Physically cross-linked chitosan hydrogels as topical vehicles for hydrophilic drugs.
Physically cross-linked chitosan hydrogels with lauric, myristic, palmitic or stearic acid were prepared by freeze-drying and have been studied for topical use. This study selected propranolol hydrochloride as a hydrophilic model drug to design a transdermal delivery system. We evaluated the effect of the nature of the cross-linker on drug permeation through porcine skin and the main permeation parameters (diffusion coefficient, flux and lag time) were calculated. All the chitosan hydrogels analysed provided more transcutaneous permeation of propranolol hydrochloride than the corresponding solution of the commercial drug. Among the different chitosan vehicles, chitosan-laurate and chitosan-myristate hydrogels enhanced lyophilised drug diffusion through the skin with respect to chitosan-palmitate and chitosan-stearate hydrogels. This can been explained by the interaction of the hydrogels with the stratum corneum, increasing the solubility of the drug in the skin.
Cerchiara
T
T
Department of Pharmaceutical Sciences, Bologna University, Via S. Donato 19/2, 40127 Bologna, Italy.
Luppi
B
B
Bigucci
F
F
Orienti
I
I
Zecchi
V
V
D000279:Administration, Cutaneous; D000818:Animals; D002686:Chitin / Q000031:analogs & derivatives* / Q000737:chemistry*; D048271:Chitosan; D003432:Cross-Linking Reagents / Q000737:chemistry*; D005612:Freeze Drying; D020100:Hydrogels / Q000737:chemistry*; D066298:In Vitro Techniques; D007848:Laurates / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D009226:Myristates / Q000737:chemistry; D010168:Palmitates / Q000737:chemistry; D010539:Permeability; D014677:Pharmaceutical Vehicles / Q000737:chemistry; D011433:Propranolol / Q000008:administration & dosage / Q000493:pharmacokinetics; D012869:Skin Absorption; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013228:Stearates / Q000737:chemistry; D013552:Swine; D014783:Viscosity
D003432:Cross-Linking Reagents; D020100:Hydrogels; D007848:Laurates; D009226:Myristates; D010168:Palmitates; D014677:Pharmaceutical Vehicles; D013228:Stearates; D002686:Chitin; D048271:Chitosan; D011433:Propranolol