SNEDDS USE OF SIMPLEX LATTICE DESIGN IN DEVELOPMENT OF SELF NANOEMULSIFYING DRUG DELIVERY SYSTEM CONTAINING ROSUVASTATIN CALCIUM
Objective: The aim of present work was enhancing permeability and solubility of rosuvastatin calcium by self nanoemulsifying drug delivery system (SNEDDS) using mixtures of oil, co-solvent, surfactant and co-surfactant.
Methods: Screening of surfactants and oil was done by solubility method and pseudo ternary phase diagrams of oil, surfactant/co-surfactant and water were developed using water titration method. Pseudo-ternary phase diagrams were constructed to identify the efficient self-emulsification region. A series of SNEDDS formulations were prepared using labrasol/cremophor El with combination of peceol/ethyl oleate by using simplex lattice design. Prepared formulation evaluated for refractive index, turbidimetric, droplet size, zeta potential & polydispersity index, self-emulsification, stability tests, viscosity and in-vitro diffusion studies.
Results: The optimal SNEDDS was comprised of 15% oil (peceol : ethyloleate in 1:1 ratio), 50% Labrasol and 35% Cremophor EL. The average globule size of optimized formulation was about 22.95±1.50 nm was found. No significant variations in globule size and rosuvastatin content in SNEDDS were observed after 3 month stability study. In-vitro diffusion studies showed more than 95% drug diffusion within 15 minutes.
Conclusion: The data suggest use of rosuvastatin calcium SNEDDS to provide great potential for delivery and it increase the aqueous solubility, permeability and bioavailability of drug.
2. Dayyih W, Mallah EM, Al-Ani IH, Arafat TA. Liquorice beverage effect on the pharmacokinetic parameters of atorvastatin simvastatin, and lovastatin by liquid chromatography - mass spectroscopy / mass spectroscopy. Asian J Pharm Clin Res, 2016;9:174-9.
3. Sahoo S K, Suresh P, Acharya, U. Design and development of self-microemulsifying drug delivery systems of telmisartan for enhancement of in vitro dissolution and oral bioavailability in rabbit. International Journal of Applied Pharmaceutics,2018;10:117-26.
4. Nagarsenker MS, Date A. Design and evaluation of self-nanoemulsifying drug delivery systems for cefpodoximeproxetil. Int J Pharm, 2007;329:166-72.
5. Wang L, Dong J, Chen J, Eastoe J, Li Xuefeng. Design and optimization of a new self-nanoemulsifying drug delivery system. J Colloid Interface Sci, 2009;330:443-8.
6. Hoffman A, Dahan A. Rationalizing the selection of oral lipid based drug delivery systems by an in vitro dynamic lipolysis model for improved oral bioavailability of poorly water soluble drugs. J Controlled Release, 2008;129:1-10.
7. Skoog DA, Holler FJ, Crouch SR. Instrumental analysis. 11th ed. Delhi: Cengage Learning India Pvt Ltd; 2012.
8. Oza NA, Patel DM, Patel PU, Patel LD, Koshia HG, Ramkishan A. Establishment of level A correlation between Ex-Vivo and In-Vivo release of carvedilol reservoir-type transdermal drug delivery system. Inventi impact NDDS, 2014;116-23.
9. Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and self-microemulsifying drug delivery systems. Eur J Pharm Sci 2000;11:93-8.
10. Shen H, Zhong M. Preparation and evaluation of self-microemulsifying drug delivery systems (SMEDDS) containing atorvastatin. J Pharm Pharmacol 2006;58:1183-91.
11. Kale A, Patravale V. Design and evaluation of self-emulsifying drug delivery systems of nimodipine. AAPS Pharm Sci Tech 2008;9:191-6.
12. Nasr A, Gardouh A, Ghonaim H, Abdelghany E, Ghorab M. Effect of oils, surfactants and co-surfactants on phase behaviour and physicochemical properties of self nanoemulsifying drug delivery system for irbesartan and olmesartan. International journal of applied pharmaceutics 2016; 8:13-24.
13. Ashok K, Kuldeep S, Murugesh K, Sriram R, Ramesh M. Formulation and development of an albendazole self-emulsifying drug delivery system with enhanced systemic exposure. Acta Pharm 2012;62:563-80.
14. Patel J, Patel A, Raval M, Sheth N. Formulation and development of a self-nanoemulsifying drug delivery system of irbesartan. J Adv Pharm Tech Res 2011;2:9-16.
15. Dixit R, Nagarsenker M. Design, optimization and evaluation of self-nanoemulsifying granules of ezetimibe. Eur J Pharm Sci 2008;35:92-183.
16. Zakia B, Suyang Z, Wenli Z, Junlin W. Formulation, development and bioavailability evaluation of a self-nanoemulsifying drug delivery system of atorvastatin calcium. Int J Pharm 2013;29:1103-13.
17. Balakrishnan P, Lee J, Oh D. Enhanced oral bioavailability of dexibuprofen by a novel solid self-emulsifying drug delivery system. Eur J Pharm Biopharm 2009;72:539-45.
18. Jumaa M, Kleinebudde P, Muller BW. Mixture experiments with the oil phase of parenteral emulsions. Eur. J. Pharm. Biopharm. 1998;46:161–7.
19. Kang BK, Lee JS, Chon SK, Jeong SY, Yuk SH, Khang G, Lee HB, Cho SH. Development of self-micro-emulsifying drug delivery systems for oral bioavailability enhancement of simvastatin in beagle dogs. Int. J. Pham. 2004; 274:65-73.
20. Sriamornsak P, Limmatvapirat S, Piriyaprasarth S, Mansukmanee P, Huang Z. A new self-emulsifying formulation of mefenamic acid with enhanced drug dissolution. Asian J Pharm Sci 2015;10:121-7.
21. Parmar K, Patel J, Sheth N. Self nano-emulsifying drug delivery system for embelin: design, characterization and in vitro studies. Asian J Pharm Sci 2015;10:396-404.
22. Gursoy RN, Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed Pharmacother 2004;58:173-82.
22. Vogel AI. Vogel's textbook of quantitative chemical analysis. 5th ed. Jeffrey GH, Bassett J, Mendham J, Denney R. editors; 1989:220-5.
23. Zhang P, Liu Y, Feng N, Xu J. Preparation and evaluation of self-microemulsifying drug delivery system of oridonin. Int J Pharm 2008;355:269-76.
24. Nasr A, Gardouh A, Ghonaim H, Abdelghany E, Ghorab M. Effect of oils, surfactants and co-surfactants on phase behavior and physicochemical properties of self-nanoemulsifying drug delivery system for irbesartan and olmesartan. International journal of applied pharmaceutics 2016; 8:13-24.
25. Ehab I, Saleh A, Ahmed M, Mansoor A. Preparation and in-vitro characterization of self-nanoemulsified drug delivery system of all-trans-retinol acetate. Int J Pharm 2004;285:109-19.
26. Bolton S, Bon C. Pharmaceutical statistics: Practical and clinical Applications, 5th ed. Informa Healthcare. 2005: 472-93.
27. Lewis GA, Mathieu D, Phan-Tan-Luu R. Pharmaceutical experimental design. New York: Marcel Dekker; 1999: 191-98.
28. Anthony NA. Pharmaceutical experimental design and interpretation. 2nd ed. Taylor and Francis Group; 2006.
29. Khanam N, Alam MI, MD Yusuf Ali, QMAI Siddiqui, A ur rahman. A review on optimization of drug delivery system with experimental designs. International Journal of Applied Pharmaceutics, 2018; 10: 7-12.
30. Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and self-microemulsifying drug delivery systems. Eur J Pharm Sci 2000;11:93-8.
31. Asr A, Gardouh A, Ghonaim H, Abdelghany E, Ghorab M. Effect of oils, surfactants and co-surfactants on phase behavior and physicochemical properties of self-nanoemulsifying drug delivery system for Irbesartan and Olmesartan. International Journal of Applied Pharmaceutics 2016;8:13-24.
This work is licensed under a Creative Commons Attribution 4.0 International License.