A Systematic Review of Piperine as a Bioavailability Enhancer
Abstract
Drug oral absorption is a crucial concern, particularly when the medication is costly, poorly bioavailable, and administered for extended periods of time. Chemical substances known as "bioenhancers" are those that, when combined with pharmaceuticals, increase their bioavailability without having a synergistic impact on the drug itself. Toxicity, expense, poor bioavailability, and long-term medication administration all contribute to the need for bioenhancers, which aid in solving the majority of these issues. Piperine, also known as 1-peperoyl piperidine, is an aromatic alkaloid produced by the Piper species. Piperine alters the lipid milieu and membrane dynamics at the site of absorption to improve permeability. The molecular nature of piperine makes it appropriate for inhibiting enzymes. By blocking several metabolising enzymes, it increases the bioavailability of many medications, including carbamazepine, curcumin, ciprofloxacin, ampicillin, metronidazole, oxytetracycline, and many more. As a result, piperine, a potent inhibitor of medication metabolism, effectively increases absorption. The mechanism, metabolic inhibition, influence of structural alterations on activity, and medications that are bioenhanced by piperine are all explored in the review that follows. It offers insight into the use of piperine as a useful bioenhancer and the advantages of a bioenhanced drug formulation over one without one. Bioavailability enhancers are typically plant-based molecules that support the biological activity, bioavailability, or uptake of drugs in combination therapy. This review article finishes with discussing piperine's capacity to increase bioavailability.
Keywords: Bioenhancers, Piperine, Oral absorption, Alkaloid.
Keywords:
Bioenhancers, Piperine, Oral absorption, AlkaloidDOI
https://doi.org/10.22270/jddt.v13i4.5781References
British Pharmacopoeia. Great Britain: The Department of Health, Social Services and Public Safety, 2007.
Brahmankar DB, Jaiswal S. Biopharmaceutics and Pharmacokinetics: A Treatise. Edn 1, Vallabh Prakashan, 1995, 24-26.
Drabu S, Khatri S, Babu S, Lohani P. Use of herbal bioenhancers to increase the bioavailability of drugs. Research Journal of Pharmaceutical, Biological and Chemical Sciences 2011; 2(4):108-119.
Patil UM, Singh A, Chakraborty AK. Role of piperine as a bioavailability enhancer. International Journal of Recent Advances in Pharmaceutical Research 2011; 1(4):16-23.
Dudhatra GB, Modi SK, Awale MM, Patel HB, Modi CM, Kumar A et al. A Comprehensive review on Pharmacotherapeutics of herbal bioenhancers. Scientific World Journal 2012; 1-33. https://doi.org/10.1100/2012/637953
Atal N, Bedi KL. Bioenhancers: Revolutionary concept to market. The Journal of Ayurveda and Integrative Medicine 2010; 1(2):96-99. https://doi.org/10.4103/0975-9476.65073
Qazi GN, et al. Council of Scientific and Industrial Research. Bioavailability / Bioefficacy Enhancing Activity of Cuminiumcyminum and Extracts and Fractions Thereof. US Patent 52873; 2004:Mar18.
Johri RK, Zutshi U. An Ayurvedic formulation 'Trikatu' and its constituents. Journal of Ethnopharmacology1992; 37:85-91. https://doi.org/10.1016/0378-8741(92)90067-2
Zutshi U, et al. A process for preparation of pharmaceutical combination with enhanced activity for treatment of tuberculosis and leprosy. Indian Patent No 1232/DEL89.Date of Pulication1989.
Lee KW, Everts H, Beynen AC. Essential oils in broiler nutrition. International Journal of Poultry Science 2004; 3: 738-752. https://doi.org/10.3923/ijps.2004.738.752
Annamalai AR, Manavlan R. Trikatu- A bioavailability enhancer. Indian Drugs 1989; 27: 595-604.
Johri RK, Thusu N, Khajuria A, Zutshi U. Piperine-mediated changes in the permeability of rat intestinal epithelial cells: the status of γ-glutamyl transpeptidase activity, uptake of amino acids and lipid peroxidation. Biochemical Pharmacology 1992; 43: 1401-1407. https://doi.org/10.1016/0006-2952(92)90195-O
Khajuria A, Thusu N, Zutshi U. Piperine modulates permeability characteristics of intestine by inducing alterations in membrane dynamics: Influence on brush border membrane fluidity, ultrastructure and enzyme kinetics. Phytomedicine 2002; 9: 224-231 https://doi.org/10.1078/0944-7113-00114
Stecher PG. The Merck index an encyclopedia of chemicals and drugs. 7th ed. Rahway: Merck & Co. 1960:823. https://doi.org/10.1097/00010694-196007000-00014
Merck Index, 11th Edition, 7442.
Shinde SA, Chavhan SA, Sapkal SB, Darakhe RA. Potential of Piperine as a bioavailability enhancer. International Journal of Biology Research
; 4(2) 03-06.
Bhardwaj RK, Glaeser H, Becquemont L, Klotz U, Gupta SK, Fromm MF. Piperine, a major constituent of black pepper, inhibits human P-glycoprotein and CYP3A4. The Journal of Pharmacology and Experimental Therapeutics 2002; 302 (2): 645-50. https://doi.org/10.1124/jpet.102.034728
Shoba G, Joy D, Joseph T, Majeed M, Rajendran R, Srinivas PS. Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers. Planta Medica 1998; 64 (4): 353-6. https://doi.org/10.1055/s-2006-957450
Faas L, Venkatasamy R, Hider RC, Young AR, Soumyanath, A. In vivo evaluation of piperine and synthetic analogues as potential treatments for vitiligo using a sparsely pigmented mouse model. British Journal of Dermatology 2008; 158 (5): 941-50. https://doi.org/10.1111/j.1365-2133.2008.08464.x
Pattanaik S, Hota D, Prabhakar S, Kharbanda P, Pandhi P. Pharmacokinetic interaction of single dose of piperine with steadystate carbamazepine in epilepsy patients. Phytotherapy Research 2009; 23(9):1281-86. https://doi.org/10.1002/ptr.2676
Jin MJ, Han HK. Effect of piperine, a major component of black pepper, on the intestinal absorption of fexofenadine and its implication on food-drug interaction. Journal of Food Science 2010; 75(3):H93-96. https://doi.org/10.1111/j.1750-3841.2010.01542.x
Janakiraman K and Manavalan R. Compatibility and stability studies of ampicillin trihydrate and piperine mixture. International Journal of Pharmaceutical Sciences and Research 2011; 2(5):1176-81.
Shoba G, et al. Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers. Planta Medica 1998; 64(4):353-56. https://doi.org/10.1055/s-2006-957450
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