LIQUE SOLID COMPACT DRUG DELIVERY SYSTEM: A REVIEW

www.wjpps.com Vol 8, Issue 10, 2019.

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Mayuri et al. World Journal of Pharmacy and Pharmaceutical Sciences

LIQUE SOLID COMPACT DRUG DELIVERY SYSTEM: A REVIEW

*Mayuri Tapkir, Arun Mahajan, and Devika Lomate

*M Pharm, Department of Pharmaceutics, der ege of Pharmacy, Nigdi, Pune.

ABSTRACT

Drugs which are orally administered possess the solubility is one of the

major problem, because of the drugs with the low aq. solubility, such

drugs get slowly dissolve and leads to low bioavailability. So, it is the

biggest provocation in front of the scientists to improve the solubility

of such drugs. Nearly about 40-50% of the drugs shows this problem.

SEDDS is novel approach for improving the solubility of the lipophilic

drug. The special feature of this delivery system is its ability to self-

emulsify, that is their propensity to form oil-in-water emulsion on

gentle agitation when diluted with aq. phase present outside the

gastrointestinal tract. SEDDS possess low cost including easily

available excipients such as natural oils or synthetic oil, surfactant, co-surfactant/ co-solvent.

The major advantage of SEDDS is that it avoid the first pass effect and get absorbed by the

lymphatic pathways. In this review we present a report on the formulation characterization,

different dosage forms and application of SEDDS with examples of currently available

marketed preparations.

KEYWORDS: Self emulsifying drug delivery, Bioavailability and Solubility enhancement.

INTRODUCTION[1]

Due to low aq. Solubility of drug, low oral bioavailability is seen and it is a major concern for

formulation scientists. So, It is major part of study for the pharmaceutical scientists to convert

those molecules into such a formulation that will show the desired bioavailability after oral

administration. There are various strategies used in formulation development that can be use

to improve the bioavailability of poorly soluble drug, it can be done by increasing the

dissolution rate or by keeping the drug in solution and maintaining the drug in solution in

intestinal lumen. SEDDS is an isotropic mixture of oil, surfactant, solvents, co-solvents/

WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES

SJIF Impact Factor 7.632

Volume 8, Issue 10, 329-345 Review Article ISSN 2278 – 4357

Article Received on

03 August 2019,

Revised on 23 August 2019,

Accepted on 13 Sept. 2019,

DOI: 10.20959/wjpps201910-14728

*Corresponding Author

Mayuri Tapkir

M Pharm, Department of

Pharmaceutics,

der ege f

Pharmacy, Nigdi, Pune.


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surfactants it can be used for the design of formulation in order to improve the oral absorption

of highly lipophilic drug.

Advantages of SEDDS[2,12,19]

1. Quick Onset of Action.

2. Reduction in the Drug Dose.

3. Ease of Manufacture and Scale up.

4. Improvement in oral bioavailability.

5. No influence of lipid digestion process.

6. Increased Drug loading capacity.

7. Best suited for poorly water soluble drug because it increases solubility.

8. Protect the drug from GIT environment.

9. Food affects drug action by causing variability. SEDDS reduce the variability of the drug

action.

10. Hydrophilic or hydrophobic medicines can be effectively incorporated inside the oil-

surfactant mixture.

Disadvantages of SEDDS[3]

1. The higher concentration of the surfactants use in theself emulsifying drug delivery

system ranges between 30% to 60% irritates the GIT.

2. In-vitro models of self –emulsifying formulations lack good predicative studies on

assessment of the formulation.

3. Co-solvent which are volatile in nature can migrate on the soft or hard gelatin capsule

shell leading to the precipitation of the lipophilic drugs.

4. Some chemical instabilities are observed in the self- emulsifying drug delivery system.

Mechanism of SEDDS[4,16,14,18]

The process by which the self-emulsification takes place is as such not yet well understood.

But, according to Reiss, Self-emulsification occurs when the entropy change that favours

dispersion is greater than the energy required to increase the surface area of the dispersion. In

addition the free energy of a standard emulsion formation may be a direct function of the

energy needed to make a brand new surface between the two phases and can be described by

the equation.

∆G = ∑N∏r²σ


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Where, ∆G = Free energy associated with the process, N= No. of droplets,

r = radius, σ = i terfacia e ergy

As we know that emulsion consists of the two different phases which tend to separate with

time to reduce the interfacial area and subsequently the emulsion is stabilized by emulsifying

agent, which form a monolayer of emulsion droplets and hence reduces the interfacial energy

as well as providing a barrier to prevent coalescence. For Better understanding the below

figure shows the simpler mechanism of formulation. When we administered the SEDDS by

oral route, the oil which is present in the SEDDS stimulates the bile secretion and there by the

drug incorporated into the oil droplet further emulsify with bile salt and when it comes in

contact with aq. fluid in GIT it spontaneously forms the emulsion. The lipid droplet which

contain drug get metabolized by enzyme lipase which is further hydrolysed into mono, di-

glycerides and fatty acids and get absorbed into the Lymphaticsystem.

Fig No.1: Mechanisms of Self Emulsifying Drug Delivery System.

Fig No.2: Mechanisms of Self Emulsifying Drug Delivery System.


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Fig No.3: Classification of Self Emulsifying Drug Delivery System.

Type I Lipid Formulation[1, 8]

In Type I lipid formulation, the excipients use are oils without surfactants i.e. tri, di and

mono-glycerides and the emulsion is stabilized by the low concentration of emulsifiers such

as 1% (w/v) Polysorbate 60 and 1.2% (w/v) Lecithin. It is a straightforward formulation for

potent medication. It is non-dispersing and requires digestion. Formulation has poor solvent

capability unless drug is extremely lipophilic.

Type II system/ Non-water soluble element system[1,8]

These systems are isotropic mixtures of lipids and lipotropic surfactants having HLB worth

but twelve that selfemulsify to make fine oil in water emulsion in binary compound

medium.Self emulsification is mostly obtained at a surfactant level above 25%w/w.But at a

surfactant level of 50-60% w/w the emulsification process may be leads to formation of

viscous liquid crystalline gels at the oil/water interface. This system is also known as Type-II

SEDDS according to lipid formulation classification system.

Type III system / Water soluble component system[1,8]

These are commonly referred to as Self-micro emulsifying drug delivery system. These

systems are formulated by using hydrophilic surfactants with HLB more than 12 and Co-

solvents such as Ethanol, Propylene glycol and Polyethylene glycols. Type III formulations

can be further divided into the Type IIIA and Type IIIB formulations in order to identify

more hydrophilic systems where the content of hydrophilic surfactants and co-solvents

increases and the lipid content reduces. This system forms the clear or almost clear dispersion


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drug absorption without digestion. Possible loss of solvent capacity on dispersion easily

digested.

Type IV system[1,8]

Type IV formulations do not contain natural lipids and represents the most hydrophilic

formulations. These formulations offer increased drug payloads (due to higher drug solubility

in surfactant and co-solvents). An example of a Type IV formulation is that the current

capsule formulation of the HIV antiviral amprenavir (Agenerase) which contains TPGS as a

surfactant and PEG 400 and propylene glycol as co-solvents.

Composition of SEDDS[5]

1. Drug or Active Pharmaceutical Ingredients 2.Natural or Synthetic oils

3. Solid or liquid surfactants 4. Co-solvent / Co-surfactants

Oils

Oil is the most important excipient in the SEDDS and it facilitate the formation of self-

emulsification. Oil helps in solubilizing the lipophilic drugs. Natural or synthetic oils can be

used in self-emulsifying drug delivery system. Oils increase the fragments of lipophilic drugs

that pass through the intestinal lymphatic system; this increases the absorption from

gastrointestinal tract depending on the nature of triglyceride. Different degrees of low chain

triglycerides (LCT) and medium chain triglyceride (MCT), monoglycerides, diglycerides

have been used in the formulation of SEDDS.

Types of oils used in marketed SEDDS: According to Bhupendra G. Prajapati.

Type of oil Marketed product Drugs

Corn oil Depakene capsule Valproic acid

Olive oil Sandimmune solution Cyclosporine

Soyabean oil Accutane soft gelatin capsule Isotretinoin

Peanut oil Prometrium soft gelatin capsule Progesterone

Bees wax Vesanoid soft gelatin capsule Tretinoin

Surfactants

There are various surfactants are available which are having the properties of self

emulsification, but the choice is limited as very few surfactants are orally acceptable. In the

formulation of SEDDS, Non-ionic surfactants are widely use because they are having the

higher value of hydrophilic and lipophilic balance. Non-ionic surfactants are preferred than

the cationic and anionic surfactants because they are not harmful.


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The concentration of surfactants use in formulation of SEDDS are 30%-60%. The higher

concentration of the surfactants lead to the irritation of the gastrointestinal tract and this is the

drawback of SEDDS. In study it has been observe that the in some cases as the concentration

of surfactant increases the droplet size also increases and in other case due to increase in

concentration of surfactant decrease in droplet size is seen.

Example: In case of Self emulsifying system containing Labrafac CM-10 and Captex-200

increasing the surfactant concentration (from 30-60%) decrease in the mean droplet size. A

smaller/minimal droplet size was observed when the surfactant concentration was in the

range of 60-80%.In case of the system containing Captex-200 and Labrasol as the

concentration of surfactants increases the droplet size also increases.

List of surfactants

Liquid stateSurfactant HLB<10 Semisolid state Surfactant HLB <10

Span 80 Imwitor 988

Span 20 Imwitor 742

Neobee M-20 Gelucire 43/01

Crill 4 Surfactant HLB >10

Miglyol 840 Chremophore RH 40

Surfactant HLB >10 Brij 96

Polysorbate 80 Myrj 45

Polysorbate 20 Vitamine E TPGS

Example of marketed preparation

Excipient name

( commercial name)

Examples of commercial

products in which it has been used

Polysorbate 20 (Tween 20) Targretin soft gelatin capsule

Polysorbate 80 (Tween 80) Gengraf hard gelatin capsule

Sorbitanmonooleate (Span80) Gengraf hard gelatin capsule

Polyoxyl-35-castor oil

(Cremophor EL)

Gengraf hard gelatin capsule,

Ritonavir soft gelatin capsule

Polyoxyethylated glycerides

(Labrafil M 2125Cs) Sandimmune soft gelatincapsules

D-α-Tocopheryl polyethylene

glycol 1000 succinate (TPGS)

Agenerase soft gelatin capsule,Agenerase

oral solution

Co-solvent/ Co-surfactants

Co-solvents are the solvents that help in dissolving immiscible phases (oil/aqueous) in a

formulation. They dissolve in either large amounts of hydrophilic surfactants or the

hydrophobic drug in oil phase.


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One or more hydrophilic solvents may be used. Co-solvents can also be referred as co-

surfactants depending on their use in a formulation.

As we know that high concentration of surfactants is required in SEDDS usually above 30%

which causes irritation in the gastrointestinal tract, co-surfactants are employed to reduce the

conc. of surfactants. Drug release is increase with increase in the concentration of the co-

surfactants.

When a co-surfactant is added (in addition to surfactant) to the system, it lowers the

interfacial tension, fluidizes the hydrocarbon region of the interfacial film and decreases the

bending stress of the interface.

Example: Myvacet 9-45, Labrafac CM-10 and lauroglycol decrease in mean emulsion

droplet diameter was observed with increase in co-surfactant concentration. In case of

Labrasol, Captex 200 and lauroglycol increase in mean emulsion droplet diameter with

increase in the concentration.

Example

Excipient name

(commercial name)

Examples of commercial products in which it has

been used

Ethanol Neoral soft gelatin capsule, Neoral oral solution, Gengraf

hard gelatin capsule, Sandimmune soft gelatin capsule.

Glycerin Neoral soft gelatin capsule, Sandimmune soft gelatin

capsule

Propylene glycol Neoral soft gelatin capsule, Neoral oral solution,

Lamprene soft gelatin capsule.

Polyethylene glycol Targretin soft gelatin capsule, Gengraf hard gelatin

capsule, Agenerase soft gelatin capsule

Selection of excipients[6,17,21]

Selection of oil phase and Selection of oil is based on the solubility of the drug. A known

amount of excess drug was added to 2 mL of each of the selected vehicle.It was mixed in

Cyclon mixer and kept at 25°C for 48 hrs. After reaching equilibrium, each vial was

centrifuged at 5000 rpm for 10 mins. Excess insoluble drug was separated by filtration using

Whatman filter paper Solubilized drug concentration was quantified by UV Spectroscopy and

insoluble drug was weighed to check the mass balance.


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Selection of surfactant and co-surfactant[6,20,]

Surfactant

The criteria for the selection of surfactant are its HLB value, drug solubility and non-toxic

nature.

Co-surfactant

Co-surfactants were selected based on their ability to form stable and clear micro-emulsion at

a minimum concentration.

Factors affecting SEDDS [10, 15, 18, 22, 25]

Nature and dose of the drug

Drugs which are to be use for the SEDDS need to be soluble in at least one of the component

of the SEDDS, especially the drugs which are use in a higher dose. Unless and until they are

not soluble in SEDDS component they are not giving the bioavailability. The drugs with the

less aqueous solubility and lipid solubility exhibit limited solubility with log p values having

an estimate of 2 are more difficult to deliver by the SEDDS.The solubility of the drug in the

oil phase determines the ability of SEDDS to keep the drug in solubilized form. The dose of

the drug should not exceed than 900 mg The concentration of surfactant or co-surfactant.

Precipitation may occur if the surfactant or co-surfactant contributes greatly to the

solubilization of drug as this leads to a low capacity of surfactant or co-surfactant to act as

solvent due to the dilution of SEDDS.

The polarity of emulsion

The polarity of the emulsion depends on the polarity of the lipophilic phase and this controls

the release of drug from the emulsion.

The temperature at which self-emulsification occur

Characterization of SEDDS[13, 14]

Droplet size

The droplet size analysis shows the quality of emulsion formed. Formulation (25µl) was

diluted with water to 25 ml in volumetric flask and gently mixed by inverting the flask. The

droplet size distribution of the resultant emulsion were determined using Malvern particle

size analyser (Model no.2600, 63mm lens Malvern UK). The values of mean emulsion

droplet diameter were compared.


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Zeta potential

Zeta potential is generally measured by the zeta potential analyser or zeta meter system.

Value of zeta potential indicates the stability of the emulsion after appropriate dilution.

Higher zeta potential indicates the good stability of the formulation. Usually the value of zeta

potential is negative due to presence of free fatty acid, but when cationic lipid such as

oleylamine is use and positive charge is develops. The droplets of positive charge have the

property of interacting efficiently with the mucosal surface of the GIT, and these interactions

are of electrostatic nature due to which strong adhesion can be expected with increased

absorbance.

Size analysis

The droplet size is mainly dependent on the nature and concentration of surfactant.

Spectroscopic techniques such as photon correlation spectroscopy and microscopic technique

are used for droplet size analysis.

Percent transmittance

This test gives the indication of transparency of diluted formulation. It is determine

spectrophotometrically after dilution of the formulation with water, keeping water as a blank.

In case of the micro-emulsion percent transmittance value near to 100% indicates clear and

transparent micro-emulsion formed.

Self-Emulsification Time

The self-emulsification time is determined by using USP dissolution apparatus 2 at 50rpm,

where 0.5 g of SEDDS formulation is introduced into 250ml of 0.1N HCL or 0.5% SLS

(Sodium Lauryl Sulphate) solution. The time for emulsification at room temperature is

indicated as self-emulsification time for the formulation.

Ternary Phase Diagram

This is the primary step before begining the formulation. It is helpful to spot best

emulsification region of oil, chemical agent and co-surfactant combos. Ternary section

diagram of chemical agent, co-surfactant associate degreed oil can plot; every of them

representing an apex of the Triangulum. The strategies are wont to plot ternary section

diagrams are specifically Dilution technique and Water volumetric analysis technique.


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Dilution method: Ternary mixtures with varying compositions of surfactant, co-surfactants

and oil were prepared. The percentage of chemical agent, co-surfactant and oil decided on the

basis of the requirements. Compositions are evaluated for nanoemulsion formation by

diluting applicable quantity of mixtures with applicable double water. Globule size of the

ensuing dispersions decided by victimisation spectroscopic analysis. The area of

nanoemulsion formation in ternary phase diagrams was identified for the respective system in

which nanoemulsion with desire globule size were obtain.

Water Titration method: The pseudoternary phase diagram is used to map the three key

excipients according to the resulting droplet size following self-emulsification, stability upon

dilution and viscosity. Surfactant mixed with co-surfactant in fixed weight ratios (1.1, 2.1,

3.1, 4.1,) then this mixture mixed with oil at room temperature (25°c). In phase diagram, the

ratio of oil to Smix was varied as 1.9, 2.8, 3.7, 4.6, 5.5, 6.4, 7.3, 8.2, and 9.1 (w/w). A small

amount of water is added into the vials under vigorous stirring by using magnetic stirrer.

Following each water addition the mixture in vials is centrifuged for 2 to 3 minute and is

incubated at 25°c for 48 hrs with gentle shaking. Each mixture was visually observed for

clarity and flowability. Then the data was plotted using Microsoft Excel and phase diagram

was obtained. After the identification of microemulsion region in the phase diagram, the

microemulsionformation were selected at desired component ratios.

Fig No.4: Ternary Phase Diagrams A and B.

Dosage forms of SEDDS[16,17]

Oral delivery Self emulsifying capsule

Poor water soluble drugs can be dissolved in SEDDS and encapsulated in hard or soft gelatin

capsules to produce convenient single unit dosage forms. Administration of capsules


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containing conventional liquid SE formulations, micro emulsion droplets form and

subsequently disperse in the GI tract to reach sites of absorption.

If irreversible phase separation of micro-emulsion occur’s an improvement of drugs

abs rpti ca ’t be expected. For handling this problem, sodium dodecyl sulfate was added

into the SE formulation.

Self-emulsifying sustained / controlled release tablets

Combination of lipids and surfactant has presented great potential preparing SE tablets. SE

tablets area unit of nice utility in preventing adverse result. Inclusion of indomethacin (or

other hydrophobic NSAID) for example, into SE tablets may increase its penetrationefficacy

through GI mucosal membrane, potentially reducingGI bleeding.

Self-emulsifying sustained /controlled release pellets

Pellets, as a multiple unit dosage form posse’s many advantages over conventional solid

dosage forms. Such as, Flexibility of manufacture, reducing intra subject and inter subject

variability of plasma profile and minimizing GI irritation without lowering drug

bioavailability.

Self-emulsifying solid dispersions

Solid dispersions may increase the dissolution rate and bioavailability of poorly water soluble

medication however still some producing difficulties and stability issues existed.

Topical delivery

Topical administration of drugs can have advantages over other methods for several reasons,

one of which is the avoidance of hepatic first pass metabolism of the drugs and related

toxicity effects.

Ocular and pulmonary delivery

For the treatment of eye disease, drugs are essentially deliveredtopically o/w micro-emulsion

have been investigated for ocularadministration, to dissolve poorly soluble drugs, to

increaseabsorption and to attain prolong release profile.

Parenteral delivery

Parenteral administration of medicines with restricted solubility could be a major downside in

business due to the very low quantity of drug truly delivered as a target web site.


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EVALUATION OF SEDDS[15]

Thermodynamic stability studies

Heating cooling cycle

Six cycles between white goods temperature 4⁰C and 45⁰C with storage at every temperature

of not but forty eight h is studied. Those formulations, that square measure stable at these

temperatures, square measure subjected to natural process check.

Centrifugation

Passed formulations are centrifuged at room temperature at 3500 rpm for 30min. Those

f rmu ati s that d es ’t sh w a y secti separati square measuretaken for the freeze

thaw stress test.

Freeze thaw cycle

Freeze was utilized to gauge the steadiness of formulation. Thermodynamic stability was

evaluated at difference temp. To check the effect of temp. the formulation was subjected to

freezethaw cycle (-20ºC) for 2-3 days. Those formulations passed this check showed smart

stability withno section separation, creaming, or cracking.

Dispersibility test

The potency of self-emulsification of oral nano or small emulsion is evaluated by employing

a customary USP XXII dissolution equipment for dispersibility check.

Solution Tested

1ml, Medium: 500 ml water, Temperature: 37 ± 1 ⁰C, Paddle spee: 50 rpm.

Grade A: Quickly forming (within one min) nano-emulsion, having a transparent or bluish

look.

Grade B : Quickly forming slightly less clear emulsion having a bluish white look.

Grade C: Fine milklite emulsion that shaped inside two min.

Grade D: uni teresti g,gray white emu si havi g s ight y i y k that’s s w t emu sify

(longer than 2 min.)

Grade E: Formulation, exhibiting either poor or stripped –down emulsification with giant oil

globules gift on thesurface.

Grade A and Grade B formulation can stay asnanoemulsion once distributed in unpleasant

person. While formulation fallingin Grade C can be counseled for SEDDS formulation.


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Turbidimetric evaluation

Nepheloturbidimetric evaluation is done to monitor the growth of emulsification. Fixed

quantity of Self emulsifying system is added to fixed quantity of suitable medium (0.1N

hydrochloric acid) under continuous stirring (50rpm) on magnetic hot plate at appropriate

temperature, and the increase in turbidity is measured, by using a turbidimeter.

However, since the time required for complete emulsification is too short, it is not possible to

monitor the rate of change of turbidity (rate of emulsification).

Viscosity determination

The SEDDS system is generally administered in soft gelatin or hard gelatin capsules. So, it

should be easily pourable into capsules and such systems should not be too thick. The

rheological properties of the micro emulsion are evaluated by Brookfield viscometer. The

viscosities determination conform whether the system is w/o or o/w. If the system has low

viscosity then it is o/w type of the system. If the system has high viscosity then it is w/o type

of the system.

Droplet size analysis

The droplet size of the emulsions is determined byphoton correlation spectroscopy (which

analyses the fluctuations in light scattering due to Brownian motion of the particles) using a

Zetasizer able to measure sizes between 10 and 5000nm.

Refractive index and percent transmittance

Refractive index and percent transmittance prove the transparency of formulation. The

refractive index of the system is measured by refractometer by putting a drop of solution on

slide and comparing it with water (1.333).The percent transmittance of the system is

measured at particular wavelength using UV spectrophotometer by using distilled water as

blank. If refractive index of system is similar to the refractive index of water (1.333) and

formulation have percent transmittance >99 percent, then formulation have transparent

nature.

Electro conductivity study

The SEDDS contains ionic or non-ionic surfactant, oil, and water. This test is performed for

measurement of the electroconductive nature of system. The electro conductivity of resultant


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system is measured by electro conductometer. In conventional SEDDSs, the charge on an oil

droplet is negative due to presence of free fatty acids.

In vitro diffusion study

In vitro diffusion studies are carried out to study the drug release behavior of formulation

from liquid crystalline phase around the droplet using dialysis technique.

Drug content

Drug from pre-weighed SEDDS is extracted by dissolving insuitable solvent. Drug content in

the solvent extract was analyzed by suitable analytical method against the standard solvent

solution of drug.

Application of SEDDS[12]

Improvement in Solubility and bioavailability. If SEDDS is employed to include the drug, the

solubility will increases because as a result of it circumvents the dissolution step in of BCS

Class-П drug (L w s ubi ity/high permeabi ity).

Ketoprofen, a non-steroidal anti-inflammatory drug (NSAID) is moderately hydrophobic (log

0.979). F r sustai ed u har ess f rmu ati it’s a drug f a ter ative and through chronic

medical aid it’s has high p te tia f r viscus irritation. Ketoprofen shows incomplete

unhareness from sustained unhareness formulations attributed to its low solubility. The

SEDDS formulation of this drug enhanced bioavailability due to increase in the solubility and

it also minimizes the gastric irritation. The release of NSAID in SEDDS is sustained because

of incorporation of gelling agent. The lipid matrix interacts readily with water in SEDDS,

leading to the formation of a fine particulate oil in-water (o/w) emulsion.The drug is

delivered to the g.i membrane by the emulsion droplets, in the dissolved state readily

accessible for absorption. Therefore SEDDS shows increase in AUC i.e. bioavailability and

Cmax of many drugs.

Protection against biodegradation

The self-emulsifying drug delivery system is ready to scale back degradation additionally as

improve absorption is also particularly helpful for medication that have low solubility and

degradation within the GI tract and low oral bioavailability. Because of acidic hydrogen ion

concentration, enzymatic degradation or hydrolyte in stomach, many drugs are degraded in

physiological system. These degradation processes will be well protected once drug is given


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within the style of SEDDS, as liquid crystalline innovate SEDDS may act as barrier between

degradation atmosphere and the drug. For example Acetylsalicylic acid (Log P=1.2,

Mw=180), a drug that degrades in the GI tract because in an acid environment, it is readily

hydrolyzed to salicylic acid. By the Oral Lipid Matrix, the oral bioavailability of un-

degraded acetylsalicylic acid is improved by 73%.

Controlling the release of drug

Sustained unleash, bioavailability improvement and bated internal organ of NSAID achieved

by completely different formulation approaches that embrace preparation of matrix pellets of

nano-crystalline NSAID, sustained unleash NSAID small particles and floating oral NSAID

systems and transdermic systems of NSAID. Processing, stability, and economic problems

are the drawbacks of preparation and stabilization of nano-crystalline or improved solubility

forms of drug. When NSAID is bestowed in SEDDS formulation, this problem can be

successfully overcome. The SEDDS formulation of this drug enhanced bioavailability due to

increase in thesolubility and it also minimizes the gastric irritation. The release of NSAID in

SEDDS is sustained because of incorporation of gelling agent. The lipid matrix interacts

readily with water in SEDDS, leading to the formation of a fine particulate Oil in-water (o/w)

emulsion.

Some representative products as SEDDS in market

Active

moiety

Trade

name

Company

name Use

Tretinoin Vesanoid Roche Used in the treatment of acute

promyelocytic leukemia

Isotretinoin Accutane Roche Used to treat cystic acne

Cyclosporine Gengraf Abbott Used as a powerful immunosuppressant

Saquinavir Fortovase Roche Used in HIV therapy

Amprenavir Agenerase GSK Used to treat HIV infection.

CONCLUSION

Self-emulsifying drug delivery system is a promising approach for the drugs with poor

aqueous solubility and hence it is more useful for the BCS Class II and Class IV drugs.

SEDDS upon administration reaches GIT system and take water from its surrounding

environment and forms the oil in water emulsion which disperse into fine droplets.

The droplet size of SEDDS ranges between 200nm -5µm. The fine droplet size provide the

higher surface area and thereby increasing absorption and greater bioavailability.


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LIQUE SOLID COMPACT DRUG DELIVERY SYSTEM: A REVIEW

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