Enhancement of skin permeation and anti- inflammatory effect of indomethacin using microemulsion
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Abstract
and enhancement ratio (Er) was observed in microemulsion formulations compared with the conventional IND gel.The anti-inflammatory effects of microemulsion formulations showed a significant increase in percent edema inhibition value after 4 hours. The optimized formulation showed a significant increase in the steady-state flux (Jss) and permeability coefficient
(Kp). The enhancement ratio (Er) was found to be 8.939 in optimized formulation F1 compared with IND gel.
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References
Kreilgaard M. Influence of microemulsions on cutaneous drug delivery.
Adv Drug Deliv Rev 2002;54 Suppl 1:S77-98.
Tenjarla S. Microemulsions: an overview and pharmaceutical
applications. Crit Rev Ther Drug Carrier Syst 1999;16:461-521.
Gasco MR. Microemulsions in the Pharmaceutical Field. Perspectives
and Applications, Industrial Applications of Microemulsions. New York:
Marcel Dekker Inc; 1997. p. 97-122.
Lawrence MJ, Rees GD. Microemulsion-based media as novel drug
delivery systems. Adv Drug Deliv Rev 2000;45:89-121.
Sintov AC, Shapiro L. New microemulsion vehicle facilitates
percutaneous penetration in vitro and cutaneous drug bioavailability
in vivo. J Controll Release 2004;95:173-83.
Gasco MR, Gallarate M, Trotta M, Bauchiero L, Gremmo E, Chiappero
O. Microemulsions as topical delivery vehicles: ocular administration
of timolol. J Pharm Biochem Anal 1989;7:433-9.
Zhu W, Yu A, Wang W, Dong R, Wu J, Zhai G. Formulation design
of microemulsion for dermal delivery of penciclovir. Int J Pharm
;360:184-90.
Kuminek G, Kratz JM, Ribeiro R, Kelmann RG, de Araújo BV, Teixeira
HF, et al. Pharmacokinetic study of a carbamazepine microemulsion in
beagle dogs. Int J Pharm 2009;378:146-8.
Djordjevic L, Primorac M, Stupar M, Krajisnik D. Characterization of
caprylocaproyl macrogolglycerides based microemulsion drug delivery
vehicles for an amphiphilic drug. Int J Pharm 2004;271:11-9.
Lee J, Lee Y, Kim J, Yoon M, Choi YW. Formulation of microemulsion
systems for transdermal delivery of aceclofenac. Arch Pharm Res
;28:1097-102.
Madhusudhan B, Rambhau D, Apte SS, Gopinath D. 1-O-alkylglycerol
stabilized carbamazepine intravenous o/w microemulsions for drug
targeting in mice. J Drug Target 2007;15:154-61.
Cevc G, Vierl U. Nanotechnology and the transdermal route: A state of
the art review and critical appraisal. J Controll Release 2010;141:277-99.
Monteiro-Riviere NA, Inman AO, Riviere JE, McNeill SC, Francoeur ML.
Topical penetration of piroxicam is dependent on the distribution of
the local cutaneous vasculature. Pharm Res 1993;10:1326-31.
Singh P. Roberts MS. Skin permeability and local tissue concentrations
of nonsteroidal anti-inflammatory drugs after topical application. J
Pharmacol Exp Ther 1994;268:144-51.
El Maghraby GM. Transdermal delivery of hydrocortisone from
eucalyptus oil microemulsion: effects of cosurfactants. Int J Pharm
;355:285-92.
Shakeel F, Baboota S, Ahuja A, Ali J, Aqil M, Shafiq S. Microemulsions
as vehicles fro transdermal delivery of aceclofenac. AAPS Pharmscitech
;8:104 Available from: [http://www.aapspharmscitech.org]. [Last
accessed on 2011 Aug 26].
Nandi I, Bari M, Joshi H. Study of Isopropyl Myristate Microemulsion
Systems Containing Cyclo-dextrins to improve the Solubility of 2
Model Hydrophobic Drugs. AAPS Pharmscitech 2003;4:10. Avalable
from: http://www.pharmscitech.org. [Last accessed on 2011 Aug 26].
Burapapadh K, Kumpugdee-Vollrath M, Chantasart D, Sriamornsak P.
Fabrication of pectin-based microemulsions loaded with itraconazole
for pharmaceutical application. Carbohydr Polym 2010;82:384-93.
Peltola S, Saarinen-Savolanien P, Kiesvaara J, Suhonen TM, Urtti A.
Microemulsion for topical delivery of estradiol. Int J Pharm 2003;
:99-107.
Rhee YS, Choi JG, Park ES, Chi SC. Transdermal delivery of ketoprofen
using microemulsions. Int J Pharm 2001;228:161-70.
Delgado-Charro MB, Iglesias-Vilas G, Blanco-MÄ•ndez J, LÅpez-Quintela
MA, Marty JP, Guy RH. Delivery of a hydrophilic solute through the
skin from novel microemulsion systems. Eur J Pharm biopharm
;43:37-42.
Baroli B, López-Quintela MA, Delgado-Charro MB, Fadda AM, Blanco-
Méndez J. Microemulsions for topical delivery of 8-methoxsalen. J
Controll Release 2000;69:209-18.
Zhao X, Liu JP, Zhang X, Li Y. Enhancement of transdermal delivery
of theophylline using microemulsion vehicle. Int J Pharm 2006;
:58-64.
Walters KA. Penetration enhancers and their use in transdermal
therapeutic systems. In: Hadgraft J, Guy RH, editors. Transdermal Drug
Delivery, Developmental Issues and Research Initiatives. New York, NY:
Marcel Dekker; 1989. p. 246.
Tadros TF. Future developments in cosmetic formulations. Int J Cosmet
Sci 1992;14:93-111.
Pattarino F, Marengo E, Gasco MR. Experimental design and partial
least squares in the study of complex mixtures: microemulsions as
drug carriers. Int J Pharm 1993;91:157-65.
Ghosh PK, Majithiya RJ, Umrethia, ML, Murthy RSR. Design and
development of microemulsion drug delivery system of acyclovir for
improvement of oral bioavailability. AAPS Pharmscitech 2006;7:77.
Available from: http://www.aapspharmscitech.org. [Last accessed on
Aug 26].
Gannu R, Palem CR, Yamsani VV, Yamsani SK, Yamsani MR. Enhanced
bioavailability of lacidipine via microemulsion based transdermal gels:
Formulation optimization, ex vivo and in vivo characterization. Int J
Pharm 2010;388:231-41.
Celesti L, Murratzu C, Valoti M, Sgaragli P, Corti P. The single-pass
perfused rabbit ear as a model for studying percutaneous absorption
of clonazepam. I. General characteristics. Methods Find Exp Clin
Pharmacol 1992;14:701-9.
Yuan Y, Li SM, Mo FK, Zhong DF. Investigation of microemulsion system
for transdermal delivery of meloxicam. Int J Pharm 2006;321:117-23.
Touitou E, Dayan N, Bergelson L, Godin B, Eliaz M. Ethosomes—novel
vesicular carriers for enhanced delivery: characterization and skin
penetration properties. J Control Release 2000;65:403-18.
Al-Swayeh PK, Clifford RH, Del Soldato P, Moore PK. A comparison of
the anti-inflammatory and antinociceptive activity of nitroaspirin and
aspirin. Br J Pharmacol 1999;129:343-50.
Winter CA. Anti-inflammatory testing methods: comparative evaluation
of indomethacin and other agents. Int Symp Nonst Antiinflamm Drugs
;82:190-202.
Shafiq S, Shakeel F, Talegaonkar S, Ahmad FJ, Khar RK, Ali M.
Development and bioavailability assessment of ramipril microemulsion
formulation. Eur J Pharm Biopharm 2007;66:227-43.
Kreilgaard M, Pedersen EJ, Jaroszewski JW. NMR characterization and
transdermal drug delivery potential of microemulsion systems. J Control
Release 2000;69:421-33.
TomÅ¡iÄ M, Podlogar F, GaÅ¡perlin M, BeÅ¡ter-RogaÄ M, Jamnik A. Water–
Tween 40®/Imwitor 308®–isopropyl myristate microemulsion as delivery
systems for ketoprofen: small-angle X-ray scattering study. Int J Pharm
;327:170-7.
Changez M, Varshney M, Chander J, Dinda AK. Effect of the composition
of lecithin/n-propanol/isopropyl myristate/water microemulsions on
barrier properties of mice skin for transdermal permeation of tetracaine
hydrochloride: in vitro. Colloids Surf B Biointerfaces 2006;50:18-25.
Lee PJ, Langer R, Shastri VP. Novel microemulsion enhancer formulation
for simultaneous transdermal delivery of hydrophilic and hydrophobic
drugs. Pharm Res 2003;20:264-9.
Takahashi K, Tamagawa S, Katagi T, Yoshitomi H, Kamada A, Rytting
JH, et al. In vitro transport of sodium diclofenac across rat abdominal
skin: effect of selection of oleaginous component and the addition
of alcohols to the vehicle. Chem Pharm Bull (Tokyo) 1991;39:154-8.
Hua L, Weisan P, Jiayu L, Ying Z. Preparation, evaluation, and NMR
characterization of vinpocetine microemulsion for transdermal delivery.
Drug Dev Ind Pharm 2004;30:657-66.
Li H, PanWS, Wu Z, Li JY, Xia LX. [Optimization of microemulsion
containing vinpocetine and its physicochemical properties]. Yao Xue
Xue Bao 2004;39:681-5.
Barthélémy P, Farah N, Laforet JP. Transcutol-product profile. Product
Information. Gattefossé. Lyon, France†1995. p. 1-10.
Craig DQ, Barker SA, Banning D, Booth SW. An investigation into the
mechanism of self-emulsification using particle size analysis and low
frequency dielectric spectroscopy. Int J Pharm 1995;114:103-10.
Huang YB, Wu PC, Ko HM, Tsai YH. Cardamon oil as a skin permeation
enhancer for indomethacin, piroxicam and diclofenac. Int J Pharm
;126:11-117.
Gasco MR, Gallarate M, Pattarino F. In vitro permeation of azelaic acid
from viscosized microemulsion. Int J Pharm 1991;69:193-6.
Mei ZN, 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.
Chang XL, Chen HB, Zhao XZ, Gao ZH, Xu HB, Yang XL. High
performance liquid chromatography determination of triptolide in vitro
permeation studies. Anal Chim Acta 2005;534:215-21.
Changez M, Chander J, Dinda AK. Transdermal permeation of tetracaine
hydrochloride by lecithin microemulsion: in vivo. Colloids Surf B
Biointerfaces 2006;48:58-66.
Chen H, Chang X, Du D, Li J, Xu H, Yang X. Microemulsion-based hydrogel
formulation of ibuprofen for topical delivery. Int J Pharm 2006;315:52-8.
Barry BW. Mode of action of penetration enhancers in human skin. J
Control Release 1987;6:85-97.
Artusi M, Nicoli S, Colombo P, Bettini R, Sacchi A, Santi P. Effect of
chemical enhancers and iontophoresis on thiocolchicoside permeation
across rabbit and human skin in vitro. J Pharm Sci 2004;93:2431-8.
Winter CA, Risley EA, Nuss GW. Carrageenin-induced edema in hind
paw of the rat as an assay for antiiflammatory drugs. Proc Soc Exp Biol
Med 1962;111:544-7.
Shakeel F, Ramadan W, Ahmed MA. Investigation of true microemulsions
for transdermal potential of indomethacin: characterization rheological
characteristics and ex vivo skin permeation studies. J Drug Target
;17:435-41.