title: Enhanced skin penetration of lidocaine through encapsulation into nanoethosomes and nanostructured lipid carriers: a comparative study.
abstract: Lipid based nanoparticles have become a major research object in topical drug delivery to enable drugs to pass the stratum corneum and reach the desired skin layer. The present investigation deals with the encapsulation of lidoacine into nanostructured lipid carriers (NLCs) and nanoethosomes for improving its dermal delivery and consequently local anesthetic efficacy. Concurrently these two topical delivery systems were compared. Lidocaine-loaded NLCs and nanoethosomes were characterized by various techniques and used for an in vitro skin penetration study using excised rat skin and Franz diffusion cells. The nanoparticles were tracked in the skin by following the Rhodamine-labled nanocarriers under fluorescent microscopy. Optimized lidocaine-loaded NLCs (size 96 nm, zeta potential -13.7 mV, encapsulation efficiency (EE) % 69.86% and loading capacity (LC) % 10.47%) and nanoethosomes (size 105.4 nm, zeta potential -33.6 mV, EE 40.14% and LC 8.02%) were chosen for a skin drug delivery study. Higher skin drug deposition of NLCs and nanoethosomal formulations compared to lidocaine hydroalcoholic solution represented a better localization of the drug in the skin. NLC formulation showed the lowest entered drug in the receptor phase of Franz diffusion cell in comparison with nanoethosomes and hydroalcoholic solution confirming the highest skin accumulation of drug. Both colloidal systems showed superiority over the drug solution for dermal delivery of lidocaine, however, NLC exhibited more promising characteristics than nanoethosomes regarding drug loading and skin targeted delivery.
authors.forename: S
authors.initials: S
authors.lastname: Babaei
authors.forename: S
authors.initials: S
authors.lastname: Ghanbarzadeh
authors.forename: Z M
authors.initials: ZM
authors.lastname: Adib
authors.forename: M
authors.initials: M
authors.lastname: Kouhsoltani
authors.forename: S
authors.initials: S
authors.lastname: Davaran
authors.forename: H
authors.initials: H
authors.lastname: Hamishehkar
mesh_terms: D000279:Administration, Cutaneous; D000779:Anesthetics, Local / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003102:Colloids / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D008012:Lidocaine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008055:Lipids / Q000737:chemistry*; D008297:Male; D008856:Microscopy, Fluorescence; D053758:Nanoparticles; D049329:Nanostructures; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012235:Rhodamines / Q000737:chemistry; D012869:Skin Absorption
chemical_list: D000779:Anesthetics, Local; D003102:Colloids; D004337:Drug Carriers; D008055:Lipids; D012235:Rhodamines; D008012:Lidocaine