Skin permeation of propranolol from polymeric film containing terpene enhancers for transdermal use

• Published in: International journal of pharmaceutics Vol. 289; no. 1; pp. 167 - 178
• Main Authors: Amnuaikit, Chomchan, Ikeuchi, Itsue, Ogawara, Ken-ichi, Higaki, Kazutaka, Kimura, Toshikiro
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 31.01.2005; Elsevier
• Subjects: Administration, Cutaneous; Animals; Biological and medical sciences; Cell Membrane Permeability - drug effects; Cellulose - analogs & derivatives; Cellulose - chemistry; Cellulose - pharmacokinetics; Cineole; Dibutyl Phthalate - chemistry; Dibutyl Phthalate - pharmacokinetics; Diffusion; Drug Carriers - chemistry; Drug Carriers - pharmacokinetics; Drug Evaluation, Preclinical - methods; General pharmacology; Male; Medical sciences; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Polymeric film; Povidone - chemistry; Povidone - pharmacokinetics; Propranolol - administration & dosage; Propranolol - pharmacokinetics; Propranolol hydrochloride; Propylene glycol; Propylene Glycol - chemistry; Propylene Glycol - pharmacokinetics; Rats; Rats, Wistar; Skin Absorption - drug effects; Skin Absorption - physiology; Terpene; Terpenes - chemistry; Terpenes - pharmacokinetics; Transdermal absorption; Polymeric film; Propranolol hydrochloride; Propylene glycol; Terpene; Transdermal absorption; Cineole; Pharmaceutical technology; Film; Control release polymer; Antiarrhythmic agent; Expectorant; β-Adrenergic receptor; Percutaneous route; Eucalyptol; Absorption; Skin; Antagonist; Pharmacokinetics; Propanediol; Propranolol; Beta blocking agent
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2004.11.007

To develop the suitable film formulations of propranolol hydrochloride (PPL) containing enhancers for transdermal use, polymeric film formulations were prepared by employing ethyl cellulose (EC) and polyvinyl pyrrolidone (PVP) as a film former, and dibutyl phthalate (DBP) as a plasticizer. Terpenes such as menthol and cineole, and propylene glycol (PG) were also employed as a chemical enhancer to improve the skin penetration of PPL. The film preparations were characterized in physical properties such as uniformity of drug content, thickness and moisture uptake capacity. Release and skin permeation kinetics of PPL from film preparations were examined in the in vitro studies using a Franz-type diffusion cell. The uniformity of drug content was evidenced by the low S.D. values for each film preparation. The moisture uptake capacity and drug release rate increased with the increase of PVP in each preparation. Enhancers examined in the present study also increased the moisture uptake capacity and release rate of PPL from the film preparations. Increasing the concentration of PPL from 1 to 2 mg/cm 2 in the film enhanced the release rate of PPL, while no effect of enhancer concentrations on the release rate from the film preparations was observed. In vitro skin permeation study showed that cineole was the most promising enhancer among the enhancers examined in the present study and suggested that the suitable compositions of film preparation would be EC:PVP:PPL = 6:3:4 with 10% (w/w) cineole and 7:2:4 with 10% (w/w) PG and cineole, which provided high skin permeation rates at 93.81 ± 11.56 and 54.51 ± 0.52 μg/cm 2/h, respectively.