title: Cromolyn as surface active drug (surfadrug): Effect of the self-association on diffusion and percutaneous permeation.
abstract: Cromolyn sodium, or disodium cromoglycate (CS), is a surface active drug: a pharmacologically active compound with an amphiphilic nature. At certain conditions it is able to self-associate in several kind of supramolecular aggregates. Since CS could play the role of both carrier and drug, bypassing the use of additional excipients and increasing the system biocompatibility, the effects of cromolyn self-aggregates on diffusion and percutaneous permeation across rabbit ear skin were investigated. Niosomes (vesicular systems, 0.5wt% of CS), monomeric and isotropic solutions (0.5 and 5wt% of CS), nematic (15wt% of CS) and hexagonal phases (30wt% of CS) were selected as supramolecular systems and tested as transdermal delivery systems. Results demonstrated that CS was able to form vesicular structures of about 500nm of diameter and this formulation gave the higher percutaneous permeation profile (systemic action), while isotropic solution and liquid crystals mesophases acted as slower release reservoir of drug on the skin surface (local action), as confirmed by diffusion coefficients. Diffusion rates through a synthetic membrane were dependent both on CS concentration present into the formulations and on its structural organization: maximum diffusion was noticed with isotropic solution, a lower amount of diffused cromolyn sodium was achieved by hexagonal phase. Consequently, CS appears as a versatile surfadrug as, depending on the disease degree, it is possible to modulate its permeation profile by choosing the most appropriate formulation.
authors.affiliation: Department of Pharmacy, Health and Nutrition Sciences University of Calabria, Arcavacata di Rende, Cosenza 87036, Italy. Electronic address: uclorena@tiscali.it.
authors.forename: Lorena
authors.initials: L
authors.lastname: Tavano
authors.affiliation: Department of Pharmacy, Health and Nutrition Sciences University of Calabria, Arcavacata di Rende, Cosenza 87036, Italy.
authors.forename: Fiore Pasquale
authors.initials: FP
authors.lastname: Nicoletta
authors.affiliation: Department of Pharmacy, Health and Nutrition Sciences University of Calabria, Arcavacata di Rende, Cosenza 87036, Italy.
authors.forename: Nevio
authors.initials: N
authors.lastname: Picci
authors.affiliation: Department of Pharmacy, Health and Nutrition Sciences University of Calabria, Arcavacata di Rende, Cosenza 87036, Italy. Electronic address: rita.muzzalupo@unical.it.
authors.forename: Rita
authors.initials: R
authors.lastname: Muzzalupo
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D004205:Cromolyn Sodium / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D004058:Diffusion; D004423:Ear; D008081:Liposomes / Q000737:chemistry / Q000494:pharmacology*; D010539:Permeability; D044367:Phase Transition; D011817:Rabbits; D012867:Skin / Q000187:drug effects* / Q000378:metabolism; D012869:Skin Absorption / Q000502:physiology; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D008081:Liposomes; D013501:Surface-Active Agents; D004205:Cromolyn Sodium
keywords: Cromolyn sodium; Diffusion; Liquid crystals; Niosomes; Permeation