Nanoemulsion as potential vehicles for transdermal delivery of pure phytopharmaceuticals and poorly soluble drug
Keywords:
Transdernmal, poorly soluble drug, phytopharmaceuticals, nanoemulsionAbstract
Nanoemulsion (NE) is defined as an O/W or W/O emulsion producing a transparent product that has a droplet size from 20-200nm and does not have the tendency to coalesce. It is promising for transdermal delivery of drugs as an efficient route of drug administration. Several mechanisms have been proposed to explain the advantages of nanoemulsions for the transdermal delivery of drugs. In transdermal delivery, the goal of dosage design is to maximize the flux through the skin into systemic circulation. A useful strategy for improving percutaneous flux is to improve the concentration of drug or choose an appropriate vehicle for the transdermal delivery. The nanoemulsions system should be a promising vehicle due to powerful ability to deliver drug through skins. With these approaches, the aim of this present study is to review the potential of nanoemulsion formulation for transdermal delivery of pure phytopharmaceuticals and poorly soluble drugs. Some nanoemulsions have however exhibited sufficiently high level of stability for them to be proposed as vehicle for drug delivery. Using the transdermal route eliminates the side effects, increases patient compliance, avoids firstpass metabolism, enhance bioavailability and maintains the plasma drug level for a longer period of time.
References
Shinoda K, Kunieda H. Phase properties
of emulsions: PIT and HLB. In: Schuster
D, ed. Encyclopedia of Emulsion
Technology New York, NY: Marcel
Dekker. 1983:337Y367.
Shafiq S, Faiyaz S, Sushma T, Ahmad FJ,
Khar RK, Ali M. Design and development
of oral oil in water ramipril nanoemulsion
formulation: in vitro and in vivo
evaluation. J Biomed Nanotech.
;3:28Y44.
Shafiq S, Faiyaz S, Sushma T, Ahmad FJ,
Khar RK, Ali M. Development and
bioavailability assessment of ramipril
nanoemulsion formulation. Eur J Pharm
Biopharm. 2007;66:227Y243.
Vladimir P, Tordilin. Nanoparticulates as
Drug Carriers: Notheastern University.
Imperial Collage Press 2006.
Amselem S, and Friedman D, Submicron
emulsion in drug targeting and delivery.
Benita S. (eds) Harwood Academic:
Amsterdam 1998.
Benita S, and Levy MY. Submicron
emulsions as colloidal drug carrier for
intravenous administration-comprehensive
physicochemical characterization. J.Pharm.
Sci. 1993;82:1069-1079
Bhargava HN, Narurkar A and Lieb
LM,Using microemulsions for drug
delivery. Pharmaceut Technol.
;11:46-54.
Osborne DW, Ward AJ, Neil KJ.
Microemulsions as topical delivery
vehicles: in-vitro transdermal studies of a
model hydrophilic drug. J Pharm
Pharmacol. 1991;43:450Y454.
Faiyaz Shakeel, Sanjula Baboota, Alka
Ahuja, Javed Ali, Mohammed Aqil And
Sheikh Shafiq1. Nanoemulsions as
Vehicles for Transdermal Delivery of
Aceclofenac. AAPS Pharm Sci Tech.
;8(4):104.
Kawakami K, Yoshikawa T, Moroto Y, et
al. Microemulsion formulation for
enhanced absorption of poorly soluble
drugs, I: prescription design. J Control
Rel. 2002;81:65Y74.
Li P, Ghosh A, Wagner RF, Krill S, Joshi
YM, Serajuddin ATM. Effect of
combined use of nonionic surfactant on
formation of oil-in-water microemulsions.
Int J Pharm. 2005;288:27Y34.
Craig DQM, Barker SA, Banning D,
Booth SW. An investigation into the
mechanisms of self-emulsification using
particle size analysis and low frequency
dielectric spectroscopy. Int J Pharm.
;114:103Y110.
Lee PJ, Langer R, Shastri VP. Novel
microemulsion enhancer formulation for
Simultaneous transdermal delivery of
hydrophilic and hydrophobic drugs.
Pharm Res. 2003; 20: 264Y269.
Warisnoicharoen W, Lansley AB,
Lawrence MJ. Light scattering
investigations on dilute non-ionic oil-inwater microemulsions. AAPS Pharm Sci
Tech [serial online]. 2002;2:E12.
Kreilgaard M, Kemme MJB, Burggraaf J,
Schoemaker RC, Cohen AF. Influence
of a microemulsion vehicle on cutaneous
bioequivalence of a lipophilic model drug
assessed by microdialysis and
pharmacodynamics. Pharm Res.
;18:593Y599.
Attwood D, Currie LRJ and Elworthy PH.
Studies of Solubilized miceller
solutions. 1. Phase studies and particlesize analysis of solution formed with
non ionic surfactants. J Coll Interf Sci.
;46:249-254.
Gasco MR, Gallarate M, Pattarino F. In
vitro permeation of azelaic acid from
viscosized microemulsions. Int J Pharm.
;69:193Y196.
Benson HAE, Transdermal Drug
Delivery: Penetration Enhancement
Techniques. Current Drug Delivery.
;2:23-33.
Kriwet K, Muller-Goymann CC.
Diclofenac release fromphospholipid drug
systems and permeation through excised
human stratum corneum. Int J Pharm.
;125:231Y242.
Flynn GL. In Percutaneous absorption,
Bronaugh, R.L Maibach, HI, Eds. Marcel
Dekker Inc. New York. 1985:17-52.
Kasting GB, Smith RL, Anderson BD. In
Prodrugs: topical and ocular drug
delivery, Sloan, K., Ed. Marcel Dekker
Inc.: New York. 1992:117-161.
Potts RO, Guy RH. Pharm. Res.
;9:663-9.
Scheuplein RJ, Blank IH, Brauner GJ,
MacFarlane DJ J. Invest Dermatol. 969;
: 63-70.
Scheuplein RJ, Blank IH. Physiol. Rev.
;51:702-747.
Elias PM, McNutt NS, Friend DS. Anat.
Rec. 1977;189:577-94.
Elias PM, Friend DS J, Cell Biol.
;65:180-191.
Nemanic MK, Elias PM, J. Histochem.
Cytochem. 1980;28:573-8.
Potts R.O, Francoeur ML J. Invest
Dermatol. 1991;96:495-9.
Bodde HE, Van den Brink I, Koerten H,
De Haan FH. J.Control Rel. 1991;15:227-
Katz M, Poulsen BJ, Brodie BB, Gilette J.
In Handbook of Experimental
Pharmacology. Eds. Springer Verlag
Berlin. 1971:103-174.
Yano T, Nakagawa A, Tsuji M, Noda K.
Life Sci., 1986;39:1043-50.
Bos JD, Meinardi MM, Exp. Dermatol.,
;9:165-9.
Barry BW, Eur. J. Pharm. Sci.,
;14:101-14.
Asbill CS, El-Kattan AF, Michniak B.
Crit. Rev. Ther. Drug Carrier Syst.,
;17:621-58.
Hadgraft J. Int. J. Pharm., 1999:184:1-6.37. Walters KA, Hadgraft J. Pharmaceutical
Skin Penetration Enhancement. Drugs and
the Pharmaceutical Sciences., New York:
Marcel Dekker Inc. 1993: Vol. 59:440.
Barry BW. Int. J. Cosmet. Sci.,
;10:281-293.
Barry BW. J. Control Rel., 1991;15:237-
Williams AC, Barry BW. Pharm. Res.,
;8:17-24.
Behl CR, Flynn GL, Kurihara T, Harper
N, Smith W, Higuchi WI, Ho NF, Pierson
CL. J. Invest. Dermatol., 1980;75:346-52.
McKenzie AW, Stoughton RB. Arch.
Dermatol., 1962;86:608-610.
Francoeur ML, Golden GM, Potts RO.
Pharm. Res., 1990;7:621-7.
Yamane MA, Williams AC, Barry BW. J.
Pharm. Pharmacol., 1995;47:978-89.
Walters K.A, Walker M, Olejnik O J.
Pharm. Pharmacol. 1988;40:525-9.
Walters KA, Hadgraft J, Guy RH. In
Transdermal drug delivery. Eds. Marcel
Dekker: New York. 1988:197-246.
Wotton PK, Mollgaard B, Hadgraft J,
Hoelgaard A. Int. J. Pharm., 1985;24:19-
Harrison JE, Watkinson AC, Green DM,
Hadgraft J, Brain K. Pharm. Res.,
;13:542-6.
Waranis RP, Siver KG, Sloan KB. Int. J.
Pharm., 1987;36:211.
Yamane MA, Williams AC, Barry BW. J.
Pharm. Pharmacol., 1995;47:978-89.
Pellett M A, Roberts MS, Hadgraft J.
Int. J. Pharm., 1997;151:91-98.
Sloan KB. Sloan KB, Topical and Ocular
Drug Delivery Ed. In Prodrugs, Marcel
Dekker: New York. 1992:179-220.
Riviere JE, Heit MC. Pharm. Res.,
;14:687-97.
Banga AK, Bose S, Ghosh TK. Int. J.
Pharm., 1999;179:1-19.
Jadoul A, Bouwstra J, Preat VV. Adv.
Drug Deliv. Rev., 1999;35:89-105.
Teichmann A, Heuschkel S, Jacobi U,
Presse G, Eubert R HH, Sterry W,
Lademann J. .Comparison of stratum
corneum penetration and localization of a
lipophilic model drug applied in an o/w
microemulsion and an amphiphilic cream.
European Journal of Pharmaceutics and
Biopharmaceutics. 2007;67:699–706.
Cui J, Yu B, Zhao Y, Zhu W, Li H, Lou
H, Zhai G. Enhancement of oral
absorption of curcumin by selfmicroemulsifying drug delivery systems.
International Journal of Pharmaceutics.
;371:148–155.
Tsai Y, Lee K, Huang Y, Huang C, Wu P.
In vitro permeation and in vivo whitening
effect of topical hesperetin microemulsion
delivery system. International Journal of
Pharmaceutics. 2010;388:257–262.
Lin C, Lin H, Chen H, Yu M, Lee M.
Stability and characterisation of
phospholipid-based curcuminencapsulated Microemulsions. Food
Chemistry. 2009;116:923–928.
Wu H, Ramachandran C, Weiner N D,
Roessler B J. Topical transport of
hydrophilic compounds using water-in-oil
nanoemulsions. International Journal of
Pharmaceutics. 2001;220:63–75.
Xu J et al. The preparation of neem oil
microemulsion (Azadirachta indica) and
the comparison of acaricidal time between
neem oil microemulsion and other
formulations in vitro. Veterinary
Parasitology. 2010;169:399–403.
Mei Z, Chen H, Weng T, Yang Y, Yang
X. Solid lipid nanoparticle and
microemulsion for topical delivery of
triptolide. European Journal of
Pharmaceutics and Biopharmaceutics.
;56:189–196.
