Bioavailability augmentation of silymarin using natural bioenhancers: An <i>in vivo</i> pharmacokinetic study

Javed, Shamama; Kohli, Kanchan; Ahsan, Waquar

doi:10.1590/s2175-97902022e20160

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Brazilian Journal of Pharmaceutical Sciences

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Article • Braz. J. Pharm. Sci. 58 • 2022 • https://doi.org/10.1590/s2175-97902022e20160 copy

Bioavailability augmentation of silymarin using natural bioenhancers: An in vivo pharmacokinetic study

Authorship SCIMAGO INSTITUTIONS RANKINGS

Abstract

Pharmacokinetic studies were carried out in male and female rats to quantify silymarin as silybin (A+B) after the oral administration of various silymarin formulations combined with three bioenhancers, namely, lysergol, piperine, and fulvic acid, and compared with plain silymarin formulation (control). A non-compartmental analysis, model independent analysis, was utilized, and various pharmacokinetic parameters (C _max, T _max, and AUC _0-t) were calculated individually for each treatment group, and the values were expressed as mean ± SEM (n = 6). Plasma samples obtained from the rats were analyzed for the concentration of silymarin through a validated RP-HPLC method and on the basis of data generated from the pharmacokinetic studies. Results indicated that the bioenhancers augmented pharmacokinetic parameters and bioavailability increased 2.4-14.5-fold in all the formulations compared with the control. The current work envisages the development of an industrially viable product that can be further subjected to clinical trials and scientifically supports the development of silymarin as a contemporary therapeutic agent with enhanced bioavailability and medicinal values.

Keywords:
Silymarin; Bioavailability; Piperine; Fulvic acid; Lysergol

Precision	Observed concentration (µg/mL)	Precision R.S.D (%)	Accuracy Bias (%)
Inter day
0.05	0.061 ± 0.06	0.107	1.22
0.5	0.59 ± 0.05	0.092	1.19
2.0	2.56 ± 0.34	0.119	1.28
Intra day
0.05	0.054 ± 0.07	0.128	1.09
0.5	0.6 ± 0.062	0.104	1.21
2.0	2.63 ± 0.35	0.116	1.32
Repeatability	Repeatability (intra-day % R.S.D, n = 3) = 0.10- 0.12%.
Reproducibility	Reproducibility (inter-day % R.S.D, n=3) = 0.09 - 0.11%.
Selectivity	Assessed by preparing various concentrations of standard silybin within the linear range and analyzing using this method.
Recovery (%)	Good % recovery values at 0.05 (82.25%), 0.5 (83.45%) and 2.0% (84.40%) suggested accuracy of the method.
Limit of Detection	The Limit of Detection was found to be 0.038 µg/mL
Limit of Quantification	The Limit of Quantification was found to be 0.118 µg/mL.

PK Parameters	Plain silymarin Tablet (Control)	Silymarin-Lysergol Tablet	Silymarin-Piperine Tablet	Silymarin-Fulvic Acid Tablet	Silymarin-Fulvic Acid-Piperine Tablet
C_max (µg/mL)	1.51 ± 0.21	1.64 ± 0.15	1.84 ± 0.32	5.93 ± 1.23	16.32 ± 1.85
T_max (hr)	1.0 ± 0.12	1.0 ± 0.15	2.0 ± 0.18	1.5 ± 0.18	1.5 ± 0.14
AUC_(0-8h) (µg-hr/mL)	2.31 ± 1.35	5.69 ± 1.45	8.45 ± 1.65	12.37 ± 1.87	33.44 ± 1.98
MRT (hr)	2.91 ± 1.43	3.01 ± 1.12	3.79 ± 1.32	3.24 ± 1.43	3.95 ± 1.41
T_1/2 (hr)	1.84 ± 0.55	3.15 ± 1.63	3.36 ± 1.54	1.00 ± 0.17	3.75 ± 1.56
AUC_(0-∞) (µg-hr/mL)	2.55 ± 1.21	8.47 ± 1.41	11.56 ± 1.63	13.47 ± 1.78	37.27 ± 1.89
Folds increase in bioavailability	--	2.4	3.65	5.35	14.53

Universidade de São Paulo, Faculdade de Ciências Farmacêuticas Av. Prof. Lineu Prestes, n. 580, 05508-000 S. Paulo/SP Brasil, Tel.: (55 11) 3091-3824 - São Paulo - SP - Brazil
E-mail: bjps@usp.br

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[1] *Correspondence: W. Ahsan. Department of Pharmaceutical Chemistry. College of Pharmacy. Jazan University. P. Box No. 114, Jazan, Saudi Arabia. Phone: +966 552144370. Email: wmohammad@jazanu.edu.sa.