(SMEDDS)

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Self Emulsifying Drug Delivery System (SEDDS) : 

Self Emulsifying Drug Delivery System (SEDDS) Mr. Khamkar Ganesh Shashikant ……. under guidance of Mr. Kshirsagar R V Sir

Self-Micro Emulsifying Drug Delivery System (SMEDDS) : 

Self-Micro Emulsifying Drug Delivery System (SMEDDS) INTRODUCTION Drawbacks of SEDDS Approaches of Delivery Systems FORMULATION Drug Oils Surfactant Co-surfactant Co-solvent Consistency builder Polymers FACTORS AFFECTING SMEDDS MECHANISM OF SMEDDS RECENT ADVANCEMENTS Self-emulsifying sustained or controlled-release Tablets Capsules Suppositories Microemulsion Nanoparticles Pellets EVALUATION OF SMEDDS CONCLUSION REFERENCES

Self-Micro Emulsifying Drug Delivery System (SMEDDS) : 

Self-Micro Emulsifying Drug Delivery System (SMEDDS) Introduction lipophillic in nature poor aqueous solubility (BCS class II drugs) Types (SEDDS) formed using surfactants of HLB < 12 (SMEDDS) formed with surfactants of HLB > 12. Both are stable preparations improve the dissolution due to increased surface area on dispersion. Drawbacks of SEDDS Approaches of Delivery Systems

Drawbacks of SEDDS Chemical instabilities Irritates GIT Precipitation of the lipophilic drugs Physical and chemical changes in crystalline solid in Cryogenic grinding

Self-Micro Emulsifying Drug Delivery System (SMEDDS) : 

Self-Micro Emulsifying Drug Delivery System (SMEDDS) Approaches of Delivery Systems

Self-Micro Emulsifying Drug Delivery System (SMEDDS) : 

Self-Micro Emulsifying Drug Delivery System (SMEDDS) FORMULATION Drug Oils Surfactant Co-surfactant Co-solvent Consistency builder Polymers

Drug : 

Drug Win 54954 Cyclosporin Halofantrine Ontazolast Vitamin E Coenzyme Q10 Ro-15-0778 Simvastatin Biphenyl Dimethyl Dicarboxylate Indomethacin Progesterone Tocotrienols Danazol Carvediol Silymarin Atorvastatin Itraconazole Atovaquone Seocalcitol PNU-91325 Model Compounds including disopyramide, ibuprofen, Ketoprofen, and Tolbutamide

Oils : 

Oils Long chain triglyceride Medium chain triglyceride …….oils with different degree of saturation Example: olive oil, corn oil, soyabean oil, palm oil and animal fats.

Surfactant : 

Surfactant Non-ionic surfactants with high HLB value Example: Ethoxylated polyglycolysed glycerides, Tween 80,. Long chain alkyl sulfonate sulfate surfactants, Example: sodium dodecyl benzene sulfonate, sodium lauryl sulfate and dialkyl sulfo succinate Quaternary ammonium salts. Fatty alcohols Example: lauryl, cetyl and stearyl, glyceryl esters, fatty acid esters and polyoxyethylene derivatives .

co-surfactant : 

co-surfactant co-surfactant of HLB value 10-14 is used.Hydrophilic co-surfactants , pentanol and octanol to reduce the oil water interface and allow the spontaneous formulation of micro emulsion.

Co-solvent : 

Co-solvent for oral administration. Examples are ethanol, propylene glycol, and polyethylene glycol aqueous solvent such as Triacetin, (an acetylated derivative of glycerol) for example glyceryl triacetate Triacetin

Consistency builder : 

Consistency builder Example: tragacanth, cetyl alcohol, stearic acids and /or beeswax

Polymers : 

Polymers Should not ionizable at physiological pH and being capable of forming matrix Example: hydroxy propyl methyl cellulose, ethyl cellulose, etc

Self-Micro Emulsifying Drug Delivery System (SMEDDS) : 

Self-Micro Emulsifying Drug Delivery System (SMEDDS) Factors affecting Drug with limited solubility in water and lipids are most difficult to deliver by SMEDDS. A risk of precipitation, as dilution of SMEDDS will lead to lowering of solvent capacity of surfactant or co-surfactant. HLB, Chain length Degree or unsaturation of the fatty acid, Molecular weight of the hydrophilic portion Concentration of the emulsifier govern polarity of the droplets.

Self-Micro Emulsifying Drug Delivery System (SMEDDS) : 

Self-Micro Emulsifying Drug Delivery System (SMEDDS) MECHANISM No single theory explains all aspects of microemulsion formation. Schulman et al. considered that the spontaneous formation of microemulsion droplets Thermodynamic theory of formation of microemulsion ÄG = S N a r 2 óð where, ÄG is the free energy associated with the process (ignoring the free energy of the mixing), N is the number of droplets r is radius ó is arepresents athe ainterfacial aenergy.

Self-Micro Emulsifying Drug Delivery System (SMEDDS) : 

Self-Micro Emulsifying Drug Delivery System (SMEDDS) RECENT ADVANCEMENTS Self-emulsifying sustained or controlled-release Tablets Capsules Suppositories Microemulsion Nanoparticles Pellets

Self-Micro Emulsifying Drug Delivery System (SMEDDS) : 

Self-Micro Emulsifying Drug Delivery System (SMEDDS) EVALUATION OF SMEDDS Estimation of the increased drug dissolution and absorption from large surface area afforded by the emulsion Droplet polarity Droplet size, 10 to 200 nm. (Coulter nano-sizer)

Self-Micro Emulsifying Drug Delivery System (SMEDDS) : 

Self-Micro Emulsifying Drug Delivery System (SMEDDS) CONCLUSION SMEDDS appears to be unique and industrially feasible approach to overcome the problem of low oral bioavailability associated with the lipophillic drugs.

Self-Micro Emulsifying Drug Delivery System (SMEDDS) : 

Self-Micro Emulsifying Drug Delivery System (SMEDDS) REFERENCES 1 Burcham D.L.Mauri M.B., Hausner E.A. and Huang S.M., Improved oral bioavailability of the hypocholesterolemic DMP 565 in dogs following oral dosing in oil and glycol solutions, Biopharm and Drug Dispos. 1997, 18, 737.742. 2. Serajuddin A.T.M. Sheen P.C. Mufson D. Bernstein D.F. and Augustine M.A.,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. 3. Myers R.A. and Stella V.J.Systemic bioavailability of penclomedine (NSC-338720) from oil--in-water emulsions administered intraduodenally to rats, Int. J. Pharm., 1992, 78, 217.226.

Self-Micro Emulsifying Drug Delivery System (SMEDDS) : 

Self-Micro Emulsifying Drug Delivery System (SMEDDS) 4. Schwendener R.A.and SchottH., Lipophilic 1-âd arabino-furanosyl cytosine derivatives in liposomal formulations for oral and parenteral antileukemic therapy in the murine L1210 leukemia model, J. Cancer Res. Clin Oncol.1996, 122, 723.726. 5. Perng C.H. Kearney A.S. Patel K. Palepu N.R. and Zuber G. Investigation of formulation approaches to improve the dissolution of SB-210661 a poorly water soluble 5-lipoxygenase inhibitor. Int. J. Pharm. 1998, 176, 31-38.

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