EFFECT OF POLYMERS ON THE PHYSICOCHEMICAL AND DRUG RELEASE PROPERTIES OF TRANSDERMAL PATCHES OF ATENOLOL
Objective: The objective of this research work was to develop a transdermal drug delivery system containing atenolol with different ratios of hydrophilic and hydrophobic polymeric combinations, using solvent evaporation technique and to examine the effect of hydrophilicity and hydrophobicity of polymers on the physicochemical and drug release properties of transdermal patches.
Methods: Solvent casting method has been used to formulate transdermal patches. Hydroxypropyl methylcellulose (HPMC), Polyvinylpyrrolidone (PVP), Ethylcellulose (EC) in different combination ratios were used as the polymer. Propylene glycol was used as a plasticizer. Permeation enhancers such as span 80 were used to enhance permeation through the skin. In vitro diffusion study was carried out by franz diffusion cell using egg membrane as a semi-permeable membrane for diffusion.
Results: Result showed that the thickness of the all batch of patches varied from 0.32 to 0.39 mm with uniformity of thickness in each formulation. Formulations F1 to F3 had high moisture content varied from 2.07Â±0.09 to 2.56Â±0.15 and high moisture uptake value varied from 3.21Â±0.35 to 4.09Â±0.38, due to a higher concentration of hydrophilic polymers. Drug content of all batches was ranged between 85.92Â±1.32 to 95.71Â±1.42. Folding endurance values off all batches were more than 75. Formulation batches F1 to F3 showed higher cumulative drug release varied from 61.34% to 68.11% as compared to formulation batches F4 to F6.
Conclusion: Higher proportion of hydrophilic polymer in the formulation of transdermal patches, gives higher percentage drug release from prepared patches. The finding of the study indicates that hydrophilicity and hydrophobicity of polymer effects the physicochemical and drug release properties of transdermal patches and an optimum proportion of hydrophilic and hydrophobic polymer is required for the preparation of effective transdermal patches.Â
2. Cherukuri S, Batchu UR, Mandava K, Cherukuri V, Ganapuram KR. Formulation and evaluation of transdermal drug delivery of topiramate. Int J Pharm Invest 2017;7:10-7.
3. Pastore MN, Kalia YN, Horstmann M, Roberts MS. Transdermal patches: history, development, and pharmacology. Br J Pharmacol 2015;172:2179â€“209.
4. Balaji P, Thirumal M, Gowri R, Divya V, Ramaswamy V. Design, and evaluation of matrix type of transdermal patches of methotrexate. Int J Pharm Chem Biol Sci 2012;2:464 71.
5. Subedi RK, Oh SY, Chun MK, Choi HK. Recent advances in transdermal drug delivery. Arch Pharmacal Res 2010;33:339-51.
6. Keith AD. Polymer matrix consideration for transdermal devices. Drug Dev Ind Pharm 1983;9:605-21.
7. Ahad A, Aqil M, Kohli K, Chaudhary H, Sultana Y, Mujeeb M, et al. Chemical penetration enhancers: a patent review. Expert Opin Ther Pat 2009;19:969-88.
8. Aqil M, Ahad A, Sultana Y, Ali A. Status of terpenes as skin penetration enhancers. Drug Discovery Today 2007;12:1061-7.
9. Agrawal SS, Munjal P. Permeation studies of atenolol and metoprolol tartrate from three different polymer matrices for transdermal delivery. Indian J Pharm Sci 2007;69:535-9.
10. Adhikari SNR, Nayak BS, Nayak AK, Mohanty B. Formulation and evaluation of buccal patches for delivery of atenolol. AAPS PharmSciTech 2010;11:1038â€“44.
11. Kaza R, Pitchaimani R. Formulation of transdermal drug delivery system: matrix type, and selection of polymer-their evaluation. Curr Drug Discovery Technol 2006;3:279-85.
12. Bagyalakshmi J, Vamsikrishna RP, Manavalan R, Ravi TK, Manna PK. Formulation development and in vitro and in vivo evaluation of membrane-moderated transdermal systems of ampicillin sodium in ethanol: pH 4.7 buffer solvent system. AAPS PharmSciTech 2007;8:E50-E55.
13. Costa P, Ferreira DC, Morgado R, Sousa Lobo JM. Design and evaluation of a lorazepam transdermal delivery system. Drug Dev Ind Pharm 1997;23:939-44.
14. Ubaidulla U, Reddy MVS, Ruckmani K, Ahmad FJ, Khar RK. Transdermal therapeutic system of carvedilol: Effect of the hydrophilic and hydrophobic matrix on in vitro and in vivo characteristics. AAPS PharmSciTech 2007;8:E13â€“E20.
15. Murthy SN, Hiremath SRR. Physical and chemical permeation enhancers in transdermal delivery of terbutaline sulphate. AAPS PharmSciTech 2001;2:1-5.
16. Kaur K, Kaur P, Jalhan S, Jain UK. Formulation and in vitro evaluation of transdermal matrix patches of doxofylline. Asian J Pharm Clin Res 2016;9:140-5.
17. Sethi B, Mazumder R. Comparative evaluation of selected polymers and plasticizer on transdermal drug delivery system. Int J Appl Pharm 2018;10:67-73.
18. Das PS, Saha P. Design and characterization of transdermal patches of phenformin hydrochloride. Int J Curr Pharm Res 2017;9:90-3.
19. Hardainiyan S, Kumar K, Nandy BC, Saxena R. Design, formulation, and in vitro drug release from transdermal patches containing imipramine hydrochloride as model drug. Int J Pharm Pharm Sci 2017;9:220-5.
20. Sadhasivam L, Dey N, Francis AP, Devasena T. Transdermal patches of chitosan nanoparticles for insulin delivery. Int J Pharm Pharm Sci 2015;7:84-8.