The document summarizes a study on developing a self-microemulsifying drug delivery system (SMEDDS) to enhance the solubility and dissolution of the poorly water-soluble drug candesartan cilexetil. SMEDDS were formulated using oils, surfactants, and cosurfactants. Pseudo ternary phase diagrams were used to optimize the formulations. Solid SMEDDS were developed and showed comparable drug dissolution to liquid SMEDDS. The solid SMEDDS formulations demonstrated enhanced drug release compared to commercial tablets, indicating their potential for improving bioavailability of poorly soluble drugs like candesartan cilexetil.

1. Self micro emulsified
drug delivery system
Presented by
T.SHIVAKUMAR
KOTTAM INSTITUTE OF
PHARMACY

2. WHAT IS SMEDDS
SMEEDS is mixture of oils,
surfactants, and cosurfactants, which
are emulsified in aqueous media
under conditions of gentle agitation
of digestive motility that would be
encountered in the gastro intestinal
(GI) tract.

3. AIM
Most of the new drug candidates in
development today are sparingly
soluble and associated with poor
bioavailability
The main purpose is to prepare
SMEDDS for oral bioavailability
enhancement of a poorly water soluble
drug

4. Bio pharmaceutical classification
system

5. according to bio pharmaceutical
classification system(BCS) the classII
drugs have poor solubility and high
permeability , thus the rate limiting
process of absorption is the drug
dissolution step. Formulation plays the
major role in improving the rate and
extent of absorption of such drugs from GI
tract.

6. Present study
In the present study, an attempt was
made to enhance the solubility and in
vitro dissolution of candesartan
cilexetil byformulating it as SMEDDS
for filling into hard gelatin capsules.

7. Drug profile
Candesartan Cilexetil a prodrug is
hydrolyzed to candesartan during
absorption from the gastrointestinal
tract., practically insoluble in water.
Category: Antihypertensive Agents
Subcategory: Angiotensin II Receptor
Antagonist

8. Structure

9. Materials
 Drug- Candesartan cilexetile-
Oil -Miglyol 812
Surfactants- Cremophor EL &Tween 80
Cosurfactant -Labrasol

10.  The quantity of each content will be taken
according to the pseudo ternary phase
diagram
This diagram is very essential in
manipulation of ingredients in the
formulation of SMEDDS

11. CONSTRUCTION OF PSUEDO TERNARY
PHASE DIAGRAMS:
The pseudoternary phase diagrams of oil, surfactant–
cosurfactant, and water were developed to optimize the
formulation using a water titration method. The mixtures
of oil and surfactant–cosurfactant ratios were diluted with
water in a dropwise addition. Phase diagrams were constructed
in the presence of drug to obtain the optimum concentrations
of oil, surfactant, and cosurfactant. SMEDDS form fine oil–
water emulsions upon addition to an aqueous media under
gentle agitation.

12. Pseudo ternary phase
diagram
The gray area indicates the microemulsion region

13. formulation
Four self-microemulsifying formulations were prepared
using mixtures of oils, surfactants, and cosurfactants in
various proportions. The self-microemulsification
properties, droplet size, and zeta potential of these
formulations were studied upon dilution with water.
The optimized liquid SMEDDS formulation was
converted into free flowing powder by adsorbing onto a
solid carrier for encapsulation.

15. images of pure drug substance (left), solid SMEDDS
(right; magnification

16. Dissolution studies
The dissolution characteristics of solid
intermediates of SMEDDS filled into hard gelatin
capsules was investigated and compared with
liquid formulation and commercial formulation
to ascertain the impact on self-emulsifying
properties following conversion.

17. Results
The results indicated that solid intermediates showed
comparable rate and extent of drug dissolution in a
discriminating dissolution medium as liquid SMEDDS
indicating that the self-emulsifying properties of
SMEDDS were unaffected following conversion. Also,
the rate and extent of drug dissolution for solid
intermediates was significantly higher than commercial
tablet formulation. The results from this study
demonstrate the potential use of SMEDDS as a means of
improving solubility, dissolution, and concomitantly the
bioavailability.

18. studies

19. Advantages
 Protection of sensitive drug substances.
The emulsion droplets will deliver the drug to GI
mucosa in dissolved state readily accessible for
absorption
When a polymer is incorporated in terms of SMEDDS
it gives prolonged release of medicament
They are comprised of aqueous and oily components
and therfore can accommodate both hydrophilic aswell
as lipophylic drugs

20. Disadvantages
Chemical instabilities
Irritates GIT
Precipitation of the lipophilic drugs
Physical and chemical changes in
crystalline solid in Cryogenic grinding

21. CONCLUSION
A SMEDDS formulation of a poorly water-soluble
drug, candesartan cilexetil was formulated for direct
filling into hardgelatin capsules for oral
administrationshowed faster rate of drug release than
the marketed product in
a discriminating dissolution media. The results from
this study
demonstrate the utility of SMEDDS to enhance
solubility and
dissolution of sparingly soluble compounds like
candesartan
which may result in improved therapeutic performance

22. REFERENCES
 1. Robinson JR. Introduction: semi-solid formulations for oral
drug delivery. Bull Tech Gattefosse. 1996;89:11–3
 2. Aungst BJ. Novel formulation strategies for improving oral
bioavailability of drugs with poor membrane permeation or
presystemic metabolism. J Pharm Sci. 1993;82:979–87.
 3. Constantinides PP. Lipid microemulsions for improving drug
dissolution and oral absorption: physical and biopharmaceutical
aspects. Pharm Res. 1995;12:1561–72.
 4. Pouton CW. Formulation of self-emulsifying drug delivery
systems.

23. Thank you….