Development of Solid Self – Nanoemulsified Drug Delivery System Containing Rosuvastatin
Authors: Thi Hai Yen Tran , Thi Yen Nguyen , Canh Hung Nguyen , Thi Nghia Phan , Bao Tung Pham , Dang Hoa Nguyen , Thi Thu Giang Vu 
Published: September 2020

This study aims to solidify the self-nanoemulsifying drug delivery system with rosuvastatin (SNEDDS Ros) for application in solid dosage forms. The liquid SNEDDS Ros system is solidified by granulation and spray drying methods. Solid SNEDDS Ros was evaluated on the drug content, the Carr index, nanoemulsification efficiency and several criteria of nanoemulsion, formed after emulsification of solid SNEDDS Ros, such as droplet size, polydispersion index (PDI), the drug proportion in the oil phase. The study results show that solid SNEDDS Ros, prepared by granulation method using Prosolv SMCC 90 as an adsorbent, had good flowability with the Carr index of about 15. The nanoemulsion, obtained after emulsification of the solid SNEDDS, had an average particle size of 15 nm, PDI less than 0.2, drug nanoemulsified efficiency of 94 % and drug proportion in the oil phase of 84%.

Keywords

Rosuvastatin, SNEDDS, Solid SNEDDS, solidification.

References

[1] A.G. Olsson, F. McTaggart, and A. Raza, Rosuvastatin: A Highly Effective New HMG-CoA Reductase Inhibitor. Cardiovasc. Drug Rev., 20 (2006) 303–328. https://doi.org/10.1111/j.1527-3466.2002.tb00099.x[2] A.M. Kassem, H.M. Ibrahim, and A.M. Samy, Development and optimisation of atorvastatin calcium loaded self-nanoemulsifying drug delivery system (SNEDDS) for enhancing oral bioavailability: in vitro and in vivo evaluation. J. Microencapsul 34 (2017) 319–333. https://doi.org/10.1080/02652048.2017.1328464[3] M.N. Ahsan and P.R. Prasad Verma, Solidified self nano-emulsifying drug delivery system of rosuvastatin calcium to treat diet-induced hyperlipidemia in rat: in vitro and in vivo evaluations. Ther. Deliv 8 (2017) 125–136. https://doi.org/10.4155/tde-2016-0071[4] S. Verma, S.K. Singh, P. R. P. Verma, and M. N. Ahsan, Formulation by design of felodipine loaded liquid and solid self nanoemulsifying drug delivery systems using Box-Behnken design. Drug Dev. Ind. Pharm. 40 (2014) 1358–1370. https://doi.org/10.3109/03639045.2013.819884[5] M.S. Reddy, Formulation and In Vitro Characterization of Solid-self Nanoemulsifying Drug Delivery System of Atorvastatin Calcium. Asian J. Pharm. 11 (2018) 991-999. https://dx.doi.org/10.22377/ajp.v11i04.1771.[6] N. Kulkarni, N. Ranpise, and G. Mohan, Development and evaluation of solid self nano-emulsifying formulation of rosuvastatin calcium for improved bioavailability. Trop. J. Pharm. Res. 14 (2015) 575–582. https://doi.org/10.4314/tjpr.v14i4.3[7] A.O. Kamel and A.A. Mahmoud, Enhancement of human oral bioavailability and in vitro antitumor activity of rosuvastatin via spray dried self-nanoemulsifying drug delivery system. J. Biomed. Nanotechnol. 9 (2013) 26–39. https://doi.org 10.1166/jbn.2013.1469.[8] H.A. Abo Enin and H.M. Abdel-Bar, Solid super saturated self-nanoemulsifying drug delivery system (sat-SNEDDS) as a promising alternative to conventional SNEDDS for improvement rosuvastatin calcium oral bioavailability. Expert Opin. Drug Deliv. 13 (2016) 1513–1521. https://doi.org/10.1080/17425247.2016.1224845