Relationship between the Amount of Propranolol Permeating through the Stratum Corneum of Guinea Pig Skin after Application of Propranolol Adhesive Patches and Skin Irritation.

Abstract

In the present study we evaluated the relationship between the cumulative amount of propranolol permeating through the stratum corneum and the formation of erythema, a skin irritation reaction, after transdermal application of adhesive patches containing propranolol to the skin of guinea pigs. The intensity of erythema was expressed in terms of a* values measured with a chromameter. The a* values increased in guinea pigs after application of the adhesive patches containing 0.4 mg/cm2 of propranolol to the skin. Since the adhesive patches showed good adhesion to the skin (propranolol content is less than the saturated concentration in the adhesive base) and the cumulative amount of propranolol permeating through the stratum corneum is small, the development of erythema was considered to be mainly due to physical factors such as peeling. Even in adhesive patches containing 0.8 mg/cm2 or 1.2 mg/cm2 of propranolol, a* values increased, although adhesion to the skin is low because of crystallization of propranolol in the adhesive base. On the other hand, in these two adhesive patches, the cumulative amount of propranolol permeating through the stratum corneum increased up to 24 h after application. These findings suggest that the skin irritation reaction is due to propranolol mainly absorbed transdermally, because there is a high correlation between the cumulative amount of propranolol permeating through the stratum corneum and the a* values (r = 0.928).

Elastic Liposomes Mediated Transdermal Deliveryof an Anti-Hypertensive Agent: Propranolol Hydrochloride

“…The enhancement in transdermal flux of propranolol hydrochloride by elastic liposomal formulation is comparable to those reported in previous finding. 3,4 Further, formulation El-Sp80 3 showed the highest percent skin deposition of 11.41 AE 5.2 as compared to other formulations. Better transdermal flux and lower lag phase with our formulation was perhaps due to combination of one or more of following mechanisms: (1) increase in thermodynamic activity, (2) increased skin vehicle partitioning of drug, (3) altering the barrier properties by interacting with skin component, and (4) elasticity of vesicle membrane.…”

“…This would explain that many systems containing propranolol hydrochloride have been recently developed for oral and buccal 1,2 and transdermal administration. 3,4 The weak intrinsic ability of propranolol hydrochloride to cross the skin has been partially improved using prodrugs, micellar solubilization, and chemical penetration enhancers. [5][6][7] However, all these approaches are not successful in improving the transdermal flux to desired level.…”

Effect of Transdermally Delivered Aspirin on Blood Coagulation Parameters

“…It provided efficient matrix to build up a large reservoir of drug in the skin and to achieve greater permeation with a lower amount of drug. Greater penetration with a lower concentration of drug is always preferable as [26], has reported increased irritation on increasing drug concentration in the transdermal device.…”

Effects of Ethylcellulose and 2-Octyldodecanol Additives on Skin Permeation and Irritation with Ethylene-Vinyl Acetate Copolymer Matrix Patches Containing Formoterol Fumarate

“…[22][23][24][25] Moreover, adhesive plasters with low tensile stress and removal force and short stress relaxation time have lowest levels of skin irritation.…”