Abstract
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.
Highlights
In the current scenario, hypertension is the major factor for cardiovascular disease and the leading cause of death in economically developed countries
Ang II is formed in a two-step: angiotensinogen converted to angiotensin I (AngI), which is converted by angiotensin converting enzyme (ACE) into angiotensin II (AngII)
Transdermal patches containing aliskiren hemifumarate were prepared by a solvent casting method
Summary
Hypertension is the major factor for cardiovascular disease and the leading cause of death in economically developed countries. The renin-angiotensin system (RAS) is the main regulator of blood pressure and body fluid volume and acts primarily via the effects of the octapeptide hormone, angiotensin II (AngII). Ang II is formed in a two-step: angiotensinogen converted to angiotensin I (AngI), which is converted by angiotensin converting enzyme (ACE) into AngII. Ang II increases blood pressure and exerts direct growth-promoting effects on cardiac and renal tissue that causes organ damage [1,2,3]. Topical delivery for treatment of hypertension shows better results. The barrier causing agent during transdermal delivery is “Skin”. Skin plays a vital role for the transportation of the drug. There are three routes from which molecules can penetrate the skin: (1) intracellular, (2) intercellular lipids, and (3) appendages. Absorption through the skin is affected by a number of factors including the origin (human, animal), type of skin, physicochemical properties of the compound and formulations, as well as possible skin pretreatment and environmental factors [6,7,8,9]
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