Enhanced bioavailability and hypolipidemic activity of Simvastatin formulations by particle size engineering: Physicochemical aspects and in vivo investigations

Biochemical Engineering Journal

Volumn 79, Issue , 2013, Pages 221-229

  Chavhan, Sandip ^a   Joshi, Garima ^a   Petkar, Kailash ^a   Sawant, Krutika ^a  

^a M S UNIVERSITY OF BARODA   (India)

Author keywords

Absorption; Biomedical; Kinetic parameters; Nanosuspension; Optimization; Supercritical antisolvent process

Indexed keywords

BIOMEDICAL; NANO-SUSPENSIONS; PARTICLE SIZE ENGINEERING; PHYSICOCHEMICAL PROPERTY; POORLY WATER-SOLUBLE DRUGS; SUPERCRITICAL ANTISOLVENT PROCESS; SUPERCRITICAL ANTISOLVENTS; SURFACTANT CONCENTRATIONS;

ABSORPTION; BIOCHEMISTRY; CARBON DIOXIDE; KINETIC PARAMETERS; MILLING (MACHINING); OPTIMIZATION; PARTICLE SIZE; RATS; SOLUBILITY;

SUPERCRITICAL FLUID EXTRACTION;

CHOLESTEROL; SIMVASTATIN; SURFACTANT; TRIACYLGLYCEROL;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CHOLESTEROL BLOOD LEVEL; CONTROLLED STUDY; CRYSTAL STRUCTURE; DEPENDENT VARIABLE; DISSOLUTION; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG SCREENING; DRUG SOLUBILITY; FACTORIAL DESIGN; HYPERLIPIDEMIA; HYPOLIPEMIA; HYPOLIPIDEMIC ACTIVITY; IN VIVO STUDY; NONHUMAN; PARTICLE SIZE; PHARMACEUTICAL ENGINEERING; PHARMACODYNAMICS; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; PROCESS OPTIMIZATION; RAT; TRIACYLGLYCEROL BLOOD LEVEL;

EID: 84883748317     PISSN: 1369703X     EISSN: 1873295X     Source Type: Journal    
DOI: 10.1016/j.bej.2013.08.007     Document Type: Article

References (32)

1. Murtaza G. Solubility enhancement of Simvastatin: a review. Acta Pol. Pharm. 2012, 69:581-590.
2. Yamamura S., Rogers L.A. Characterization and dissolution behaviour of nifedipine and phosphatidylcholine binary systems. Int. J. Pharm. 1996, 130:65-73.
3. Rao M., Mandage Y., Thanki1 K., Bhise S. Dissolution improvement of simvastatin by surface solid dispersion technology. Dissolut. Technol. 2010, 27-34.
4. Kakran M., Sahoo N.G., Li L., Judeh Z., Wang Y., Chong K., Loh L. Fabrication of drug nanoparticles by evaporative precipitation of nanosuspension. Int. J. Pharm. 2010, 383:285-292.
5. Hojjati M., Yamini Y., Khajeh M., Vatanara A. Solubility of some statin drugs in supercritical carbon dioxide and representing the solute solubility data with several density-based correlations. J. Supercrit. Fluids 2007, 41:187-194.
6. Schachter M. Chemical, pharmacokinetic and pharmacodynamic properties of statins: an update. Fundam. Clin. Pharmacol. 2005, 19:117-125.
7. Cheng H., et al. Evaluation of sustained/controlled-release dosage forms of 3-hydroxy-3- methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors in dogs and humans. Pharm. Res. 1993, 10:1683-1687.
8. Ambike A.A., Mahadik K.R., Paradkar A. Spray-dried amorphous solid dispersions of Simvastatin, A low Tg drug: in vitro and in vivo evaluations. Pharm. Res. 2005, 22:990-998.
9. Ungaro F., Giovino C., Catanzano O., Miro A., Mele A., Quaglia F., Rotonda M.I.L. Use of cyclodextrins as solubilizing agents for simvastatin: effect of hydroxypropyl-β-cyclodextrin on lactone/hydroxyacid aqueous equilibrium. Int. J. Pharm. 2011, 404:49-56.
10. Jun S.W., Kim M., Kim J., Park H.J., Lee S., Woo J., Hwang S.J. Preparation and characterization of simvastatin/hydroxypropyl-β-cyclodextrin inclusion complex using supercritical antisolvent (simvastatin SAS product) process. Eur. J. Pharm. Biopharm. 2007, 66:413-421.
11. Kang B., Lee J.S., Chon S.K., Jeong S.Y., Yuk S.H., Khang G., Lee H.B., Cho S.H. Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int. J. Pharm. 2004, 274:65-73.
12. Meng J., Zheng L. Application of mixture experimental design to simvastatin apparent solubility predictions in the microemulsifion formed by self-microemulsifying. Drug Dev. Ind. Pharm. 2007, 33:927-931.
13. Kulhari H., Pooja D., Prajapati S.K., Chauhan A.S. Performance evaluation of PAMAM dendrimer based Simvastatin formulations. Int. J. Pharm. 2011, 405:203-209.
14. Zhang Z., Bu H., Gao Z., Huang Y., Gao F., Li Y. The characteristics and mechanism of simvastatin loaded lipid nanoparticles to increase oral bioavailability in rats. Int. J. Pharm. 2010, 394:147-153.
15. Pardeike J., Muller R.H. Nanosuspensions: a promising formulation for the new phospholipase A2 inhibitor PX-18. Int. J. Pharm. 2010, 391:322-329.
16. Cerdeira A.M., Mazzotti M., Gander B. Miconazole nanosuspensions: influence of formulation variables on particle size reduction and physical stability. Int. J. Pharm. 2010, 383:285-292.
17. 2 antisolvent with enhanced mass transfer. Int. J. Pharm. 2001, 228:19-31.
18. Eerdenbrugh B.V., Froyen L., Martens J.A., Blaton N., Augustijns P., Brewster M. Characterization of physico-chemical properties and pharmaceutical performance of sucrose co-freeze-dried solid nanoparticulate powders of the anti-HIV agent loviride prepared by media milling. Int. J. Pharm. 2007, 338:198-206.
19. Adinarayana K., Ellaiah P. Response surface optimization of the critical medium components for the production of alkaline protease by a newly isolated Bacillus sp. J. Pharm. Pharm. Sci. 2002, 5:281-287.
20. Calvo P., Vila-Jato J.L., Alonso M.J. Comparative in vitro evaluation of several colloidal systems, nanoparticles, nanocapsules and nanoemulsions as ocular drug carrier. J. Pharm. Sci. 1996, 85:530-536.
21. Ali H., Shirode A., Sylvester P., Nazzal S. Preparation, characterization, and anticancer effects of simvastatin-tocotrienol lipid nanoparticles. Int. J. Pharm. 2010, 389:223-231.
22. Carlucci G., Mazzeo P., Biordi L., Bologna M. Simultaneous determination of simvastatin and its hydroxyl acid form in human plasma by high-performance liquid chromatography with UV detection. J. Pharm. Biomed. Anal. 1992, 10:693-697.
23. Palla B.J., Shah D.O. Stabilization of high ionic strength slurries using surfactant mixtures: molecular factors that determine optimal stability. J. Colloid Interface Sci. 2002, 256:143-152.
24. Merisko-Liversidge E., Liversidge G.G., Cooper E.R. Nanosizing: a formulation approach for poorly-water-soluble compounds. Eur. J. Pharm. Sci. 2003, 18:113-120.
25. Ali H.S., York P., Blagden N. Preparation of hydrocortisone NS through a bottom-up nanoprecipitation technique using microfluidic reactors. Int. J. Pharm. 2009, 375:107-113.
26. Muller R.H., Jacobs C. Buparvaquone mucoadhesive nanosuspension: preparation, optimisation and long-term stability. Int. J. Pharm. 2002, 237:151-161.
27. Kamiya S., Kurita T., Miyagishima A., Arakawa M. Preparation of griseofulvin nanoparticle suspension by high-pressure homogenization and preservation of the suspension with saccharides and sugar alcohols. Drug Dev. Ind. Pharm. 2009, 35(8):1022-1028.
28. Kocbek P., Baumgartner S., Kristl J. Preparation and evaluation of nanosuspensions for enhancing the dissolution of poorly soluble drugs. Int. J. Pharm. 2006, 312:179-186.
29. Muller R.H., Jacobs C., Kayser O. Nanosuspensions as particulate drug formulations in therapy. Rationale for development and what we can expect for the future. Adv. Drug Delivery Rev. 2001, 47:3-19.
30. Costa P., Sousa Lobo J.M. Modeling and comparison of dissolution profiles. Eur. J. Pharm. Sci. 2001, 13:123-133.
31. Company Literature on ZOCOR\(Simvastatin) Tablets, Merck and Co., Inc., NJ, USA, pp. 1Y2, 6.
32. Xia D., Quan P., Piao H., Sun S., Yin Y., Cui F. Preparation of stable nitrendipine nanosuspensions using the precipitation-ultrasonication method for enhancement of dissolution and oral bioavailability. Eur. J. Pharm. Sci. 2010, 40:325-334.