USE OF SIMPLEX LATTICE DESIGN IN DEVELOPMENT OF ORAL SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM CONTAINING ROSUVASTATIN CALCIUM
Objective: The aim of the present work was to enhance the solubility of rosuvastatin calcium by self-nano emulsifying drug delivery system (SNEDDS) using mixtures of oil, cosolvent, surfactant and cosurfactant.
Methods: Based on solubility study and emulsification efficiency, Preliminary investigations of various oils, surfactants and cosurfactants were carried out for the selection of the proper SNEDDS ingredients. 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 a combination of peceol: ethyl oleate by using the simplex lattice design. Prepared formulation evaluated for refractive index, turbidimetric, droplet size, zeta potential and polydispersity index, self-emulsification, stability tests, viscosity and in vitro diffusion studies.
Results: The best formula for SNEDDS in the current study were: 15% oil (peceol: ethyloleatein 1:1 ratio), 50% Labrasol and 35% Cremophor EL. All the SNEDDS batches globule size was found to be varied from 22.90±1.50 nm to 43.90±1.40 nm. and no significant variations in globule size were observed after 3 mo stability studies. All the batches % transparency was found to be varied from 95.40±1.40% to 99.50±1.10% and drug diffused in 10 min varied from 63.65±1.51% to 93.72±1.46 %.
Conclusion: The data suggest the use of rosuvastatin calcium SNEDDS to offer the potential for delivery and it increases the aqueous solubility and bioavailability of the 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. Asian J Pharm Clin Res 2016;9:174-9.
3. Sahoo SK, 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. Int J Appl Pharm 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. Gawali P, Gupta A, Kachare S, Kshirsagar S. Formulation and evaluation of matrix-based sustained release tablets of quetiapinefumarate and the influence of excipients on drug release. J Chem Pharm Res 2012;4:3073-81.
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 PharmSciTech 2008;9:191-6.
12. Nasr A, Gardouh A, Ghonaim H, Abdelghany E, Ghorab M. Effect of oils, surfactants and cosurfactants on phase behaviour and physicochemical properties of self-nano emulsifying drug delivery system for irbesartan and olmesartan. Int J Appl Pharm 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, et al. 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. Vogel AI. Vogel's textbook of quantitative chemical analysis. 5th ed. Jeffrey GH, Bassett J, Mendham J, Denney R. editors; 1989. p. 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 cosurfactants on phase behavior and physicochemical properties of self-nanoemulsifying drug delivery system for irbesartan and olmesartan. Int J Appl Pharm 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. p. 472-93.
27. Lewis GA, Mathieu D, Phan-Tan-Luu R. Pharmaceutical experimental design. New York: Marcel Dekker; 1999. p. 191-8.
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 Urrahman. A review on optimization of drug delivery system with experimental designs. Int J Appl Pharm 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-nano emulsifying drug delivery system for Irbesartan and Olmesartan. Int J Appl Pharm 2016;8:13-24.
This work is licensed under a Creative Commons Attribution 4.0 International License.