Lorena Tavano1, Elisabetta Mazzotta2, Rita Muzzalupo2. 1. Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via Pietro Bucci, Ed. Polifunzionale, 87036 Arcavacata di Rende, Italy. Electronic address: uclorena@tiscali.it. 2. Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via Pietro Bucci, Ed. Polifunzionale, 87036 Arcavacata di Rende, Italy.
Abstract
HYPOTHESIS: Due to the well-know surfactant-like properties of diclofenac sodium (DS), vesicular systems consisting exclusively of DS, named diclosomes, were designed with the aim to minimize or avoid the use of other excipients and to improve the formulation biocompatibility. EXPERIMENTS: Diclosomes were designed and characterized in terms of dimensions, polydispersity index, ξ-potential, drug retained, stability as a function of storage time and ex-vivo percutaneous permeation profiles. Additionally, diclosomes were incorporated into gel dosage forms and their performance in terms of permeation enhancement were evaluated. FINDINGS: DS was found to form nanosized vesicular systems, both alone and in presence of cholesterol. Increasing hydrophobicity (due to the presence of cholesterol) resulted in smaller vesicles, always spherical and homogeneous in shape. Permeation of DS from free solution was found to be lower respect to ones obtained for all diclosomal formulations, allowing these aggregates to be considered as percutaneous permeation enhancers. DS permeated from diclosomal gels was higher than that obtained with traditional niosomal gel, DS plain gel and commercial specialty Voltaren Emulgel® 1%, while containing a considerably lower drug amount.
HYPOTHESIS: Due to the well-know surfactant-like properties of diclofenac sodium (DS), vesicular systems consisting exclusively of DS, named diclosomes, were designed with the aim to minimize or avoid the use of other excipients and to improve the formulation biocompatibility. EXPERIMENTS: Diclosomes were designed and characterized in terms of dimensions, polydispersity index, ξ-potential, drug retained, stability as a function of storage time and ex-vivo percutaneous permeation profiles. Additionally, diclosomes were incorporated into gel dosage forms and their performance in terms of permeation enhancement were evaluated. FINDINGS:DS was found to form nanosized vesicular systems, both alone and in presence of cholesterol. Increasing hydrophobicity (due to the presence of cholesterol) resulted in smaller vesicles, always spherical and homogeneous in shape. Permeation of DS from free solution was found to be lower respect to ones obtained for all diclosomal formulations, allowing these aggregates to be considered as percutaneous permeation enhancers. DS permeated from diclosomal gels was higher than that obtained with traditional niosomal gel, DS plain gel and commercial specialty Voltaren Emulgel® 1%, while containing a considerably lower drug amount.