Effect of penetration enhancers on the transdermal delivery of bupranolol through rat skin.
Bupranolol (BPL) is a suitable drug candidate for transdermal drug delivery system development based on its favorable physicochemical and pharmacokinetic properties. The effect of different penetration enhancers on the permeation of BPL across rat skin was studied using side-by-side diffusion cells. 2-Pyrrolidone (PY), 1-methyl-2-pyrrolidone (MPY), and propylene glycol (PG) at various concentrations were used as penetration enhancers along with 0.4% w/v aqueous suspension of BPL. Menthol at different concentrations in isopropanol-water (6:4) mixture also was used as an enhancer wherein BPL at 0.4% w/v was completely solubilized. Skin pretreatment studies were carried out with all the above enhancers to understand their role in the penetration enhancement effect. PY and MPY at 5% w/v concentrations increased the permeation of BPL by 3.8- and 2.4-fold, respectively, versus control (p < .01). PG at 10% and 30 w/v concentrations increased the flux of BPL by 2.5- and 5.0-fold, respectively, versus control (p < .001). Menthol at 2% w/v concentration increased the flux of BPL by 3.8-fold (p < .01) and further increase in menthol concentration significantly decreased the flux of BPL. Overall, pyrrolidones and menthol at low concentrations (5% w/v or less) and PG at 30% w/v concentration were effective as penetration enhancers for BPL.
Babu
R Jayachandra
RJ
College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, USA. jaychandrababu@yahoo.com
Pandit
Jayanta Kumar
JK
D019840:2-Propanol / Q000008:administration & dosage / Q000737:chemistry; D000279:Administration, Cutaneous; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D000818:Animals; D002046:Bupranolol / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D002463:Cell Membrane Permeability / Q000187:drug effects; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D008610:Menthol / Q000008:administration & dosage / Q000737:chemistry; D019946:Propylene Glycol / Q000008:administration & dosage / Q000737:chemistry; D011760:Pyrrolidinones / Q000008:administration & dosage / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000187:drug effects / Q000378:metabolism*; D012869:Skin Absorption / Q000187:drug effects; D013997:Time Factors; D014867:Water / Q000008:administration & dosage / Q000737:chemistry
D000319:Adrenergic beta-Antagonists; D004337:Drug Carriers; D011760:Pyrrolidinones; D014867:Water; D008610:Menthol; D019946:Propylene Glycol; D002046:Bupranolol; C038678:N-methylpyrrolidone; C028537:2-pyrrolidone; D019840:2-Propanol