FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF METOPROLOL TARTRATE USING PERMEATION ENHANCERS OF NATURAL AND SYNTHETIC ORIGIN

  • SHIKHA BAGHEL CHAUHAN Department of Pharmaceutics, Amity Institute of Pharmacy, Amity University, Noida, Uttar Pradesh, India
  • SUSHILA SAINI Research Scholar, Department of Pharmaceutics, Amity Institute of Pharmacy, Amity University, Noida, Uttar Pradesh, India

Abstract

Objective: Oral metoprolol tartrate has a short elimination half-life (2-3h) and low bioavailability undergoes extensive first-pass metabolism and frequent dosing. The aim of the present investigation was to formulate, develop and evaluate metoprolol tartrate transdermal patches using various synthetic and natural penetration enhancers.


Methods: Enhancers used were eugenol, limonene, basil oil, urea and SLS (sodium lauryl sulphate). Polymer used was chitosan and PEG 400 used as a plasticizer. Transdermal Films were prepared by using solvent casting method. FTIR and DSC were studied to assess any interaction between the drug and polymers. Films were evaluated for Physico-chemical Characteristics like thickness, weight variation, folding endurance, moisture loss, moisture absorption and drug content. In vitro skin permeation studies were performed using Keshary chien cell For 24 h across rat skin.


Results: Chitosan was found to be a suitable polymer for matrix formation. 3.5% w/w was used to optimize to formulate transdermal patches. 1.5% of total solution v/v lactic acid was used for dissolution of chitosan. 2.5%v/v of total solution PEG 400 was used to provide plasticity and smoothness to the patches. From the evaluation of patches formulation, F10 containing Basil oil as penetration enhancer in the concentration of 1.5% v/v was found to be best among all batches because of its consistent release rate For 24 h and extent of drug release was 85.20%. It can be concluded that naturally occurring volatile oils i.e., terpenes appear acceptable permeation enhancer and shows the best permeation across skin as indicated by high percutaneous enhancement ability.


Conclusion: The developed transdermal patches are stable, non-irritating, and had increased efficacy of metoprolol and therefore had a good potential for hypertension treatment.

Keywords: Transdermal drug delivery system, Chitosan, PEG 400, Penetration Enhancers, Basil oil, Limonene, Eugenol, Urea, Sodium lauryl sulphate

References

1. Tripathi KD. Essential of medical pharmacology. 6th ed; 2010;6:539.
2. Sharma HL, Sharma KK. Principle of pharmacology. 1st Edition; 2011. p. 19.
3. Wexler R, Aukerman G. Non pharmacological strategies for managing hypertension. Am Fam Physician 2006;11:1953-6.
4. MahFoud Felix, Himmel Frank, Ukena Christan, Schunkert Heribert, Bohm Michael, Weil Joachim. Treatment strategies for resistant arterial hypertension. Dtsch Arztebl 2011;43:725-31.
5. Zamanian TR, Haddad Francois, Doyle LR, Weinacker BA. Management strategies for patient with pulmonary hypertension in the intensive care unit. Crit Care Med 2007;35:2037-50.
6. Sowmya C, Suryaprakash Reddy C, Amrutha V, Anil Kumar D, Lohitha M. Transdermal therapeutic systems. Int J Pharm Industrial Res 2012;2:197-211.
7. Rastogi V, Pragya, Upadhyay P. A brie F view on antihypertensive drugs delivery through transdermal patches. Int J Pharm Sci Res 2012;3:1955-70.
8. Patel D, Patel N, Parmar M. Transdermal drug delivery systems: review. Int J Pharm Toxic Res 2011;1:61-80.
9. Patel D, Chaudhary SA, Parmar, Bhura N. Transdermal drug delivery system: an review. Pharma Innovation 2012;4:78-87.
10. Prabhakar D, Sreekanth J, Jayaveera KN. Transdermal drug delivery patches: a review. J Drug Delivery Ther 2013;3:213-21.
11. Yadav V, Sipai A, Mamatha Y, Prasantha V. Transdermal drug delivery: a technical write up. J Pharm Sci Innovation 2012;1:5-12.
12. Mudavath Hanumanaik, Patel D, Kumar G, Patel SK, Singh I. Design, evaluation and recent trends in transdermal drug delivery system. Int J Pharm Sci Res 2012;3:2393-406.
13. Dhangwal M. Transdermal drug delivery system. Pharma tutor; 2015.
14. John L, Kumar A. Comparison of amlodipine transdermal patch using HPMC and chitosan. Asian J Pharm Clin Res 2014;7:86-90.
15. Satheeshababu BK, Kumar SKL. Synthesis of conjugated chitosan and its effect on drug permeation from transdermal patches. Indian J Pharm Sci 2013;75:162-70.
16. Can AS, Erdal MS, Gungor S. Optimization and characterization of chitosan films for transdermal delivery of ondansetron. Molecules 2013;18:5455-71.
17. Madhulatha A. Formulation and evaluation of transdermal patches. Int J Res Pharm Med Sci 2013;4:351-62.
18. Balamurugan M, Agrawal SS. Formulation and evaluation of chitosan-based bioadhesive transdermal drug delivery system of lisinopril for prolonged drug delivery. Pharm Sin 2013;4:1-7.
19. Chauhan SB, Naved T. Formulation and development of transdermal drug delivery system of ethinylestradiol and medroxyprogesterone acetate for antifertility treatment. Int J ChemTech Res 2017;10:1164-71.
20. Chauhan SB, Naved T. Formulation and development of transdermal drug delivery system of antifertility drugs using a combination of polymers. Int J Pharma Bio Sci 2017;8:30-5.
21. Chauhan S, Naved T, Parvez N. Formulation and development of transdermal drug delivery system of ethinylestradiol and testosterone: in vitro evaluation. Int J Appl Pharm 2019;11:55-60.
22. Chauhan S, Naved T, Parvez N. Effect of hydrophilic and hydrophobic polymer matrix on the transdermal drug delivery of ethinylestradiol and medroxyprogesterone acetate. Int J Appl Pharm 2019;11:210-5.
23. Chauhan SB, Naved T, Parvez N. Formulation development and evaluation of proniosomal gel of ethinylestradiol and levonorgestrel for antifertility treatment. Asian J Pharm Clin Res 2019;12:364-8.
24. Denge MS, Walde SR, Ittadwar AM. Development and characterization of transdermal patches of ondansetron hydrochloride. Int J Pharm Pharm Sci 2012;4:293-8.
25. Jadhav JK, Sreenivas SA. Formulation and in vitro evaluation of indomethacin transdermal patches using polymers HPMC E5 and ethyl cellulose. Int J Pharm Pharm Sci 2012;4:550-6.
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CHAUHAN, S. B., & SAINI, S. (2019). FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF METOPROLOL TARTRATE USING PERMEATION ENHANCERS OF NATURAL AND SYNTHETIC ORIGIN. International Journal of Applied Pharmaceutics, 11(5), 317-323. https://doi.org/10.22159/ijap.2019v11i5.32759
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