678
Views
24
CrossRef citations to date
0
Altmetric
Research Articles

Improved oral bioavailability and therapeutic efficacy of dabigatran etexilate via Soluplus-TPGS binary mixed micelles system

, , , , &
Pages 687-697 | Received 06 Oct 2016, Accepted 23 Dec 2016, Published online: 23 Jan 2017

References

  • Hankey GJ, Eikelboom JW. Dabigatran etexilate. A new oral thrombin inhibitor. Circulation 2011;123:1436–50.
  • Huisman MV, Lip GY, Diener H-C, et al. Dabigatran etexilate for stroke prevention in patients with atrial fibrillation: resolving uncertainties in routine practice. Thromb Haemost 2012;107:838.
  • Li Y-Z, Gong G-Q, Yang W-H, et al. Antithrombotic activity of HY023016, a novel dabigatran prodrug evaluated in animal thrombosis models. Thromb Res 2013;131:425–35.
  • Remko M. Molecular structure, lipophilicity, solubility, absorption, and polar surface area of novel anticoagulant agents. J Mol Struct THEOCHEM 2009;916:76–85.
  • Connolly SJ, Ezekowitz MD, Yusuf S, et al. Dabigatran versus warfarin in patients with atrial fibrillation. N Engl J Med 2009;361:1139–51.
  • Lu Y, Park K. Polymeric micelles and alternative nanonized delivery vehicles for poorly soluble drugs. Int J Pharm 2013;453:198–214.
  • Saxena V, Hussain MD. Poloxamer 407/TPGS mixed micelles for delivery of gambogic acid to breast and multidrug-resistant cancer. Int J Nanomedicine 2012;7:713.
  • Jin X, Zhou B, Xue L, San W. Soluplus(®) micelles as a potential drug delivery system for reversal of resistant tumor. Biomed Pharmacother 2015;69:388–95.
  • Mu L, Seow P. Application of TPGS in polymeric nanoparticulate drug delivery system. Colloids Surf B Biointerfaces 2006;47:90–7.
  • Duan Y, Zhang B, Chu L, et al. Evaluation in vitro and in vivo of curcumin-loaded mPEG-PLA/TPGS mixed micelles for oral administration. Colloids Surf B Biointerfaces 2016;141:345–54.
  • Zhang Z, Ma L, Jiang S, et al. A self-assembled nanocarrier loading teniposide improves the oral delivery and drug concentration in tumor. J Control Release 2013;166:30–7.
  • Dou J, Zhang H, Liu X, et al. Preparation and evaluation in vitro and in vivo of docetaxel loaded mixed micelles for oral administration. Colloids Surf B Biointerfaces 2014;114:20–7.
  • Wei Z, Hao J, Yuan S, et al. Paclitaxel-loaded Pluronic P123/F127 mixed polymeric micelles: formulation, optimization and in vitro characterization. Int J Pharm 2009;376:176–85.
  • Zeng N, Gao X, Hu Q, et al. Lipid-based liquid crystalline nanoparticles as oral drug delivery vehicles for poorly water-soluble drugs: cellular interaction and in vivo absorption. Int J Nanomedicine 2012;7:3703–18.
  • Dian L, Yu E, Chen X, et al. Enhancing oral bioavailability of quercetin using novel soluplus polymeric micelles. Nanoscale Res Lett 2014;9:1–11.
  • Zhang Z, Gao F, Bu H, et al. Solid lipid nanoparticles loading candesartan cilexetil enhance oral bioavailability: in vitro characteristics and absorption mechanism in rats. Nanomedicine 2012;8:740–7.
  • Kuma H, Nagashima R, Hatae H, et al. Beneficial effect of EPA (20:5 n-3 PUFA) on preventing venous thromboembolism: a rat tail thrombosis model experiment. Thromb Res 2013;131:107–8.
  • Xu J, Du M, Yang X, et al. Thrombolytic effects in vivo of nattokinase in a carrageenan-induced rat model of thrombosis. Acta Haematol 2014;132:247–53.
  • Jones M-C, Ranger M, Leroux J-C. pH-sensitive unimolecular polymeric micelles: synthesis of a novel drug carrier. Bioconjug Chem 2003;14:774–81.
  • Derakhshandeh K, Soheili M, Dadashzadeh S, Saghiri R. Preparation and in vitro characterization of 9-nitrocamptothecin-loaded long circulating nanoparticles for delivery in cancer patients. Int J Nanomedicine 2010;5:1–9.
  • Shoaib MH, Tazeen J, Merchant HA, Yousuf RI. Evaluation of drug release kinetics from ibuprofen matrix tablets using HPMC. Pak J Pharm Sci 2006;19:119–24.
  • Mo R, Jin X, Li N, et al. The mechanism of enhancement on oral absorption of paclitaxel by N-octyl-O-sulfate chitosan micelles. Biomaterials 2011;32:4609–20.
  • Ishiguro N, Kishimoto W, Volz A, et al. Impact of endogenous esterase activity on in vitro p-glycoprotein profiling of dabigatran etexilate in Caco-2 monolayers. Drug Metab Dispos 2014;42:250–6.
  • Ohura K, Sakamoto H, Ninomiya S-i, Imai T. Development of a novel system for estimating human intestinal absorption using Caco-2 cells in the absence of esterase activity. Drug Metabo Dispos 2010;38:323–31.
  • Mentlein R, Rix-Matzen H, Heymann E. Subcellular localization of non-specific carboxylesterases, acylcarnitine hydrolase, monoacylglycerol lipase and palmitoyl-CoA hydrolase in rat liver. Biochim Biophys Acta 1988;964:319–28.
  • Block W, Arndt R. Chromatographic study on the specificity of bis-p-nitrophenylphosphate in vivo. Identification of labelled proteins of rat liver after intravenous injection of bis-p-nitro[14C]phenylphosphate as carboxylesterases and amidases. Biochim Biophys Acta 1978;524:85–93.
  • Duncan R, Richardson SC. Endocytosis and intracellular trafficking as gateways for nanomedicine delivery: opportunities and challenges. Mol Pharm 2012;9:2380–402.
  • Härtter S, Sennewald R, Nehmiz G, Reilly P. Oral bioavailability of dabigatran etexilate (Pradaxa®) after co-medication with verapamil in healthy subjects. Br J Clin Pharmacol 2013;75:1053–62.
  • Mayor S, Pagano RE. Pathways of clathrin-independent endocytosis. Nat Rev Mol Cell Biol 2007;8:603–12.
  • Abramov E, Cassiola F, Schwob O, et al. Cellular mechanism of oral absorption of solidified polymer micelles. Nanomedicine 2015;11:1993–2002.
  • Roger E, Lagarce F, Garcion E, Benoit J-P. Biopharmaceutical parameters to consider in order to alter the fate of nanocarriers after oral delivery. Nanomedicine 2010;5:287–306.
  • Lind ML, Jacobsen J, Holm R, Müllertz A. Intestinal lymphatic transport of halofantrine in rats assessed using a chylomicron flow blocking approach: the influence of polysorbate 60 and 80. Eur J Pharm Sci 2008;35:211–18.
  • Fan Z, Wu J, Fang X, Sha X. A new function of vitamin E-TPGS in the intestinal lymphatic transport of lipophilic drugs: enhancing the secretion of chylomicrons. Int J Pharm 2013;445:141–7.
  • Linn M, Collnot E-M, Djuric D, et al. Soluplus® as an effective absorption enhancer of poorly soluble drugs in vitro and in vivo. Eur J Pharm Sci 2012;45:336–43.
  • Panwar P, Pandey B, Lakhera P, Singh K. Preparation, characterization, and in vitro release study of albendazole-encapsulated nanosize liposomes. Int J Nanomedicine 2010;5:101–8.
  • Ho P-Y, Yeh T-K, Yao H-T, et al. Enhanced oral bioavailability of paclitaxel by D-alpha-tocopheryl polyethylene glycol 400 succinate in mice. Int J Pharm 2008;359:174–81.
  • Collnot E-M, Baldes C, Wempe MF, et al. Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity. Mol Pharm 2007;4:465–74.
  • Vasir JK, Tambwekar K, Garg S. Bioadhesive microspheres as a controlled drug delivery system. Int J Pharm 2003;255:13–32.
  • Simkhada JR, Cho SS, Mander P, et al. Purification, biochemical properties and antithrombotic effect of a novel Streptomyces enzyme on carrageenan-induced mice tail thrombosis model. Thromb Res 2012;129:176–82.
  • Stangier J, Stähle H, Rathgen K, et al. Pharmacokinetics and pharmacodynamics of dabigatran etexilate, an oral direct thrombin inhibitor, with coadministration of digoxin. J Clin Pharmacol 2012;52:243–50.
  • Wienen W, Stassen J-M, Priepke H, et al. Effects of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate, on thrombus formation and bleeding time in rats. Thromb Haemost 2007;98:333–8.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.