The effect of polysorbate 20 and polysorbate 80 on the solubility of quercetin
All claims expressed in this article are solely those of the authors and do not necessarily represent those of their affiliated organizations, or those of the publisher, the editors and the reviewers. Any product that may be evaluated in this article or claim that may be made by its manufacturer is not guaranteed or endorsed by the publisher.
Background: Quercetin acts as an antioxidant, anti-inflammatory, wound healing, and anti-aging so quercetin can be used as a topical preparation. However, it has low solubility in water at 0.01 mg/ml at 25°C. Increasing the solubility of quercetin in water was done by the addition of surfactants.
Objective: This study compared the solubility of quercetin in Polysorbate 20 (P20) and Polysorbate 80 (P80) in a citrate buffer medium pH 4.5±0.2.
Methods: The surfactants Polysorbate 80 and Polysorbate 20 differ in their alkyl chain length. Polysorbate 80 has an alkyl chain length of 18, while Polysorbate 20 has an alkyl chain length of 12. The concentrations of surfactant are above, below, and at the critical micelle concentration (CMC) values. The concentrations of quercetin were determined at the maximum wavelength by spectrophotometric method.
Results: The results of the quercetin solubility test without surfactant were 3.89±0.59 mg/L. The results of the quercetin solubility test by adding Polysorbate 20 at a concentration of 42.0 ppm; 57.5 ppm; and 73.0 ppm were 3.62±0.72, 4.04±0.23 and 8.35±1.97 mg/L, respectively. While the solubility of quercetin by adding Polysorbate 80 at a concentration of 4.0 ppm, 11.5 ppm, and 19.0 ppm was 11.15±0.72, 11.37±1.23 and 14.17±1.96 mg/L, respectively. The solubility of quercetin is greater after the addition of surfactant Polysorbate 20 only at the concentration above the CMC value and the solubility of quercetin is greater with the addition of surfactant Polysorbate 80 at all concentrations. Surfactant Polysorbate 20 increases the solubility of quercetin in citrate buffer pH 4.5±0.2 only at concentrations above the CMC value of 2.14 times. Polysorbate 80 can increase the solubility of quercetin in citrate buffer pH 4.5±0.2 at concentrations below, at, and above CMC by 2.87, 2.92, and 3.63 times, respectively.
Conclusion: Polysorbate 80 can increase the solubility of quercetin in citrate buffer pH 4.5±0.2 higher than Polysorbate 20.
Kelly GS. Quercetin. Altern Med Rev 2011;16;172-95.
Madaan K, Lather V, Pandita D. Evaluation of polyamidoamine dendrimers as potential carriers for quercetin, a versatile flavonoid. Drug delivery 2016;23:254-62. DOI: https://doi.org/10.3109/10717544.2014.910564
N'Da DD. Prodrug strategies for enhancing the percutaneous absorption of drugs. Molecules 2014;19:20780-807. DOI: https://doi.org/10.3390/molecules191220780
Allen LV, Ansel HC. Ansel’s pharmaceutical dosage forms and drug delivery systems, 10th ed. Philadelphia: Wolters Kluwer Health; 2014.
Seedher N, Kanojia M. Micellar solubilization of some poorly soluble antidiabetic drugs: a technical note. AAPS PharmSciTech 2008;9:431-6. DOI: https://doi.org/10.1208/s12249-008-9057-5
Rangel-Yagui CO, Hsu HWL, Pessoa-Jr A, Tavares LC. Micellar solubilization of ibuprofen: influence of surfactant head groups on the extent of solubilization. Rev de Ciên Farm Basica 2005;41:237-46. DOI: https://doi.org/10.1590/S1516-93322005000200012
Wang S, Ye F, Wei F, Zhao G. Spray-drying of curcumin-loaded octenyl succinate corn dextrin micelles stabilized with maltodextrin. Powder Technol 2017;307: 56-62. DOI: https://doi.org/10.1016/j.powtec.2016.11.018
Mourya VK, Inamdar N, Nawale RB, Kulthe SS. Polymeric micelles: general considerations and their applications. Indian J Pharm Educ Res 2011;45:128-38.
Butt HJ, Graf K, Kappl M. Physics and chemistry of interfaces. New York: John Wiley & Sons; 2013.
Cagel M, Tesan FC, Bernabeu E, et al. Polymeric mixed micelles as nanomedicines: Achievements and perspectives. J Pharm Biopharm 2017;113:211-28. DOI: https://doi.org/10.1016/j.ejpb.2016.12.019
Rowe RC, Sheskey P, Quinn M. Handbook of pharmaceutical excipients. London: Libros Digitales-Pharmaceutical Press; 2009.
Florence AT, Attwood D. Drug absorption basic and the oral route. In: Physicochemical Principles of Pharmacy, 6th ed. London: Pharmaceutical Press; 2016.
Hoppe K, Sznitowska M. The effect of polysorbate 20 on solubility and stability of candesartan cilexetil in dissolution media. AAPS PharmSciTech 2014;15:1116-25. DOI: https://doi.org/10.1208/s12249-014-0109-8
Moon YJ, Wang L, DiCenzo R, Morris ME. Quercetin pharmacokinetics in humans. Biopharm Drug Dispos 2008;29:205-17. DOI: https://doi.org/10.1002/bdd.605
Pakade VE, Lesaoana M, Tavengwa NT. Effect of pH, time and temperature on forced degradation studies of quercetin in presence of polymers. Asian J Chem 2016;28:2181-7. DOI: https://doi.org/10.14233/ajchem.2016.19913
Patil S, Choudhary B, Rathore A, et al. Enhanced oral bioavailability and anticancer activity of novel curcumin loaded mixed micelles in human lung cancer cells. Phymed 2015;22:1103-11. DOI: https://doi.org/10.1016/j.phymed.2015.08.006
Bhardwaj V, Bhardwaj T, Sharma K, et al. Drug–surfactant interaction: thermo-acoustic investigation of sodium dodecyl sulfate and antimicrobial drug (levofloxacin) for potential pharmaceutical application. RSC Adv 2014;4:24935-43. DOI: https://doi.org/10.1039/C4RA02177K
Shalaby MN, El-Shamy OAA. Performance of some surfactants as wetting agents. Tenside Surfac Det 2005;42:373-8. DOI: https://doi.org/10.3139/113.100280
Copyright (c) 2023 the Authors
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.