1. 1Self-Emulsifying Drug Delivery System (SEDDS)Presented by,Mr.Panke Ashutosh AbhimanyuM. Pharm-II Sem.PUNE DISTRICT EDUCATION ASSOCIATIONSSeth Govind Raghunath Sable College of Pharmacy, Saswad.Department of Pharmaceutics2014-15

2. 2CONTENTS 3. Introduction3 Self-emulsifying drug delivery systems(SEDDS ) are defined as isotropic mixturesof oils, surfactants and co-solvents. 4. Advantages41. Enhanced oral bioavailability2. Selective targeting of drug(s) towardspecific absorption window in GIT.3. Protection of drug(s) from the hostileenvironment in gut.4. Reduced variability including food effects.5. Protective of sensitive drug substances. 5. Drawback Of SEDDS5 Lack of good predicative in vitro models forassessment of the formulations. The large quantity of surfactant in self-emulsifyingformulations (30-60%) irritates Volatile co-solvents can migrate on capsuleshell. 6. Composition of SEDDSs6Composition of SEDDSs Drug (API) Oil SurfactantCo-Surfactants 7. Drug7The drugs with poor aqueous solubility and high permeability are classified asclass II drug by Biopharmaceutical classification system (BCS). These drugs areuse for formulate SEDDS.Class IILow SolubilityHigh PermeabilityClass IHigh SolubilityHigh PermeabilityClass IVLow SolubilityLow PermeabilityClass IIIHigh SolubilityLow PermeabilityPermeabilitySolubility 8. Oil8 Oils are the most important excipient. Help in solubilizing the lipophilic drug in a high amount. Facilitate self-emulsification and increase the fraction oflipophilic drug transported. Increase absorption from the GI tract. Both long-chain triglyceride and medium-chain triglycerideoils with different degrees of saturation have been used forthe formulation of SEDDSs. 9. Lipid Ingredients9 Corn oil Olive oil Sesame oil Soyabean oil Peanut oil Hydrogenated soyabean oil Hydrogenated vegetable oils 10. Surfactants10 Non-ionic surfactants with high hydrophiliclipophilicbalance (HLB) values are used in formulation of SEDDSs Surfactant strength ranges between 3060% w/w of theformulation in order to form a stable SEDDS. A large quantity of surfactant may irritate the GIT. Non-ionic surfactants are less toxic as compared to ionicsurfactants. 11. List of Surfactants11 Polysorbate 20 (Tween 20) Polysorbate 80 (Tween 80) Sorbitan monooleate (Span 80) Polyoxy-40- hydrogenated castor oil 12. Co-solvents/Co-Surfactants12 Co-solvents help to dissolve large amounts ofhydrophilic surfactants or the hydrophobic drug inthe lipid base. These solvents sometimes play the role as co-surfactantin the micro-emulsion systems. 13. Co-solvents/Co-Surfactants13Co-solvents Co-surfactants Span 20 Span 80 Capryol 90 Lauroglycol Ethanol Glycerin Propylene glycol PEG 14. Mechanism of self emulsification14 The free energy of the conventional emulsion is adirect function of the energy required to create anew surface between the oil and water phases In emulsification process the free energy (G)associated is given by the equation: 15. Mechanism of self emulsification15where, G = free energy associated with the process(ignoring the free energy of mixing) N = number of droplets r = Radius of droplets = interfacial energy 16. Mechanism of self emulsification16 The two phases of emulsion tend to separate withtime to reduce the interfacial area, and subsequently,the emulsion is stabilized by emulsifying agents. 17. General formulation Approach Preliminary solubility profiling studies are performed forselection of oil. Drug excipient compatibility studies. Preparation of a series of SEDDS system containing drugin various oil and surfactant with different combinations. Optimization of formulation on the basis of in vitro self-emulsification17properties, droplet size analysis, stabilitystudies, robustness to dilution upon addition to waterunder mild agitation conditions. 18. Evaluation of SEDDS181. Thermodynamic Stability Studies2. Dispersibility test3. Turbidimetric Evaluation4. Viscosity Determination5. Droplet Size Analysis and Particle Size Measurements6. Refractive Index and Percent Transmittance7. Electro Conductivity Study8. In vitro Diffusion Study9. Drug Content10. In vivo permeability studies 19. Thermodynamic Stability Studies19Heating cooling cycle Six cycles between refrigerator temperature 4Cand 45C with storage at each temperature of notless than 48 h is studied. Those formulations, which are stable at thesetemperatures, are subjected to centrifugation test. 20. Thermodynamic Stability Studies20Centrifugation Passed formulations are centrifuged at roomtemperature at 3500 rpm for 30 min. Those formulations that does not show any phaseseparation are taken for the freeze thaw stresstest. 21. Thermodynamic Stability Studies21 Freeze thaw cycle:- Freeze was employed to evaluate the stability offormulation.Thermodynamic stability was evaluated at differencetemp. To chake the effect of temp. the formulation wassubjected to freeze thaw cycle(-20C) for 2-3 days. 22. Freeze thaw cycle:-22 Formulation are exposed to at least three freezethaw cycles. Those formulations passed this testshowed good stability with no phase separation,creaming, or cracking. Suppose it shows thermodynamically unstableformulation which had larger droplet sizedistribution upon dilution. 23. Dispersibility test23 The efficiency of self-emulsification of oral nano or microemulsion is evaluated by using a standard USP XXIIdissolution apparatus 2 for dispersibility test. Solution Tested: 1ml Medium: 500 ml water Temperature: 37 1 C. Paddle speed : 50 rpm 24. Dispersibility test24 Grade A: Rapidly forming (within 1 min) nano-emulsion, havinga clear or bluish appearance. Grade B : Rapidly forming slightly less clear emulsion having abluish white appearance. Grade C: Fine milky emulsion that formed within 2 min. Grade D: Dull, grayish white emulsion having slightly oily appearancethat is slow to emulsify (longer than 2 min). Grade E: Formulation, exhibiting either poor or minimal emulsificationwith large oil globules present on the surface. Grade A and Grade B formulation will remain as nanoemulsion whendispersed in GIT. While formulation falling in Grade C could berecommended for SEDDS formulation. 25. Turbidimetric Evaluation25 Nepheloturbidimetric evaluation is done to monitorthe growth of emulsification. Fixed quantity of Selfemulsifying system is added to fixed quantity ofsuitable medium (0.1N hydrochloric acid) undercontinuous stirring (50 rpm) on magnetic hot plate atappropriate temperature, and the increase inturbidity is measured, by using a turbidimeter However, since the time required for completeemulsification is too short, it is not possible tomonitor the rate of change of turbidity (rate ofemulsification) 26. Viscosity Determination26 The SEDDS system is generally administered insoft gelatin or hard gelatin capsules. So, it shouldbe easily pourable into capsules and suchsystems should not be too thick to create aproblem.The rheological properties of the microemulsion are evaluated by Brookfield viscometer. 27. Droplet Size Analysis27 The droplet size of the emulsions is determined byphoton correlation spectroscopy (which analysesthe fluctuations in light scattering due to Brownianmotion of the particles) using a Zetasizer able tomeasure sizes between 10 and 5000 nm. 28. Refractive Index and Percent Transmittance28 Refractive index and percent transmittance prove thetransparency of formulation. The refractive index of the system is measured byrefractometer by putting a drop of solution on slideand comparing it with water (1.333). The percent transmittance of the system is measured atparticular wavelength using UV spectrophotometer byusing distilled water as blank. If refractive index of system is similar to the refractiveindex of water (1.333) and formulation have percenttransmittance > 99 percent, then formulation havetransparent nature. 29. Electro Conductivity Study29 The SEDD system contains ionic or non-ionicsurfactant, oil, and water. This test is performed for measurement of theelectro conductive nature of system. The electro conductivity of resultant system ismeasured by electro conductometer. In conventional SEDDSs, the charge on an oildroplet is negative due to presence of free fattyacids. 30. In vitro Diffusion Study30 In vitro diffusion studies are carried out to study thedrug release behavior of formulation from liquidcrystalline phase around the droplet using dialysistechnique. 31. Drug Content31 Drug from pre-weighed SEDDS is extracted bydissolving in suitable solvent. Drug content in thesolvent extract was analyzed by suitable analyticalmethod against the standard solvent solution ofdrug. 32. Conclusion32Selfemulsifying drug delivery systems are apromising approach for the formulation of drugcompounds with poor aqueous solubility. Theoral delivery of hydrophobic drugs can be madepossible by SEDDSs, which have been shown tosubstantially improve oral bioavailability. Withfuture development of this technology, SEDDSswill continue to enable novel applications in drugdelivery and solve problems associated with thedelivery of poorly soluble drugs. 33. References33 34. References P.A. Patel, et al Self Emulsifying Drug Delivery System: A Review, Research J.34Pharm. and Tech. 1(4): Oct.-Dec. 2008,313-323. A.Kumar, et al Self Emulsifying Drug Delivery System (SEDDS): Future Aspect .Int J Pharm Pharm Sci, Vol 2, Suppl 4, 713,7-13. J.Tang, et al Preparation of Self-emulsifying Drug Delivery Systems of Ginkgobiloba Extracts and In vitro Dissolution Studies. Asian Journal of TraditionalMedicines, 2006, 1,3-4 . R. Sachan, et al Self-Emulsifying Drug Delivery System A Novel Approach forenhancement of Bioavalibility. Pharm Tech Res.2010,2(3) 1738-1745 . M. Chitneni et al Intestinal Permeability Studies of Sulpiride Incorporated in to self-microemulsifyingdrug delivery system (smedds) Pak. J. Pharm. Sci., .24,2, April2011,.113-121. 35. 35THANK YOU !