Effect of formulations variables on the in vitro percutaneous permeation of Sodium Diclofenac from new vesicular systems obtained from Pluronic triblock copolymers.
The objectives of our study were to evaluate the ability of Pluronic L64 surfactant to give niosomal systems alone or after its functionalization with acrylic groups. The achieved formulations were tested for the percutaneous permeation of Sodium Diclofenac as model drug. In vitro experiments were conducted by Franz diffusion cells, using rabbit ear skin. Data recorded over 24h were compared with those obtained from the drug solution, as control. In addition, the stability of niosomes was improved polymerizing the acryloyl groups of the monomers, because, as reported in the literature, polymerized vesicles maintain their shape for long periods of time, and show remarkable increase in drug encapsulation efficiency. Mean vesicles diameter, drug entrapment efficiency, percutaneous permeation and release profiles were investigated for all vesicles with different composition. The results indicated an increase in mean vesicles diameter and entrapment efficiency with the increase of polymerizable moieties amount. These properties were found to be more evident when the vesicles were polymerized. In addition cytotoxic effects were estimated. The results of this study showed that niosomes based on commercial, functionalized or a mixture of both Pluronic L64 surfactants can be used to achieve retarded release and to enhance the permeation of Sodium Diclofenac, without incurring unacceptable toxicity.
Tavano
Lorena
L
Dipartimento di Scienze Farmaceutiche Università della Calabria, Ponte P. Bucci, Ed. Polifunzionale, 87030 Rende, Italy.
Muzzalupo
Rita
R
Trombino
Sonia
S
Cassano
Roberta
R
Pingitore
Attilio
A
Picci
Nevio
N
D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004008:Diclofenac / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods; D066298:In Vitro Techniques; D007700:Kinetics; D008081:Liposomes / Q000737:chemistry / Q000648:ultrastructure; D046529:Microscopy, Electron, Transmission; D010539:Permeability; D020442:Poloxamer / Q000737:chemistry*; D011817:Rabbits; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption
D000894:Anti-Inflammatory Agents, Non-Steroidal; D008081:Liposomes; D020442:Poloxamer; D004008:Diclofenac; C514452:pluronic L64