Self Emulsifying Drug Delivery System: A Gentle Approach for drug delivery

Authors

  • Anoop Patel Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, Meerut, U.P., India, 250001
  • Neha Sharma Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, Meerut, U.P., India, 250001
  • Anoop Kumar Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, Meerut, U.P., India, 250001

Keywords:

Self micro emulsifying drug delivery system, surfactant, oil, co-surfactant

Abstract

Oral route still remains the favorite route of drug administration in many diseases because it is very suitable for drug delivery and non invasive. Till today it attracts to many researchers for investigation in the development of new dosage forms. The major problem in oral drug formulations is low and erratic bio-availability due to less water solubility and permeability of the drug across the biological membrane. This may arise high inter and intra subject variability due to lack of dose proportionality and therapeutic failure. It is estimated that 40% of new active constituents which are investigated recently show poor water solubility due to their lipophilic nature. The improvement of bio-availability of these drugs with such properties presents one of the greatest challenges in drug formulations. Several technologies are used for overcome these problems including micronization, solid dispersions, cyclodextrins complex formation and different lipid based drug delivery systems. Selfemulsifying drug delivery system is one the most important and advanced technology for enhancing the oral bio-availability as well reducing in dose. This system also gained attraction for enabling more consistent drug absorption, selective targeting of drugs in GIT, and protection of drugs from the inner environment of gut.

References

Amidon GL. H et al., A theoretical basis

for a biopharmaceutic drug classification:

the correlation of in vitro drug product

dissolution and in vivo bioavailability.

Pharm. Res. 12

Aungst BJ. Novel formulation strategies

for improving oral bioavailability of drugs

with poor membrane permeation or

presystemic metabolism. J. Pharm. Sci.

; 82: 979-986.

Burcham DL. et al. Improved oral

bioavailability of the hypocholesterolemic

DMP 565 in dogs following oral dosing in

oil and glycol solutions, Biopharm. Drug

Dispos. 1997; 18: 737-742.

Serajuddin ATM. et al. Effect of vehicle

amphiphilicity on the dissolution and

bioavailability of a poorly water-soluble

drug from solid dispersion. J. Pharm.

Sci. 1988; 77: 414-417.

Aungst BJ, Nguyen N, Rogers NJ, Rowe

S. MH. Improved oral bioavailability of an

HIV protease inhibitor using Gelucire

/14 and Labrasol vehicles. B.T.

Gattefosse 1994;87: 49-54.

Wakerly DQM, Pouton MG, Meakin CW,

Morton BJ, FS. Self-emulsification of

vegetable oil-non-ionic surfactant

mixtures. ACS Symp. Ser. 1986; 311:

-255.

Craig, et al. An investigation into the

physico-chemical properties of selfemulsifying systems using low frequency

dielectric spectroscopy, surface tension

measurements and particle size

analysis. Int. J. Pharm. 1993; 96: 147-

Toguchi H, Ogawa Y, Iga, T. Yashiki K,

Shimamoto T. Gastrointestinal

absorption of ethyl 2 chloro-3-(4-(2-

methyl-2-phenylpropyloxy)

phenyl)propionate from different dosage

forms in rats and dogs, Chem. Pharm.

Bull. 1990; 38: 2792-2796.

Kararli TT. et al. Oral delivery of a renin

inhibitor compound using emulsion

formulations. Pharm. Res. 1992; 9: 888-

Schwendener RA, Schott H. Lipophilic 1-

beta-D-arabinofuranosyl cytosine

derivatives in liposomal formulations for

oral and parenteral antileukemic therapy

in the murine L1210 leukemia model, J.

Cancer Res. Clin. Oncol. 1996; 122:

-726.

Kreuter J, Colloidal drug delivery

systems.In: J,Kreuter editor. New York:

Marcel Dekker, 1994.

Gregoriadis G. Liposome

Technology.1993 2ndedition vol.1

Uchegbu IF, Florence AT. Non ionic

surfactant vesicles(niosomes)physical

and pharmaceutical chemistry. Adv Coll

Int Sci 1995;58:1-55

Paul BK, Moulik SP. Microemulsion: An

overview. Disp Sci . 1997; 18:301-367.

Moulik SP, Paul BK. Structure dynamics

and transport properties of

microemulsion. Adv Coll Int Sci

;78:99-199

Tenjarala S. Microemulsion: An overview

and pharmaceutical application. Crit Rev

Ther drug carrier syst 1999;16:461-521

Kantarias, Rees GD, Lawrence MJ,

Gelatin based organogels: rheology and

application in ionophoretic transdermal

drug delivery. J Contr Del. 1999; 60:355-

Watnasirichikul SS, et al. Preparation of

biodegradeble insulin nanocapsules from

biocompatible microemulsions. Pharm

Res. 2002; 17:684-689

Lawrence MJ. Surfactant Systems: Their

use in drug delivery. Chem. Soc Rev.

; 23:417-424

Cortesi R, Nastruzzi C. Liposomes,

micelles and microemulsions as a new

delivery system for cytotoxic alkaloids.

Pharm Sci and Tech Today. 1995;2:288-

Kahlweit M, Busse G, Faulhaber

B..Preparing nontoxic microemulsions

with alkyl monoglucosides and the role

of alkane diols as cosolvent

.Langmuir.1996; 12:861-862

Trotta M, Ugazio E, Gggasco

MR.Psedoternary phase diagram of

lecithin based microemusion:influence

of monoalkly phosphate. J Phar

Pharmacol. 1995; 47:451-454

Das ML,Bhattacharya PK, Moulik SP,

Model biological microemulsoion :Part1.

Phase behavior and physicochemical

properties of cholesteryl benzoate and

sodium deoxycholate contained

microemulsion Ind J Biochem Biophys

.1989; 26:24-29

Mukhopadhyay L, et al.

Thermodyanamics of formation of

biological microemulsion with cinnamic

alcohol, AOT, tween-20 and water and

kinetics of alkaline fading of crastal violet

in them. J Coll Int Sci. 1997; 186: 1-8

Acharya A, et al. Physicochemical

investigation of microemulsification of

coconut oil and water using

polyoxyethylene 2-cetyl ether(brij-52)

and isopropanol or ethanol. J Coll Int

Sci. 2002; 245:163-170

Majhi P, Moulik SP, Physicochemical

studies on biological macro and

microemulsion.vi.mixing behavior of

eucalyptus oil, water and

polyoxyethylene sorbitan monolaurate

(tween -20)assisted by n-butanol and

cinnamic alcohol. J Disp Sci Tech. 1999;

:1407-1427

Gupta S, et al. Preparation of

prospective plant oil derived

microemulsion vehicles for drug delivery.

Ind J Biochem Biophys. 2006; 43:254-

Shukla A, et al. Microemulsion for drug

delivery studied by dynamic light

scattering:effect of interparticle

intreractions in oil-in-water

microemulsion . J Pharm Sci. 2001;

:730-738

Kreilgaard M, Pederson EJ, Jarozewski

JW, NMR characterization and

transdermal drug delivery potential of

microemulsion systems. J control Rel.

; 69:421-433

Malcomson C, Lawrence MJ.

Comparison of the incorporation of

model steroids into non-ionocmicellar

and microemulsion systems. J Pharm

Pharmacol. 1993; 45:141-143

Constantinides PP. Lipid microemulsions

for improving drug dissolution and oral

absorption :physical and

biopharmaceutical aspects. Pharm Res .

; 12:1561-1572

Gupta S, et al. Designing and testing of

an effective oil-in-water microemulsion

drug delivery system for in vivo

application. Drug Del. 2005;12:267-273

Kagan A garti N, Microemulsions as

transdermal drug delivery vehicles. Adv

coll int sci. 2006:123-126:369-385

Hazra B, et al.Microemulsion

encapsulation of diospyrin a plantderived bisnapthoquinonoid of potential

chemotherapeutics activity. J Pharm

Pharmacol. 1998; 50:191-196

Von Corswant C, et al. Microemulsions

based on soyaben phosphatidylcholine

and triglycerides phase behavior and

microstructure. Langmuir. 1997;13:507-

Trotta M, Gasco MR, Morel S, .Release

of drugs from oil-water microemulsion. J

Contr Rel. 1989; 10:237-243

Von Corswant C ,Thorne P, Engstrom S.

Triglycerides based microemulsion for

intravenous administration of sparingly

soluble substances J Pharm Sci. 1998:

:200-208

Moreno MA, et al. Lyophilised lecithin

based oil-in-water microemulsion as new

and low toxic delivery system for

amphotericin B .Pharm Res. 2001;

:344-351

Charman SA, et al. Self emulsifying drug

delivery systems: formulation and

biopharmaceutical evaluation of an

investigational lipophilic compound.

Pharm Res. 1992; 9:87-93.

Constantinides PP. Lipid microemulsions

for improving drug dissolution and oral

absorption: physical and

biopharmaceutical aspects, Pharm. Res.

; 12: 1561-1572.

Craig DQM. The use of self-emulsifying

systems as a means of improving drug

delivery, B.T. Gattefosse 1993; 86; 21-

Pouton CW. SEDDS: Assessment of the

efficiency of emulsification. Int J Pharm.

; 27:335-348.

Shah NH, et al. Self-emulsifying drug

delivery systems (SEDDS) with

polyglycolyzed glycerides for improving

in vitro dissolution and oral absorption of

lipophilic drugs. Int J Pharm. 1994;

:15-23.

Patil P, Joshij, paradkar. Effect of

formulatiuon variables on preparation

and evaluation of gelled self-emulsifying

drug delivery system(SEDDS)of

ketoprofen.AAPS Pharm Sci

Tech.2004;5(3):34-42

Pouton CW, Charman WN. The potential

of oily formulations for drug delivery to

the gastro-intestinal tract. Adv Drug Deliv

Rev. 1997; 25:1-2.

Serajuddin ATM, et al. Effect of vehicle

amphiphilicity on the dissolution and

bioavailability of a poorly water-soluble

drug from solid dispersion, J. Pharm.

Sci. 1988; 77: 414-417.

Mittal pooja et al. , Potential assessment

of Transcutol P and Lauroglycol FCC as

Co-Surfactants forformulation of self

Microemulsifying Drug Delivery Systems

(Smedds), International Journal

Pharmaceutical

Sciences;2012:4(1),1742-1745

Shinde Ganesh et al: Self

Microemulsifying Drug Delivery System:

A Novel approach for Hydrophobic

Drugs, International Journal

Pharmaceutical Sciences, 2011;3(1)

Khamkar Ganesh S.Self Micro Emulsifyi

ng Drug Delivery System (Smeed) O/W

Microemulsion For Bcs Class Ii Drugs: A

approach to enhance an oral bioavailabili

ty;int. J. Pharm. Pharm. Sci,2011,3(3),1-

Rajan b mistry, nirav s sheth;a review: s

elf emulsifying drug delivery system;

Int J Pharm Pharm Sci, 2011,3(2),23- 28.

Sachan R. etal, Self-Eumlsifying Drug

Delivery System A Novel Approach for

enhancement of Bioavalibility, Int. J.

PharmTech Res.;2010,2(3):1738-1745.

Amidon, G. et.al. A theoretical basis for

a biopharmaceutic drug classification:

the correlation of in vitro drug product

dissolution and in vivo bioavailability,

Pharm.Res. 1995; 12: 413-420.

Reiss H. Entropy-induced dispersion of

bulk liquids, J. Colloids Interface Sci.

; 53:61-70.

Dabros T. et al. Emulsification through

area contraction, J. Colloids Interface

Sci.1999; 210 :222-230

Groves MJ, Mustafa RMA, Carless JE.

Phase studies of mixed phosphated

surfactantsn-hexane and water, J.

Pharm. Pharmacol. 1974; 26: 616-623.

Rang MJ, Miller CA, Spontaneous

emulsification of oils containing

hydrocarbon, non-ionic surfactant, and

oleyl alcohol, J. Colloids Interface Sci.

; 209: 179-192.

Wakerly MG, Pouton CW, Meakin BJ.

Evaluation of the selfemulsifying

performance of a non-ionic surfactantvegetable oil mixture, J. Pharm.

Pharmacol. 1987; 39: 6P.

Pouton CW, Wakerly MG, Meakin BJ.

Self-emulsifying systems for oral delivery

of drugs, Proc. Int. Symp. Control.

Release Bioact. Mater. 1987; 14: 113-

Craig DQM. et al. An investigation into

the mechanisms of self-emulsification

using particle size analysis and low

frequency dielectric spectroscopy, Int. J.

Pharm. 1995; 114: 103-110.

Pouton C.W. Self-emulsifying drug

delivery systems: assessment of the

efficiency of emulsification, Int. J. Pharm.

; 27: 335-348.

Grove M., et al. Bioavailability of

seocalcitol II: development and

characterisation of self-microemulsifying

drug delivery systems (SMEDDS) for

oral administration containing medium

and long chain triglycerides . Eur J

Pharm Sci. 2004 ; 28: 233-242.

Kimura M. et al. Relationship between

the molecular structures and

emulsification properties of edible oils,

Biosci. Biotech. Biochem. 1994;58:

-1261.

Hauss DJ. et al. Lipid-based delivery

systems for improving the bioavailability

and lymphatic transport of a poorly

water-soluble LTB4 inhibitor, J. Pharm.

Sci. 1998; 87: 164-169.

Farah N, Laforet JP,Denis J. Selfmicroemulsifying drug delivery systems

for improving dissolution of drugs: in

vitro/in vivo evaluation, Pharm. Res. ;

:1994 S202.

Yuasa H. et al Evaluation of milk

fatglobule membrane (MFGM) emulsion

for oral administration: absorption of alinolenic acid in rats and the effect of

emulsion droplet size, Biol. Pharm. Bull.

; 17:756-758.

Georgakopoulos E, Farah N, Vergnault

G. Oral anhydrous nonionic

microemulsions administrated in softgel

capsules, B.T. Gattefosse 1992; 85:11-

Swenson ES, Milisen WB, Curatolo W.

Intestinal permeability enhancement:

efficacy, acute local toxicity and

reversibility, Pharm. Res. 1994; 11:1132-

Amemiya T, Mizuno S, Yuasa H,

Watanabe J. Development of emulsion

type new vehicle for soft gelatin capsule.

I. Selection of surfactants for

development of new vehicle and its

physicochemical properties, Chem.

Pharm. Bull. 1998; 47: 309-313.

Meinzer A, Mueller E, Vonderscher J.

Microemulsion a suitable galenical

approach for the absorption

enhancement of low soluble compounds.

B.T. Gattefosse 1995; 88: 21-26.

Vonderscher J, Meinzer A. Rationale for

the development of Sandimmune Neoral.

Transplant. Proc. 1994; 26: 2925-2927.

Karim A. et al. HIV protease inhibitor SC-

: a novel method of optimizing

bioavailability profile via a microemulsion

drug delivery system, Pharm. Res. 1994;

:S368.

Uchegbu IF, Vyas SP. Non-ionic

surfactant based vesicles (niosomes) in

drug delivery, Int. J. Pharm. 1998; 172:

-70.

Shafiq S. et al. Development and

bioavailability assessment of ramipril

nanoemulsion formulation Eur. J. Pharm.

Biopharm 2007; 66: 227–243.

patil p, Vandana p, paradkar p

formulation of self-emulsifying drug

delivery system for oraldelivery of

simvastatin:In vitro and in vivo

evaluation. Acta pharma. 2007; 57: 111-

Vergote GJ, et al. An oral controlled

release matrix pellet formulation

containing nanocrystalline ketoprofen. Int

J Pharm. 2001; 219:81-87.

Yamada T, Onishi H, Machida Y.

Sustained release ketoprofen

microparticles with ethylcellulose and

carboxymethylethylcellulose. J Control

Release. 2001;75:271-282.

Roda A, et al. Bioavailability of a new

ketoprofen formulation for once-daily oral

administration. Int J Pharm.

;241:165-172.

El-Kamel AH, et al. Preparation and

evaluation of ketoprofen floating oral

delivery system. Int J Pharm.

;220:13-21.

Rhee Y-S, et al. Transdermal delivery of

ketoprofen using microemulsions. Int J

Pharm. 2001; 228:161-170.

Gao P. et al. Enhanced oral

bioavailability of a poorly water soluble

drug PNU- 91325 by supersaturable

formulations, Drug

Dev.Ind.Pharm.2004;30:221-229.

Schwarz J. Solid self-emulsifying dosage

form for improved delivery of poorly

soluble hydrophobic compounds and the

process of preparation thereof. US

patent application No. 2003 0 072 789.

Trull AK. et al. Enhanced absorption of

new oral cyclosporin microemulsion

formulation, Neoral, in liver transplant

recipients with external biliary diversion,

Transplant. Proc. 1994; 26: 2977–2978.

Mueller EA. et al. Improved dose

linearity of cyclosporine

pharmacokinetics from a microemulsion

formulation, Pharm. Res. 1994;11: 301–

Kovarik JM. et al Reduced inter- and

intraindividual variability in cyclosporine

pharmacokinetics from a microemulsion

formulation, J. Pharm. Sci 1994; 83:

–446.

Khoo SM. et al. Formulation design and

bioavailability assessment of lipidic selfemulsifying formulations of Halofantrine,

Int. J. Pharm. 1998;167: 155–164.

Julianto T, Yuen KH, Mohammad Noor

A. Improved bioavailability of vitamin E

with a self emulsifying formulation, Int. J.

Pharm. 2000; 200: 53–57.

Kommuru TR. et al. Self-emulsifying

drug delivery systems (SEDDS) of

coenzymeQ10: formulation development

and bioavailability assessment, Int. J.

Pharm. 2001;212: 233–246.

Kang B.K. et al. Development of selfmicroemulsifying drug delivery systems

(SMEDDS) for oral bioavailability

enhancement of simvastatin in beagle

dogs, Int. J. Pharm. 2004; 274: 65-73.

Kim CK, Cho YJ, Gao Z.G. preparation

and evaluation of biphenyl dimethyl

dicarboxylate microemulsions for oral

delivery, J.control.Release 2001;70: 149-

Kim J.Y, Ku Y., Enhancedabsorption of

indomethacin after oral or rectal

administration of a self-emulsifying

system containing indomethacin to rats,

Int. J. Pharm. 2000; 174: 81–89.

Tuleu C. et al. Comparative

bioavailability study in dogs of a selfemulsifying formulation of progesterone

presented in a pellet and liquid form

compared with an aqueous suspension

of progesterone, J. Pharm. Sci. 2004;

: 1495–1502.

Yap SP, Yuen KH. Influence of lipolysis

and droplet size on tocotrienol

absorption from self-emulsifying

formulations, Int. J. Pharm. 2004; 281:

–78.

Porter CJH. et al. Susceptibility to lipasemediated digestion reduces the oral

bioavailability of danazol after

administration as a medium chain lipidbased microemulsion formulation,Pharm.

Res. 2004;21: 1405–1412.

Wei L. et al. Preparation and evaluation

of SEDDS and SMEDDS containing

carvedilol,Drug Dev. Ind. Pharm.

;31: 785–794.

Iwanaga K. et al. Disposition of

lipidbased formulation in the intestinal

tract affects the absorption of poorly

water-soluble drugs, Biol. Pharm. Bull.

; 29: 508–512.

Wu W, Wang Y, Que L. Enhanced

bioavailability of silymarin by

selfmicroemulsifying drug delivery

system, Eur. J. Pharm. Biopharm. 2006;

: 288–294.

Shen H, Zhong M. Preparation and

evaluation of self-microemulsifying drug

delivery systems (SMEDDS) containing

atorvastatin, J. Pharm. Pharmacol. 2006;

: 1183–1191.

Hong J.-Y. et al. A new selfemulsifying

formulation of itroconazole with improved

dissolution and oral absorption, J.

Control. Release. 2006;110:332–338

Sek L. et al. Examination of the impact

of a range of Pluronic surfactants on the

in vitro solubilisation behaviour and oral

bioavailability of lipidic formulations of

atovaquone, J. Pharm. Pharmacol. 2006;

: 809–820.

Grove M. et al. Bioavailability of

seocalcitol II: development and

characterisation of self-microemulsifying

drug delivery systems (SMEDDS) for

oral administration containing medium

and long chain triglycerides, Eur J.

Pharm. Sci .2006;28: 233–242.

Araya H.et al. The novel formulation

design of self-emulsifying drug delivery

systems (SEDDS) type o/w

microemulsion I: enhancing effects on

oral bioavailability of poorly water soluble

compounds in rats and beagle dogs,

Drug Metab. Pharmacokinet. 2005; 20:

–256.

Downloads

Published

2012-09-30

How to Cite

Anoop Patel, Neha Sharma, & Anoop Kumar. (2012). Self Emulsifying Drug Delivery System: A Gentle Approach for drug delivery. International Journal of Drug Delivery, 4(3), 297–309. Retrieved from https://ijdd.arjournals.org/index.php/ijdd/article/view/152

Issue

Section

Review Article