COMPARATIVE EVALUATION OF SELECTED POLYMERS AND PLASTICIZER ON TRANSDERMAL DRUG DELIVERY SYSTEM
Keywords:Transdermal Patches, Aliskiren Hemifumarate, Methocel (K15 and K100), Ethocel (4 and 10), Gelatin, Chitosan, Eudragit (RL and RS), Glycerin, Propylene glycol, Solvent casting method, Hypertension
Objective: The present work was aimed at preparation of transdermal patches by a solvent casting method using a varying concentration of polymers i.e. methocel (K15 and K100), ethocel (4 and 10), gelatin, chitosan, eudragit (RL and RS) grade using plasticizer (glycerin and propylene glycol).
Methods: The ratio of drug to polymers and plasticizer was varied and the effect of formulation variables was studied. Prepared transdermal patches were evaluated for physicochemical properties, in-vitro permeation studies, content uniformity, primary skin irritation studies and FT-IR studies.
Results: The formulated transdermal patch by using Methocel K 100 M showed good physical properties. The average weight of patches prepared using glycerin as a plasticizer were ranged from 42.33-67.00 mg and propylene glycol as a plasticizer were ranged from 40.67-67.67 mg. The percentage moisture absorption varies from 1.76 to 10.73 for patches formulated using glycerin and 2.28 to 7.97 for propylene glycol patches. The percentage moisture loss from patches prepared using glycerin was ranged from 2.75 to 11.54 and 2.87 to 12.02 from propylene glycol. The water vapour transmission rate from patches prepared using glycerin was ranged from 0.25 to 0.92 and 0.41 to 1.76. The formulated patch showed the acceptable quantity of medicament ranged from (100.20-101.05%). This result met the test content uniformity as per BP (85% to 115%). According to that, the drug was consistent throughout the patches. The formulation PGD is considered as the best formulation, since it shows a maximum in vitro drug release as 43.75 % at 24 h. The drug release kinetics studied showed that the majority of formulations was following zero order.
Conclusion: In conclusion, controlled release transdermal drug delivery system patches of aliskiren can be prepared using polymer combinations, with a different plasticizer. The release rate of drug depends upon the polymer. However, release kinetics followed zero order.
Wood JM, Maibaum J, Rahuel J, Grutter MG, Cohen NC, Rasetti V, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor. Biochem Biophys Res Commun 2003;308:698â€“705.
Raman VK, Lee YA, Lindpaintner K. The cardiac reninâ€“angiotensinâ€“aldosterone system and hypertensive cardiac hypertrophy. Am J Cardiol 1995;76:18D-23D.
Mezzano SA, Ruiz-ortega M, Egido J. Angiotensin II and renal fibrosis. Hypertension 2001;38:635â€“8.
Skeggs LT, Kahn JR, Lentz K, Shumway NP. Preparation, purification and amino acid sequence of a polypeptide rennin substrate. J Exp Med 1957;106:439â€“53.
Fisher ND, Hollenberg NK. Is there a future for rennin inhibitors. Expert Opin Investig Drugs 2001;10:417â€“26.
Larraneta E, Lutton REM, Woolfson AD, Donneley RF. Microneedle arrays as transdermal and intradermal drug delivery systems: materials science, manufacture and commercial development. Mater Sci Eng 2016;104:1â€“32.
Chen Y, Quan P, Liu X, Fang L. Novel chemical permeation enhancers for transdermal drug delivery. Asian J Pharm Sci 2014;9:51-64.
Stoicea N, Fiorda-Diaz J, Joseph N, Shabsigh M, Arias-Morales C, Gonzalez-Zacarias AA, et al. Advanced analgesic drug delivery and nanobiotechnology. Drugs 2017;3:1-4.
Herman A, Herman AP. Essential oils and their constituents as skin penetration enhancer for transdermal drug delivery: a review. J Pharm Pharmacol 2014;67:473â€“85.
Vizseralek G, Berko S, Toth G, Balogh R, Budai-Szucs M, Csanyi E, et al. Permeability test for transdermal and local therapeutic patches using Skin PAMPA method. Eur J Pharm Sci 2015;76:165â€“72.
Ahad A, Al-Jenoobi FI, Al-Mohizea AM, Akhtar N, Raish M, Aqil M, et al. Systemic delivery of b-blockers via transdermal route for hypertension. Saudi Pharm J 2015;23:587â€“602.
Prausnitz MR, Langer R. Transdermal drug delivery. Nat Biotechnol 2008;26:1261â€“8.
Polat BE, Blankschtein D, Langer R. Low-frequency sonophoresis: application to the transdermal delivery of macromolecules and hydrophilic drugs. Expert Opin Drug Delivery 2010;7:1415â€“32.
Ham AS, Buckheit RW. Current and emerging formulation strategies for the effective transdermal delivery of HIV inhibitors. Ther Delivery 2015;6:217â€“29.
Gradman AH, Pinto R, Kad R. Current concepts: renin inhibition in the treatment of hypertension. Curr Opin Pharmacol 2008;8:120â€“6.
Sadeghpour A, Rappolt M, Ntountaniotis D, Chatzigeorgiou P, Viras K, Megariotis G, et al. Comparative study of interactions of aliskiren and AT1 receptor antagonists with lipid bilayers. Biochim Biophys Acta 2015;184:984â€“94.
Ubaidulla U, Reddy MVS, Kandasamy R, Khar RK. The transdermal therapeutic system of carvedilol: effect of hydrophilic and hydrophobic matrix on in vitro and in vivo characteristics. AAPS PharmSciTech 2007;8:E1-E8.
Amnuaikit C, Ikeuchi I, Ogawara K, Higaki K, Kimura T. Skin permeation of propranolol from a polymeric film containing terpene enhancers for transdermal use. Int J Pharm 2005;289:167â€“78.
Gupta RR, Jain SK, Varshney M. AOT water-in-oil microemulsions as a penetration enhancer in transdermal drug delivery of 5-fluorouracil. Colloids Surf B 2005;41:25â€“32.
Sadeq ZA, Rajab NA. Studying the effect of different variables on the formulation of mucoadhesive buccal patches of captopril. Int J Appl Pharm 2017;9:16-21.
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.