DEVELOPMENT OF MICROEMULSION FORMULATION FOR ORAL DELIVERY OF ROSUVASTATIN CALCIUM
Abstract
The purpose of conducting this study was to prepare an oral microemulsion formulation of Rosuvastatin calcium (RC) to improve its water solubility. Oil in water microemulsion was formulated using Oleic acid, Tween 80 and Polyethylene Glycol-400(PEG-400) as oil, surfactant and co-surfactant, respectively. The ideal proportion of surfactant: co-surfactant (Smix) was chosen by constructing pseudoternary diagrams. The microemulsion formulations which proved to be stable after thermodynamic stability testing were further evaluated for physical characteristics. Selected formulations were evaluated for droplet size, zeta potential, polydispersity index, viscosity and % drug content. The results were suggestive that optimized microemulsion formulation (F2) was thermodynamically stable and clear having a droplet size of 74.29 nm and zeta potential of -18.44. In vitro dissolution study for optimized microemulsion was performed using a dialysis bag method and cumulative % drug release was determined. The result from the release study was indicative of improved solubility of Rosuvastatin calcium which may serve to boost up the oral bioavailability of drug.
Keywords:
Rosuvastatin calcium, Drug release, Oral delivery, MicroemulsionDOI
https://doi.org/10.25004/IJPSDR.2020.120106References
Mishra PR , Panda PK , Chowdar y K A . Evaluat ion of acute hypolipidemic activity of different plant Extracts in Triton Wr-1339 I induced hyperlipidemia in albino rats. 2011;934:925–934.
Austin MA, Breslow J, Hennekens CH, Buring JI, Willett WC, Krauss RM. Low density lipoprotein subclass patterns and risk of myocardial infarction. JAMA. 1988;260:1917–1921.
Murphy SL, Xu JQ, KD K. Deaths: Preliminary data for 2010. National vital statistics reports, Table B. Hyattsville, MD: National Center for Health Statistics; 2012.
Jorgensen T, Capewell S, Prescott E, Allender S, Sans S, Zdrojewski T. Population-level changes to promote cardiovascular health. Eur. J. Prev. Cardiol. 2013;20(3):409-421.
Curioni CC, Lourenco PM. Long-term weight loss after diet and exercise: a systematic review. Int J Obes (Lond). 2005;29:1168–1174.
Makris A, Foster GD. Dietary approaches to the treatment of obesity. Psychiatr Clin North Am. 2011;34:813–827.
Sever PS, Dahlof B, Poulter NR, et al. Prevention of coronary and stroke events with atorvastatin in hypertensive patients who have average or lower-than-average cholesterol concentrations, in the Anglo-Scandinavian Cardiac Outcomes Trial–Lipid Lowering Arm (ASCOT-LLA): a multicentre randomised controlled trial. Lancet. 2003;361:1149–1158.
Brugts JJ, Yetgin T, Hoeks SE, et al. The benefits of statins in people without established cardiovascular disease but with cardiovascular risk factors: meta-analysis of randomised controlled trials. BMJ. 2009;338:b2376.
Nissen SE, Nicholls SJ, Sipahi I, Tuzcu EM. Effect of very highintensity statin therapy on regression of coronary atherosclerosis: The ASTEROID trial J. Am. Med. Assoc. (2006);295(13):1556-1565
Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M. DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2017 Nov 8. doi: 10.1093/nar/gkx1037.
Akbari BV, Valaki BP, Mardiya VH, Akbari AK, Vidyasagar G. Enhancement of solubility and dissolution rate of rosuvastatin calcium by complexation with β cyclodextrin. Int J Pharm Biol Arch. 2011;2(1):511–520.
Callender SP, Mathews JA, Kobernyk K, Wettig SD. Microemulsion utility i n p harmaceuticals: I mplications f or m ulti-drug d elivery. International journal of pharmaceutics. 2017;526(1-2):425-442.
Garcia-Celma MJ, Azemar N, Pes MA, Solans C. Solubilization of antifungal drugs in water/POE (20) sorbitan monooleate/oil systems. Int J Pharm. 1994;105:77–81.
Silva AE, Barratt G, Chéron M, Egito EST, Development of oil-in water microemulsions for the oral delivery of Amphotericin B, Int. J. Pharm. 2013;454(2):641-648.
Sarciaux J, Acar L, Sado P. Using microemulsion formulations for oral drug delivery of therapeutic peptides. Int J Pharm. 1995; 120(2):127–136.
Singh G, Pai RS. Trans-resveratrol self-nano-emulsifying drug delivery system (SNEDDS) with enhanced bioavailability potential: optimization, pharmacokinetics and in situ single pass intestinal perfusion (SPIP) studies. Drug Delivery. 2015 May 19;22(4):522-30.
Liu R, Water-insoluble drug formulation, CRC press, 2008;2:p. 134.
Singh AK, Chaurasiya A, Awasthi A, Mishra G, Asati D, Khar RK, et al. Oral bioavailability enhancement of exemestane from selfmicroemulsifying drug delivery system [SMEDDS]. AAPS PharmSciTech. 2009;10(3):906–916.
Yin YM, Cui FD, Mu CF, Choi MK, Kim JS, Chung SJ, Shim CK, Kim DD. Docetaxel microemulsion for enhanced oral bioavailability: preparation and in-vitro and in vivo evaluation. J Control. Release. 2009;140:86-94.
Podlogar F, Gasperlin M, Tomsic M, Jamnik A, Rogac MB. Structural charac - terisation of water-Tween 40/Imwitor 308-isopropyl myristatemicro emulsions using different experimental methods. Int J Pharm. 2004;276(1-2):115-128.
Ali MS, Alam MS, Alam N, Siddiqui MR. Preparation, characterization and stability study of dutasteride loaded nanoemulsion for treatment of benign prostatic hypertrophy. Iran J Pharm Res. 2014; 13:1125–1140.
Ramesh Shah R, Shripal Magdum Ch, Shivagonda Patil Sh, Shanawaj Niakwade N. Preparation and Evaluation of Aceclofenac Topical Microemulsion. Iran J Pharm Res. 2010;9(1):5–11.
Srinivas C, Sagar VS. Enhancing the bioavailability of simvastatin using microemulsion drug delivery system. Asian J Pharm Clin Re 2012;15(4):134e139.
Moghimipour E., Salimi A., Eftekhari S. Design and characterization of microemulsion systems for naproxen. Adv. Pharm. Bull. 2013;3:63–71.
Alany RG, Tucker IG, Davies NM, Rades T. Characterizing colloidal structures of pseudo ternary phase diagrams formed by oil/water/amphiphile systems. Drug Dev Ind Pharm. 2001;27(1):31-38.
Kang BK, Lee JS, Chon SK, Jeong SY, Yuk SH, Khang G, Lee HB, Cho SH. Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int. J. Pharm. 2004;274:65-73.
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