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Pharmacokinetic and pharmacodynamic studies of etodolac loaded vesicular gels on rats by transdermal delivery

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Abstract

Background

The present study includes the development of liposomal and ethosomal gels for transdermal delivery to overcome the side effects associated with oral route.

Methods

The liposomes and ethosomes were prepared by 32 factorial design using film hydration and cold methods, respectively. Different concentrations of liposomal (ETO-LG) and ethosomal (ETO-EG) gels were prepared at 1%, 2 and 3% (w/v) using carbopol 940 NF. 1%w/v ETO-LG & ETO-EG were optimized upon rheological studies of prepared gels. The optimized gels were further characterized for various physicochemical properties and biophysical studies using FTIR, pharmacokinetic (PK) and pharmacodynamic (PD) studies. The pharmacodynamic activity was performed using carrageenan paw oedema model. The prepared vesicular gels were compared with 45% v/v ethanolic ETO-solution and marketed gel PROXYM® in all the characteristic parameters.

Results

The pharmacokinetic study reveals that the half life of etodolac in ETO-EG was 1.56 folds whereas ETO-LG showed 1.31 folds higher than PROXYM®. The mean residence time (MRT) of etodolac in ETO-EG and ETO-LG is increased in 1.57 and 1.25 folds, respectively, when compared to PROXYM®. The ETO-EG showed higher percentage reduction in oedema (81.67%) compared to other test products.

Conclusion

The pharmacokinetic and pharmacodynamic studies indicated that the vesicular gels show better results compared to PROXYM®. The correlation coefficient value between PK and PD was found to be 0.9635.

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Abbreviations

PK:

Pharmacokinetic

PD:

Pharmacodynamic

HSPC:

Hydrogenated soya Phosphotidylcholine

RBF:

Round bottom flask

ETO-LG:

Etodolac liposomal gel

ETO-EG:

Etodolac ethosomal gel

RIE:

Reduction in oedema

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Acknowledgements

Author thankful to UGC-RGNF Scheme for providing sufficient fund to complete the project.

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Authors and Affiliations

  1. Department of Pharmaceutical Technology, A.U. College of Pharmaceutical Sciences, Andhra University, Visakhapatnam, Andhra Pradesh, 530003, India

    Nimmathota Madhavi, Beeravelli Sudhakar & Jayanthi Vijaya Ratna

  2. Department of Chemistry, Institute of Technology, GITAM (Deemed to be University), Visakhapatnam, Andhra Pradesh, 530045, India

    K. V. N. Suresh Reddy

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  1. Nimmathota Madhavi
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  2. Beeravelli Sudhakar
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Correspondence to Nimmathota Madhavi.

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Madhavi, N., Sudhakar, B., Suresh Reddy, K.V.N. et al. Pharmacokinetic and pharmacodynamic studies of etodolac loaded vesicular gels on rats by transdermal delivery. DARU J Pharm Sci 26, 43–56 (2018). https://doi.org/10.1007/s40199-018-0214-4

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