Effects of formulations and penetration enhancers on the diffusional parameters for the percutaneous absorption of propranolol hydrochloride

Document Type : Original Article

Authors

1 Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Egypt

2 Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia

Abstract

Propranolol hydrochloride, the com. available form of propranolol, was formulated as gels using different cellulose polymers viz. methylcellulose, CM-​cellulose, and hydroxypropyl methylcellulose (HPMC)​.  In vitro percutaneous absorption study of the gels was conducted using improved franz diffusion cells and rabbit skin as a membrane.  The highest extent of drug penetration was obtained upon using HPMC gel formulation.  Therefore, the influence of drug concn. on its percutaneous absorption was investigated utilizing HPMC gel formulation.  The extent of drug percutaneous absorption was found to increase as drug concn. increases.  Anal. of the diffusional parameters, govern the skin penetration process, revealed that diffusion coeff. of the drug did not change as drug concn. varies.  On the other hand, the apparent permeability coeff., and the apparent partition coeff., showed dependency on drug concn.  The limit value of the partition coeff. was detd., graphically, and found to be 0.2411.  The influence of skin penetration enhancers, such as Azone, n-​decyl alc., and 1,​8-​cineol, on the percutaneous absorption of the drug was studied.  An overall low enhancing effect (max. of 5.7-​fold compared to a control) was obtained using 1,​8-​cineol.  This finding was attributed to the opposite influence of the cited enhancers on the diffusion coeff. and the partition coeff. of the drug.  The enhancers increase the resistance of the skin to the penetration of drug mols. (decreasing the diffusion coeff.)​.  Meanwhile, the enhancers facilitate the partitioning process of the drug mols. from the gel to the skin as the apparent partition coeff. increases.