents Chemother 1990;34:107-10.

Birchall JC, Marichal C, Campbell L, Alwan A, Hadgraft J, Gumbleton

M. Gene expression in an intact ex-vivo skin tissue model following

percutaneous delivery of cationic liposome-plasmid DNA complexes.

Int J Pharm 2000;197:233-8.

Babiuk S, Baca-Estrada M, Babiuk LA, Ewen C, Foldvari M. Cutaneous

vaccination: the skin as an immunologically active tissue and the

challenge of antigen delivery. J Control Rel 2000;66:199-214.

Babiuk S, Baca-Estrada ME, Foldvari M, Baizer L, Stout R, Storms M,

et al. Needle-free topical electroporation improves gene expression

from plasmids administered in porcine skin. Mol Ther 2003;8:

-8.

Shahiwala A, Misra A. Studies in topical application of niosomally

entrapped nimesulide. J Pharm Sci 2002;5:220-5.

Manconi M, Sinico C, Valenti D, Loy G, Fadda AM. Niosomes as carriers

for tretinoin. I. Preparation and properties. Int J Pharm 2002;234:

-48.

Agarwal R, Katare OP, Vyas SP. Preparation and in vitro evaluation of

liposomal/niosomal delivery systems for antipsoriatic drug dithranol.

Int J Pharm 2001;228:43-52.

Namdeo A, Jain NK. Niosomal delivery of 5-fluorouracil. J Microencapsul

;16:731-40.

Vora B, Khopade AJ, Jain NK. Proniosome based transdermal delivery

of levonorgestrel for effective contraception. J Control Rel 1998;54:

-65.

Sentjurc M, Vrhovnik K, Kristl J. Liposomes as a topical delivery system:

the role of size on transport studied by the EPR imaging method. J

Control Rel 1999;59:87-97.

Cevc G. Transferosomes, liposomes and other lipid suspensions on the

skin: permeation enhancement, vesicle penetration and transdermal

drug delivery. Crit Rev Ther Drug Carrier Syst 1996;13:257-388.

Cevc G, Blume G. Biological activity and characteristics of triamcinolone-

acetonide formulated with the self-regulating drug carriers,

Transfersomes. Biochim Biophys Acta 2003;1614:156-64.

Cevc G, Blume G. New highly efficient formulation of diclofenac for the

topical, transdermal administration in ultradeformable drug carriers,

transfersomes. Biochim Biophys Acta 2001;1514:191-205.

Cevc G, Gebauer D, Stieber J, Schatzlein A, Blume G. Ultraflexible

vesicles, transfersomes, have an extremely low pore penetration

resistance and transport therapeutic amounts of insulin across the

intact mammalian skin. Biochim Biophys Acta 1998;1368:201-15.

Blume G, Cevc G, Crommelin MD, Bakker-Woudenberg IA, Kluft C,

Storm G. Specific targeting with poly (ethylene glycol)-modifeied

liposomes: coupling of homing devices to the ends of the polymeric

chains combines effective target binding with long circulation times.

Biochim Biophys Acta 1993;1149:180-4.

Biana G, Touitou E. Ethosomes: new prospects in transdermal delivery.

Crit Rev Ther Drug Carrier Syst 2003;20:63-102.

Touitou E, Godin B, Dayan N, Weiss C, Piliponsky A, Levi-Schaffer F.

Intracellular delivery mediated by an ethosomal carrier. Biomaterials

;22:3053-9.

Dayan N, Touitou E. Carriers for skin delivery of trihexyphenidyl. HCL:

ethosomes vs liposomes. Biomaterials 2000;21:1879-85.

Touitou E, Dayan N, Bergelson L, Godin B, Eliaz MJ. Ethosomes: Novel

vesicular carriers for delivery. Control Rel 2000;65:403-18.

Vyas SP, Khar RK. Introduction to parenteral drug delivery. Targeted and

controlled drug delivery. New Delhi: CBS Publishers and Distributors;

p. 3-37.

Kossovsky N, Gelman A, Rajguru S, Nguyan R, Sponsler E, Hnatyszyn CK,

et al. Control of molecular polymorphism by a structured carbohydrate/

ceramic delivery vehicle-aquasomes. J Control Release 1996;39:383-8.

Luo D, Han E, Belcheva N, Saltzman WM. A self-assembled, modular

delivery system mediated by silica nanoparticles. J Control Release

;95:333-41.

Kligman AM. Topical pharmacology and toxicology of dimethylsulfoxide.

J Am Med Assoc1965;193:796-804.

Southwell D, Barry BW. Penetration enhancers for human skin: mode

of action of 2-Pyrrolidone and dimethylformamide on partition and

diffusion of model compound water, n-alcohol and caffeine. J Invest

Dermatol 1984;82:507-15.

Barry BW, Southwell D, Woodford R. Optimization of bioavailability

of topical steroid: penetration enhancers under occulsion. J Invest

Dermatol 1984;82:49-52.

Bennett SL, Barry BW, Woodford R. Optimization of bioavailability

of topical steroid: non –occluded penetration enhancers under

thermodynamic control. J Pharm Pharmacol 1984;37:294-304.

Menczel EM. Delipidization of the cutaneous permeability barrier

and Percutaneous penetration. In: Smith EW, Maibach HI, editors.

Percutaneous penetration enhancers. Boca Raton FL: CRC Press; 1995.

p. 383-392.

Oerta RP. Protein conformational change induced in human

stratum corneum by organic sulphoxides: an infrared spectroscopic

investigation. Biopolymer 1997;16:2329-45.

Anigbog ANC, William AC, Barry BW, Edwards HGM. Fourier transform

raman spectroscopy of interaction between the penetration enhancer

dimethylsulphoxide and human stratum corneum. Int J Pharm

;125:265-82.

William AC, Barry BW. Penetration enhancer. Adv Drug Deliv 2004;56:

-18.

Hoogstrate AJ, Verhoef J, Brusee, Ijzerman AP, Spies F, Bodde HE. Kinetic,

ultrastructural aspects and molecular modeling of transdermal peptide

flux enhancement by N-alkylazocylohepton. Int J Pharm1991;76:37-47.

Park ES, Chang SJ, Rhee YS, Chis C. Effect of adhesive and permeation

enhancer on the skin permeation of captopril. Drug Deve Ind Pharma

;27:975-80.

Aungst BJ, Rogers NJ, Shefter E. Enhancement of naloxone penetration

through human skin in vitro using fatty acid, fatty alcohol, surfactant,

sulfoxide and amide. Int J Pharm 1986;33:244-7.

Aungst BJ. Structure effect studies of fatty acid isomers as skin

penetration enhancers and skin irritant. Pharm Res 1989;6:244-7.

Shin SC, Lee HJ. Controlled release of triprolidone using ethylene-vinyl

acetate membrane and matrix system. Int J Pharm 2002;54:201-06.

William AC, Barry BW. Essential oil as novel human skin penetration

enhancer. Int J Pharm 1989;57:7-9.

Cornwell PA, Barry BW. Sesquiterpene components of volatile oils as

skin penetration enhancers for the hydrophilic permeant 5-fluorouracil.

J Pharm Pharmacol 1994;46:261-9.

Morimoto H, Woda Y, Seki T, Sugibayashi K. In vitro skin permeation

of morphin hydrochloride during the finite application of

penetrationenhancing system containing water, ethanol and L-menthol.

Biol Pharm Bull 2002;25:134-6.

Jain AK, Thomas NS, Panchagnula R. Transdermal drug delivery of

imipramine hydrochloride. I. Effect of terpenes. J Control Release

;79:93-101.

EL-Kuttan AF, Asbill CS, Michniak BB. The effect of terpenes enhancer

lipophilicity on the percutaneous permeation of hydrocortisone

formulated in HPMC gel system. Int J Pharm 2000;198:179-89.

Rajadhyaksha V, Pfister WR. Oxazolidinones. Drug cosmet Ind

;1:36-47.

Seth B. Transdermal delivery using decycyloxazolidin- 2-one. Arzeim-

forsch. Drug Res 1999;42:120-22.

Asbill CS, Michniak BB. Percutaneous penetration enhancers: Local

versus transdermal activity. Research focus 2000;3:36-41.

Singh PB, Choudhury PK. Penetration enhancers for transdermal drug

delivery of systemic agents. J Pharm Res 2007;6:44-50.

Bucks D, Maibach HI. Occlusion does not uniformly enhance

penetration in vivo. In: Bronaugh RL, Maibach HI, editors. Percutaneous

Absorption; Drugs–Cosmetics–Mechanisms–Methodology. 3rd ed. New

York: Marcel Dekker; 1999.

Walkley K. Bound water in stratum corneum measured by differential

scanning calorimetry. J Invest Dermatol 1972;59:225-7.

Berner B, Mazzenga GC, Otte JH, Steffens RJ, Juang RH, Ebert CD. Ethanol:

water mutually enhanced transdermal therapeutic system: II. Skin

permeation of ethanol and nitroglycerin. J Pharm Sci 1989;78:402-07.

Friend D, Catz P, Heller J, Reid J, Baker R. Transdermal delivery of

levonorgestrel I. alkanols as permeation enhancers. J Control Release

;7:243-50.

Pershing LK, Lambert LD, Knutson K. In vivo Mechanism of ethanol-

enhanced estradiol permeation across human skin. Pharm Res

;7:170-5.

Tupker RA, Pinnagoda J, Nater JP. The transient and cumulative

effect of sodium lauryl sulphate on the epidermal barrier assessed

by transepidermal water loss: inter-individual variation. Acta Derm

Venereol 1990;70:1-5.




DOI: http://dx.doi.org/10.22377/ajp.v4i3.143

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