Elastic liposomes mediated transdermal delivery of an anti-hypertensive agent: propranolol hydrochloride.
One major problem encountered in transdermal drug delivery is the low permeability of drugs through the skin barrier. In the present investigation ultradeformable lipid vesicles, that is, elastic liposomes were prepared incorporating propranolol hydrochloride for enhanced transdermal delivery. Elastic liposomes bearing propranolol hydrochloride were prepared by conventional rotary evaporation method and characterized for various parameters including vesicles shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, turbidity, and in vitro drug release. In vitro flux, enhancement ratio (ER), and release pattern of propranolol hydrochloride were calculated for transdermal delivery. In vivo study conducted on male albino rats (Sprague Dawley) was also taken as a measure of performance of elastic liposomal, liposomal, and plain drug solution. The better permeation through the skin was confirmed by confocal laser scanning microscopy (CLSM). Results indicate that the elastic liposomal formulation for transdermal delivery of propranolol hydrochloride provides better transdermal flux, higher entrapment efficiency, ability as a self-penetration enhancer and effectiveness for transdermal delivery as compared to liposomes.
Mishra
Dinesh
D
Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, Sagar (MP), 470003 India. dineshdops@yahoo.com
Garg
Minakshi
M
Dubey
Vaibhav
V
Jain
Subheet
S
Jain
N K
NK
D000279:Administration, Cutaneous; D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D015194:Diffusion Chambers, Culture; D004339:Drug Compounding / Q000379:methods; D004548:Elasticity; D006801:Humans; D007700:Kinetics; D008081:Liposomes; D008297:Male; D008560:Membrane Fluidity; D018613:Microscopy, Confocal; D009924:Organ Culture Techniques; D010316:Particle Size; D010539:Permeability; D010743:Phospholipids / Q000737:chemistry*; D011433:Propranolol / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption; D012995:Solubility; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry
D000959:Antihypertensive Agents; D008081:Liposomes; D010743:Phospholipids; D013501:Surface-Active Agents; D011433:Propranolol