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Xenobiotica
the fate of foreign compounds in biological systems
Volume 48, 2018 - Issue 12
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Animal Pharmacokinetics and Metabolism

Efficient brain uptake of piperine and its pharmacokinetics characterization after oral administration

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Pages 1249-1257 | Received 27 Sep 2017, Accepted 11 Nov 2017, Published online: 28 Nov 2017

References

  • Artursson P. (1990). Epithelial transport of drugs in cell culture. I: a model for studying the passive diffusion of drugs over intestinal absorptive (Caco-2) cells. J Pharm Sci 79:476–82
  • Asano T, Ishihara K, Morota T, et al. (2003). Permeability of the flavonoids liquiritigenin and its glycosides in licorice roots and davidigenin, a hydrogenated metabolite of liquiritigenin, using human intestinal cell line Caco-2. J Ethnopharmacol 89:285–9
  • Ball K, Bouzom F, Scherrmann JM, et al. (2012). Development of a physiologically based pharmacokinetic model for the rat central nervous system and determination of an in vitro-in vivo scaling methodology for the blood-brain barrier permeability of two transporter substrates, morphine and oxycodone. J Pharm Sci 101:4277–92
  • Bhardwaj RK, Glaeser H, Becquemont L, et al. (2002). Piperine, a major constituent of black pepper, inhibits human P-glycoprotein and CYP3A4. J Pharmacol Exp Ther 302:645–50
  • Bhat BG, Chandrasekhara N. (1986). Studies on the metabolism of piperine: absorption, tissue distribution and excretion of urinary conjugates in rats. Toxicology 40:83–92
  • Bhat BG, Chandrasekhara N. (1987). Metabolic disposition of piperine in the rat. Toxicology 44:99–106
  • Butt MS, Pasha I, Sultan MT, et al. (2013). Black pepper and health claims: a comprehensive treatise. Crit Rev Food Sci Nutr 53:875–86
  • Capasso R, Izzo AA, Borrelli F, et al. (2002). Effect of piperine, the active ingredient of black pepper, on intestinal secretion in mice. Life Sci 71:2311–17
  • Caron A, Lelong C, Bartels T, et al. (2015). Clinical and anatomic pathology effects of serial blood sampling in rat toxicology studies, using conventional or microsampling methods. Regul Toxicol Pharmacol 72:429–39
  • Chemistry RSO. (2013). Merck index. Cambridge, UK: Royal Society of Chemistry
  • Chonpathompikunlert P, Wattanathorn J, Muchimapura S. (2010). Piperine, the main alkaloid of Thai black pepper, protects against neurodegeneration and cognitive impairment in animal model of cognitive deficit like condition of Alzheimer’s disease. Food Chem Toxicol 48:798–802
  • Clinic PUPSHE . (1974). Initial experience of treating epilepsy by piperine. Beijing, China: Academic Journal of Peking University Health Science Center, 214–22
  • D’hooge R, Pei YQ, Raes A, et al. (1996). Anticonvulsant activity of piperine on seizures induced by excitatory amino acid receptor agonists. Arzneimittelforschung 46:557–60
  • Da Cruz GM, Felipe CF, Scorza FA, et al. (2013). Piperine decreases pilocarpine-induced convulsions by GABAergic mechanisms. Pharmacol Biochem Behav 104:144–53
  • Do MT, Kim HG, Choi JH, et al. (2013). Antitumor efficacy of piperine in the treatment of human HER2-overexpressing breast cancer cells. Food Chem 141:2591–9
  • Dong Y, Huihui Z, Li C. (2015). Piperine inhibit inflammation, alveolar bone loss and collagen fibers breakdown in a rat periodontitis model. J Periodontal Res 50:758–65
  • FDA . (2001). Guidance for industry: bioanalytical method validation. US Department of Health and Human Services. Food and Drug Administration, Center for Drug Evaluation and Research (CDER), Center for Veterinary Medicine (CV). Silver Spring, MD: FDA
  • Flückiger F, Hanbury D. (1879). Pharmacographia. In: A history of the principaldrugs of vegetable origin, met with in Great Britain and British India. 2nd ed. London: Macmillan, 663–9
  • Food and Drug Administration (FDA). (2005). Guidance for industry: estimating the maximum safe starting dose in initial clinical trials for therapeutics in adult healthy volunteers. Silver Spring, MD: Center for Drug Evaluation and Research (CDER)
  • Friden M, Bergstrom F, Wan H, et al. (2011). Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. Drug Metab Dispos 39:353–62
  • Friden M, Winiwarter S, Jerndal G, et al. (2009). Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. J Med Chem 52:6233–43
  • Gage GJ, Kipke DR, Shain W. (2012). Whole animal perfusion fixation for rodents. J Vis Exp 65: 3564
  • Goldstein A, Aronow L. (1960). The durations of action of thiopental and pentobarbital. J Pharmacol Exp Ther 128:1–6
  • Habgood MD, Sedgwick JE, Dziegielewska KM, Saunders NR. (1992). A developmentally regulated blood-cerebrospinal fluid transfer mechanism for albumin in immature rats. J Physiol 456:181–92
  • Hammarlund-Udenaes M, Friden M, Syvanen S, Gupta A. (2008). On the rate and extent of drug delivery to the brain. Pharm Res 25:1737–50
  • Han Y, Chin Tan TM, Lim LY. (2008). In vitro and in vivo evaluation of the effects of piperine on P-gp function and expression. Toxicol Appl Pharmacol 230:283–9
  • Houston JB. (1994). Utility of in vitro drug metabolism data in predicting in vivo metabolic clearance. Biochem Pharmacol 47:1469–79
  • Khajuria A, Zutshi U, Bedi KL. (1998). Permeability characteristics of piperine on oral absorption–an active alkaloid from peppers and a bioavailability enhancer. Indian J Exp Biol 36:46–50
  • Li C, Wang Q, Ren T, et al. (2016). Non-linear pharmacokinetics of piperine and its herb-drug interactions with docetaxel in Sprague-Dawley rats. J Pharm Biomed Anal 128:286–93
  • Lohmann C, Hüwel S, Galla HJ. (2002). Predicting blood-brain barrier permeability of drugs: evaluation of different in vitro assays. J Drug Target 10:263–76
  • Loryan I, Friden M, Hammarlund-Udenaes M. (2013). The brain slice method for studying drug distribution in the CNS. Fluids Barriers CNS 10:6
  • Loryan I, Hammarlund-Udenaes M. 2014. Drug discovery methods for studying brain drug delivery and distribution. In M. Hammarlund-Udenaes , E.C.M. De Lange , R.G. Thorne (eds.). Drug delivery to the brain: physiological concepts, methodologies and approaches. New York: Springer, 271–316
  • Lu C, Li P, Gallegos R, et al. (2006). Comparison of intrinsic clearance in liver microsomes and hepatocytes from rats and humans: evaluation of free fraction and uptake in hepatocytes. Drug Metab Dispos 34:1600–5
  • Ma Y, Tian M, Liu P, et al. (2014). Piperine effectively protects primary cultured atrial myocytes from oxidative damage in the infant rabbit model. Mol Med Rep 10:2627–32
  • Mao QQ, Huang Z, Zhong XM, et al. (2014). Piperine reverses chronic unpredictable mild stress-induced behavioral and biochemical alterations in rats. Cell Mol Neurobiol 34:403–8
  • Markowska M, Oberle R, Juzwin S, et al. (2001). Optimizing Caco-2 cell monolayers to increase throughput in drug intestinal absorption analysis. J Pharmacol Toxicol Methods 46:51–5
  • Moghadamnia AA, Zangoori V, Zargar-Nattaj SS, et al. (2010). Effect of breastfeeding piperine on the learning of offspring mice: interaction with caffeine and diazepam. J Exp Pharmacol 2:111–20
  • Okwute SK, Egharevba HO. (2013). Piperine-type amides: review of the chemical and biological characteristics. Int J Chem 5:99
  • Priprem A, Chonpathompikunlert P, Sutthiparinyanont S, Wattanathorn J. (2011). Antidepressant and cognitive activities of intranasal piperine-encapsulated liposomes. Adv Biosci Biotechnol 2:108
  • Promod Kumar Sahu GS. (2014). Pharmacokinetic study of piperine in Wistar rats after oral and intravenous administration. Int J Drug Deliv 6:82
  • Shao B, Cui C, Ji H, et al. (2015). Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems: in vitro, in vivo and in situ intestinal permeability studies. Drug Deliv 22:740–7
  • Singh J, Dubey RK, Atal CK. (1986). Piperine-mediated inhibition of glucuronidation activity in isolated epithelial cells of the guinea-pig small intestine: evidence that piperine lowers the endogeneous UDP-glucuronic acid content. J Pharmacol Exp Ther 236:488–93
  • Sumit Roy AG, Himanshu C, Anup KM, et al (2012). Pharmacokinetic study of Piperine in mice plasma after orally and intravenous administration. Int J Drug Deliv 4:107
  • Sun L, Stenken JA. (2003). Improving microdialysis extraction efficiency of lipophilic eicosanoids. J Pharm Biomed Anal 33:1059–71
  • Tsuji A, Terasaki T, Takabatake Y, et al. (1992). P-glycoprotein as the drug efflux pump in primary cultured bovine brain capillary endothelial cells. Life Sci 51:1427–37
  • Van Breemen RB, Li Y. (2005). Caco-2 cell permeability assays to measure drug absorption. Expert Opin Drug Metab Toxicol 1:175–85
  • Van Liempd S, Morrison D, Sysmans L, et al. (2011). Development and validation of a higher-throughput equilibrium dialysis assay for plasma protein binding. J Lab Autom 16:56–67
  • Yusuf M, Khan M, Khan RA, Ahmed B. (2012). Preparation, characterization, in vivo and biochemical evaluation of brain targeted Piperine solid lipid nanoparticles in an experimentally induced Alzheimer’s disease model. J Drug Target 21:300–11
  • Zapata A, Chefer VI, Shippenberg TS. (2009). Microdialysis in rodents. Curr Protoc Neurosci 7:7.2
  • Zhang L, Lin G, Chang Q, Zuo Z. (2005). Role of intestinal first-pass metabolism of baicalein in its absorption process. Pharm Res 22:1050–8
  • Zhong Feng GJ. (2010). Pharmacokinetics of piperine from piperlongum in rats. Pharmacol Clin Chinese Materia Medica 26:34--6

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