Abstract
Ferulic acid is contained in some Chinese herbal medicines such as Ligusticum chuanxiong or Angelica sinensis. Studies have focused on the treatment of inflammatory diseases and pain using ferulic acid. However, little is known about its pharmacokinetics after transdermal administration. The present research investigated the pharmacokinetic behavior of ferulic acid in rat plasma and skin microdialysate after ferulic acid transdermal or intragastric administration. Samples collected at predetermined time points were determined by a simple and sensitive HPLC-UV method. The pharmacokinetic parameters were estimated using non-compartmental analysis with DAS 2.0 software. The values of AUC0-t and Cmax after intragastric administration (20 mg/kg) in plasma were 281.47 ± 46.76 min mg/L and 12.20 ± 2.46 mg/L, respectively. After emulsion transdermal administration (117 mg/kg, 35 mg/4 cm2), the values of AUC0-t and Cmax in plasma and skin microdialysate were 953.90 ± 175.30 min mg/L, 7630.47 ± 1410.33 min mg/L, 3.00 ± 0.61 mg/L, and 19.08 ± 4.39 mg/L, respectively. Here, we show a promising delivery system for ferulic acid that could replace traditional administration, and a better understanding of the transdermal pharmacokinetics of ferulic acid, which may be helpful for further clinical and laboratory studies.
Similar content being viewed by others
References
Mir SM, Ravuri HG, Pradhan RK, Narra S, Kumar JM, Kuncha M, et al. Ferulic acid protects lipopolysaccharide-induced acute kidney injury by suppressing inflammatory events and upregulating antioxidant defenses in Balb/c mice. Biomed Pharmacother. 2018;100:304–15. https://doi.org/10.1016/j.biopha.2018.01.169.
Doss HM, Dey C, Sudandiradoss C, Rasool MK. Targeting inflammatory mediators with ferulic acid, a dietary polyphenol, for the suppression of monosodium urate crystal-induced inflammation in rats. Life Sci. 2016;148:201–10. https://doi.org/10.1016/j.lfs.2016.02.004.
Zhang L, Wang QD, Shi HM. Influence of ferulic acid on the pain-depression dyad induced by reserpine. Acta Pharm Sin. 2013;48(1):32–7.
Liu YM, Shen JD, Xu LP, Li HB, Li YC, Yi LT. Ferulic acid inhibits neuro-inflammation in mice exposed to chronic unpredictable mild stress. Int Immunopharmacol. 2017;45:128–34. https://doi.org/10.1016/j.intimp.2017.02.007.
Meng R, Chen YQ, Chen Q. Effect of ferulic acid glial activaton and inflammatory cytokines expression in the cerebral cortex of Alzheimer’s like model mice. Chin Hosp Pharm J. 2018;38(1):50–3.
Feng BB, Zhang JH, Zhang JF, Chen G, Xu XY. Comparative study on pharmacokinetics of tetramethylpyrazine, ferulic acid and their compatibility. China J Chin Mater Med. 2010;35(7):900–3.
Ou YZ, Pan LL, Tang JM, Yang Y, Wang B. Studies on pharmacokinetics of ferulic acid, rhizoma chuanxiong and naodesheng capsule in rat. China J Chin Mater Med. 2010;35(2):226–8.
Zhang JF, Yuan HH, Lin D, Tang Q, Xu XY. Study on pharmacokinetics of ferulic acid loaded liposome in chitosan microspheres in rats. China J Chin Mater Med. 2011;36(13):1751–4.
Mo LL, Wang SJ, Yang BK. Permeability of ferulic acid in Caco-2 cell model and its absorption properties in rats in vivo. China Tradit Herb Drugs. 2012;43(5):947–51.
Chen XM, Wang XW, Luo J, Jia P, Wang XY, Xiao CN, et al. Pharmacokinetic studies of xuebijing injection in rats. Chin J Pharm Anal. 2012;32(5):744–8+54.
Zhang CY, Zhang H, Dong Y, Ren WG, Chen HW. Study on compatibility of salviae miltiorrhizae radix et rhizoma and chuanxiong rhizoma based on pharmacokinetics of effective components salvianolic acid B and ferulic acid in rat plasma. China J Chin Mater Med. 2015;40(8):1589–93.
Kalia YN, Guy RH. Modeling transdermal drug release. Adv Drug Deliv Rev. 2001;48(2–3):159–72. https://doi.org/10.1016/S0169-409X(01)00113-2.
Lee H, Song C, Baik S, Kim D, Hyeon T, Kim D. Device-assisted transdermal drug delivery. Adv Drug Deliv Rev. 2018;127:35–45. https://doi.org/10.1016/j.addr.2017.08.009.
Jin SG, Yousaf AM, Son MW, Jang SW, Kim DW, Kim JO, et al. Mechanical properties, skin permeation and in vivo evaluations of dexibuprofen-loaded emulsion gel for topical delivery. Arch Pharm Res. 2015;38(2):216–22. https://doi.org/10.1007/s12272-014-0367-8.
Roberta L, Antonio C, Stefano G, Sergio C. Transport efficiency in transdermal drug delivery: what is the role of fluid microstructure? Colloids Surf B: Biointerfaces. 2016;139:294–305. https://doi.org/10.1016/j.colsurfb.2015.11.064.
Marwah H, Garg T, Goyal AK, Rath G. Permeation enhancer strategies in transdermal drug delivery. Drug Delivery. 2016;23(2):564–78. https://doi.org/10.3109/10717544.2014.935532.
Lan Y, Wang YJ, Tao Y, Ru QG, Wang YF, Yu JX, et al. Comparison of essential oil from mentha haplocalyx and menthol used as penetration enhancers. China J Chin Mater Med. 2016;41(8):1516–22.
Bai J, Lu Y, Du SY, Liu CM. Pharmacokinetics of ferulic acid in transdermal delivery. China J Chin Mater Med. 2013;38(5):743–7.
Bai J, Lu Y, Du SY, Liu CM, Li PY, Li Y. Preparation and in vitro in vivo evaluation of chuanxiong cataplasm. Chin J Trad Chin Med Pharm. 2013;28(5):1259–66.
Erdő F, Hashimoto N, Karvaly G, Nakamichi N, Kato Y. Critical evaluation and methodological positioning of the transdermal microdialysis technique. A review J Control Release. 2016;233:147–61. https://doi.org/10.1016/j.jconrel.2016.05.035.
Tomas A, Stilinović N, Sabo A, Tomić Z. Use of microdialysis for the assessment of fluoroquinolone pharmacokinetics in the clinical practice. Eur J Pharm Sci. 2019;131:230–42. https://doi.org/10.1016/j.ejps.2019.02.032.
Ahad A, Aqil M, Kohli K, Sultana Y, Mujeeb M. The ameliorated longevity and pharmacokinetics of valsartan released from a gel system of ultradeformable vesicles. Artif Cells Nanomed Biotechnol. 2016;44(6):1457–63. https://doi.org/10.3109/21691401.2015.1041638.
Nair RS, Morris A, Billa N, Leong CO. An evaluation of curcumin-encapsulated chitosan nanoparticles for transdermal delivery. AAPS PharmSciTech. 2019;20(2):69–81. https://doi.org/10.1208/s12249-018-1279-6.
Tripti S, Neeraj U, Mukta A, Swarnlata S, Shailendra S, Amit A. Biomedical applications of microemulsion through dermal and transdermal route. Biomed Pharmacother. 2018;108:1477–94. https://doi.org/10.1016/j.biopha.2018.10.021.
Zhang LW, Al-Saleh SA, Suwayeh A, Hsieh PW, Fang JY. A comparison of skin delivery of ferulic acid and its derivatives: evaluation of their efficacy and safety. Int J Pharm. 2010;399(1–2):44–51. https://doi.org/10.1016/j.ijpharm.2010.07.054.
Monti D, Tampucci S, Chetoni P, Burgalassi S, Saino V, Centini M, et al. Permeation and distribution of ferulic acid and its α-cyclodextrin complex from different formulations in hairless rat skin. AAPS PharmSciTech. 2011;12(2):514–20. https://doi.org/10.1208/s12249-011-9609-y.
Otto A, Plessis JD, Wiechers JW. Formulation effects of topical emulsions on transdermal and dermal delivery. Int J Cosmet Sci. 2009;31(1):1–19. https://doi.org/10.1016/j.ejpb.2017.12.004.
Hoppel M, Reznicek G, Kählig H, Kotisch H, Resch GP, Valenta G. Topical delivery of acetyl hexapeptide-8 from different emulsions: influence of emulsion composition and internal structure. Eur J Pharm Sci. 2015;68:27–35. https://doi.org/10.1016/j.ejps.2014.12.006.
Kováčik A, Kopečná M, Vávrová K. Permeation enhancers in transdermal drug delivery: benefits and limitations. Expert opinion on drug delivery. 2020;17(2):145–55. https://doi.org/10.1080/17425247.2020.1713087.
Shruti C, Jonathan G, Hardman. Factors affecting drug absorption and distribution. Anaesth Intens Care Med. 2017;18(7):335–9. https://doi.org/10.1016/j.mpaic.2017.04.007.
Funding
The paper is supported by Key Laboratory of Neuropsychiatric Drug Reserch of Zhejiang Province (2019E10021).
Author information
Authors and Affiliations
Corresponding author
Ethics declarations
Conflict of Interest
The authors declare that they have no conflict of interest.
Additional information
Publisher’s Note
Springer Nature remains neutral with regard to jurisdictional claims in published maps and institutional affiliations.
Rights and permissions
About this article
Cite this article
Yan, N., Tang, Z., Xu, Y. et al. Pharmacokinetic Study of Ferulic Acid Following Transdermal or Intragastric Administration in Rats. AAPS PharmSciTech 21, 169 (2020). https://doi.org/10.1208/s12249-020-01709-w
Received:
Accepted:
Published:
DOI: https://doi.org/10.1208/s12249-020-01709-w