1. SELF EMULSIFIED DRUG DELIVERY
SYSTEM (SEDDS)
Presented By
B. Swadeep M.pharm.,
Mobile No 9032638446
M.R. COLLEGE OF PHARMACY
2. CONTENTS
INTRODUCTION
LIPID FORMULATION
CLASSIFICATION SYSTEM
FORMULATION DEVELOPMENT
SOLID SELF EMULSIFYING DRUG
DELIVERY SYSTEM
CHARACTERIZATION
BIOPHARMACEUTICAL ISSUES
M.R. COLLEGE OF PHARMACY
3. INTRODUCTION
Poor drug solubility is a frequently encountered
problem for pharmaceutical formulation scientists,
since most of the new chemical entities synthesized
are hydrophobic.
Lipid based systems are a promising choice for the
delivery of hydrophobic drug substances. These
systems avoid the dissolution step upon oral
administration and bypass first pass effect.
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4. DEFINITION
SEDDS are isotropic mixtures of drug, lipids and
surfactants, usually with one or more hydrophilic co-
solvents or co-emulsifiers. Upon mild agitation
followed by dilution with aqueous media, these
systems can form fine (oil in water) emulsion
instantaneously.
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5. MECHANISM
According to Reiss:
self-emulsification occurs when the entropy
change that favors dispersion is greater than
the energy required to increase the surface
area of the dispersion.
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6. LIPID FORMULATION
CLASSIFICATION SYSTEM (LFCS)
TYPE 1
DRUG
+
LIPID
+
LIPOPHILIC
SURFACTANT
HLB< 12
DRUG
+
LIPID
DRUG
+
LIPID
+
COSOLVENT
+
HYDROPHILIC
SURFACTANTS
HLB>12
DRUG
+
COSOLVENTS
+
HYDROPHILIC
SURFACTANTS
TYPE 4TYPE 3TYPE 2
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8. EXCIPIENTS
LIPIDS SURFACTANTS COSOLVENTS
Solubilize
lipophilic drug
Promotes
lymphatic
transport
protection of
drugs
Eg: Corn oil,
Olive oil
Usual surfactant
concentration 30-60%
w/w formulation
Increases
permeability
Eg:Tween,Span,
Labrafil,Cremophor
Enhance the
dissolution of
surfactants & drug
in lipid base
Act as cosurfactants
in SMEDDS
Eg Ethanol,
Propylene
glycol,PEG
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13. CAPSULE
FILLING
• Liquid or semisolid self emulsifying formulations are
encapsulatedincapsulefororalroute
SPRAY
DRYING
• Lipids, surfactants, drug, solid carriers are solubilized before
spray drying.
• The solubilized liquid formulation is then atomized in to a spray
of droplets.
• The droplets introduced in to a drying chamber , water
evaporates forming dry particles
• Such particles can be further prepared into tablets or capsules
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14. SPRAY
COOLING
• Molten formula is sprayed in to a cooling chamber
• On contact with cooling air, the matter droplets congeal
re-crystallize in to spherical solid particles
• To atomize the liquid mixture and to generate droplets
rotary pressure, two fluid or ultrasonic atomizers are
used
ADSORPTION
ON SOLID
CARRIERS
• SEDDS can be absorbed up to (70% w/w) on suitable
careers
• Solid cross linked polymers, nanoparticle adsorbents
• Eg: Silica, slicates, magnesium tri silicate, magnesium
hydroxide, talcum, cross povidone, cross linked Na
CMC, cross linked poly methyl methacrylate,
lactose,maltodextrin.
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15. Droplet size
Turbidity measurement
Electron microscopic studies
Emulsification time
Zeta potential measurement
Equilibrium phase diagram
Liquefaction time
Small angle neutron scattering
Small angle x-ray scattering
CHARECTERIZATION
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20. COMPOUND
SELECTION
Compounds which are in
BCS type II drugs
When conventional
formulations approaches i.e
salt or crystalline form ,
particle size reduction , solid
dispersions or the addition
surfactants have failed.
ROLE OF
LIPOLYSIS
Digestion of lipid
formulation could reduce the
solubility of the drug in the
GI gut lumen,which would
result in precipitation of the
drug and a decrease in the
absorption rate.
For such compounds type II,
type III systems might be
preferable , since the
presence of surfactant can
inhibit digestion of oil with
in the formulation.
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21. EFFECT OF
P-GP
Enhanced uptake of
hydrophobic drugs
formulated as SEDDS
from the GI tract is also
due to P-gp drug efflux.
Excipients incorporated
SEDDS/SMEDDS can inhibit
both presystemic drug
metabolism & intestinal
efflux mediated by P-gp
resulting in an increased oral
absorption of cytotoxic drugs.
LYMPHATIC
TRANSPORT
Primary physiological
purpose of the intestinal
lymphatic system is to
assimilate dietary lipid
from the gut.
Lymphatic transport can
be responsible for a
portion of the total uptake
of hydrophobic drugs.
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22. RECENT ADVANCES
• Helps to reduce or prevent drug
precipitation upon GI fluid dilution.
•Cellulose polymer, hydroxy propyl
methylcellulose (HPMC), was used
as a viscosity enhancer
SUPERSATURATED
SEDDS
• Incorporation of a small amount of
cationic lipid (2.5±3%),
oleylamine.
• Positively charged droplets
attracted to the negatively charged
physiological compounds in lumen.
POSITIVELY
CHARGED SEDDS
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23. LITERATURE UPDATES ON BIOAVAILABILITY
ENHANCEMENT USING SELF EMULSIFYING
FORMULATIONS
DRUG ENHANCEMENT DOSAGE FORM SPECIES
Acyclovir 3.5 fold Pure drug solution Male albino rats
Anethole Trithione 2.5 fold Tablets rabbits
Carvedilol 4.13 fold Commercial tablet Beagle dogs
Gentamycin 5 fold i.v saline Beagle dogs
Oleanolic acid 2.4 fold Tablet Rats
M.R. COLLEGE OF PHARMACY
24. Drug name Compound Dosage form Company
Neoral Cyclosporin Soft gelatin
capsules
Novartis
Norvir Ritonavir Soft gelatin
capsules
Abott laboratories
Fortavase Saquinavir Soft gelatin
capsules
Hoffmann-
LaRoche Inc.
Agenerase Amprenavir Soft gelatin
capsules
Glaxosmithkline
Solufen Ibuprofen Hard gelatin
capsules
Sanofi-Aventis
Lipirex Finofibrate Hard gelatin
capsules
Sanofi-Aventis
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25. REFERENCES
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M.R. COLLEGE OF PHARMACY
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