Supersaturated self-nanoemulsifying drug delivery systems (Super-SNEDDS) enhance the bioavailability of the poorly water-soluble drug simvastatin in dogs

AAPS Journal

Volumn 15, Issue 1, 2013, Pages 219-227

  Thomas, Nicky ^a   Holm, René ^b   Garmer, Mats ^b   Karlsson, Jens Jakob ^b   Müllertz, Anette ^c,d   Rades, Thomas ^a,c  

^a UNIVERSITY OF OTAGO   (New Zealand)

^b H LUNDBECK A S   (Denmark)

^c UNIVERSITY OF COPENHAGEN   (Denmark)

^d UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

bioavailability; in vitro digestion; in vitro lipolysis; simvastatin; supersaturated self nanoemusifying drug delivery systems (super SNEDDS) poorly soluble drugs

Indexed keywords

DRUG METABOLITE; DRUG METABOLIZING ENZYME; HALOFANTRINE; MEVINOLIN; SIMVASTATIN; SIMVASTATIN ACID; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED RELEASE FORMULATION; CONTROLLED STUDY; COOLING; DOG; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CAPSULE; DRUG DELIVERY SYSTEM; DRUG ELIMINATION; DRUG FORMULATION; DRUG HALF LIFE; DRUG SOLUBILITY; DRUG STABILITY; HEARING; IN VITRO STUDY; IN VIVO STUDY; LIPOLYSIS; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; SELF NANOEMULSIFYING DRUG DELIVERY SYSTEM; SINGLE DRUG DOSE; SMALL INTESTINE ABSORPTION; SUPERSATURATED SELF NANOEMULSIFYING DRUG DELIVERY SYSTEM; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; BIOLOGICAL AVAILABILITY; DOGS; DRUG DELIVERY SYSTEMS; DRUG STABILITY; EMULSIONS; HYDROXYMETHYLGLUTARYL-COA REDUCTASE INHIBITORS; NANOPARTICLES; SIMVASTATIN; SOLUBILITY; X-RAY DIFFRACTION;

EID: 84871970245     PISSN: 15507416     EISSN: None     Source Type: Journal    
DOI: 10.1208/s12248-012-9433-7     Document Type: Article

References (30)

1. Chakraborty S, Shukla D, Mishra B, Singh S. Lipid - an emerging platform for oral delivery of drugs with poor bioavailability. Eur J Pharm Biopharm. 2009;73(1):1-70.
2. Fahr A, Liu X. Drug delivery strategies for poorly water-soluble drugs. Expert Opin Drug Deliv. 2007;4(4):403-16. (Pubitemid 47249138)
3. Hauss DH. Oral lipid-based formulations. Adv Drug Deliv Rev. 2007;59(7):667-76. (Pubitemid 47285409)
4. Pouton CW, Porter CJH. Formulation of lipid-based delivery systems for oral administration: materials, methods and strategies. Adv Drug Deliv Rev. 2008;60(6):625-37.
5. Humberstone AJ, Charman WN. Lipid-based vehicles for the oral delivery of poorly water soluble drugs. Adv Drug Deliv Rev. 1997;25(1):103-28.
6. Anton N, Vandamme T. Nano-emulsions and micro-emulsions: clarifications of the critical differences. Pharm Res. 2011;28(5):978-85.
7. Kovarik JM, Mueller EA, Van Bree JB, Tetzloff W, Kutz K. Reduced inter- and intraindividual variability in cyclosporine pharmacokinetics from a microemulsion formulation. J Pharm Sci. 1994;83(3):444-6. (Pubitemid 24224228)
8. Mueller EA, Kovarik JM, van Bree JB, Grevel J, Lücker PW, Kutz K. Influence of a fat-rich meal on the pharmacokinetics of a new oral formulation of cyclosporine in a crossover comparison with the market formulation. Pharm Res. 1994;11(1):151-5. (Pubitemid 24040779)
9. Mueller EA, Kovarik JM, van Bree JB, Tetzloff W, Grevel J, Kutz K. Improved dose linearity of cyclosporine pharmacokinetics from a microemulsion formulation. Pharm Res. 1994;11(2):301-4. (Pubitemid 24076228)
10. Fatouros DG, Karpf DM, Nielsen FS, Müllertz A. Clinical studies with oral lipid based formulations of poorly soluble compounds. Ther Clin Risk Manag. 2007;3(4):591-604. (Pubitemid 47496964)
11. Porter CJH, Trevaskis NL, Charman WN. Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs. Nat Rev Drug Discov. 2007;6(March):231-48. (Pubitemid 46344627)
12. Strickley RG. Solubilizing excipients in oral and injectable formulations. Pharm Res. 2004;21(2):201-30. (Pubitemid 38221966)
13. Rane SS, Anderson BD. What determines drug solubility in lipid vehicles: is it predictable? Adv Drug Deliv Rev. 2008;60(6):638-56.
14. Thi TD, Van Speybroeck M, Barillaro V, Martens J, Annaert P, Augustijns P, et al. Formulate-ability of ten compounds with different physicochemical profiles in SMEDDS. Eur J Pharm Sci. 2009;38(5):479-88.
15. Christensen J, Schultz K, Mollgard B, Kristensen HG, Müllertz A. Solubilisation of poorly water-soluble drugs during in vitro lipolysis of medium- and long-chain triacylglycerols. Eur J Pharm Sci. 2004;23(3):287-96. (Pubitemid 39369884)
16. Kaukonen AM, Boyd BJ, Porter CJH, Charman WN. Drug solubilization behavior during in vitro digestion of simple triglyceride lipid solution formulations. Pharm Res. 2004;21(2):245-53. (Pubitemid 38221969)
17. Sassene PJ, Knopp MM, Hesselkilde JZ, Koradia V, Larsen A, Rades T, et al. Precipitation of a poorly soluble model drug during in vitro lipolysis: characterization and dissolution of the precipitate. J Pharm Sci. 2010;99(12):4982-91.
18. Thomas N, Holm R, Müllertz A, Rades T. In vitro and in vivo performance of novel supersaturated self-nanoemulsifying drug delivery systems (super-SNEDDS). J Control Release. 2012;160(1):25-32.
19. Tubic-Grozdanis M, Hilfinger J, Amidon G, Kim J, Kijek P, Staubach P, et al. Pharmacokinetics of the CYP 3A substrate simvastatin following administration of delayed versus immediate release oral dosage forms. Pharm Res. 2008;25(7):1591-600.
20. Pedersen TR, Tobert JA. Simvastatin: a review. Expert Opin Pharmacother. 2004;5(12):2583-96. (Pubitemid 39646520)
21. Hamelin BA, Turgeon J. Hydrophilicity/lipophilicity: relevance for the pharmacology and clinical effects of HMG-CoA reductase inhibitors. Trends Pharmacol Sci. 1998;19(1):26-37. (Pubitemid 28094090)
22. Serajuddin ATM, Ranadive SA, Mahoney EM. Relative lipophilicities, solubilities, and structure-pharmacological considerations of 3-hydroxy-3-methylglutaryl-coenzyme a (HMG-COA) reductase inhibitors pravastatin, lovastatin, mevastatin, and simvastatin. J Pharm Sci. 1991;80(9):830-4.
23. Kang BK, Lee JS, Chon SK, Jeong SY, Yuk SH, Khang G, et al. Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int J Pharm. 2004;274(1-2):65-73. (Pubitemid 38457007)
24. 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(1-2):147-53.
25. Thomas N, Müllertz A, Graf A, Rades T. Influence of lipid composition and drug load on the in vitro performance of self-nanoemulsifying drug delivery systems. J Pharm Sci. 2012;101(5):1721-31.
26. Zangenberg NH, Müllertz A, Kristensen HG, Hovgaard L. A dynamic in vitro lipolysis model: I. Controlling the rate of lipolysis by continuous addition of calcium. Eur J Pharm Sci. 2001;14(2):115-22. (Pubitemid 32737533)
27. Zangenberg NH, Müllertz A, Kristensen HG, Hovgaard L. A dynamic in vitro lipolysis model. II: Evaluation of the model. Eur J Pharm Sci. 2001;14(3):237-44. (Pubitemid 32884320)
28. Shitara Y, Sugiyama Y. Pharmacokinetic and pharmacodynamic alterations of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors: drug-drug interactions and interindividual differences in transporter and metabolic enzyme functions. Pharmacol Ther. 2006;112(1):71-105. (Pubitemid 44301483)
29. Sawada T, Sako K, Yoshihara K, Nakamura K, Yokohama S, Hayashi M. Timed-release formulation to avoid drug-drug interaction between diltiazem and midazolam. J Pharm Sci. 2003;92(4):790-7. (Pubitemid 36396995)
30. McKinnon RA, McManus ME. Localization of cytochromes P450 in human tissues: implications for chemical toxicity. Pathol (Phila). 1996;28(2):148-55. (Pubitemid 27182758)