Development of terbinafine solid lipid nanoparticles as a topical delivery system

Abstract

Abstract:To resolve problems of long treatment durations and frequent administration of the antifungal agent terbinafine (TB), solid lipid nanoparticles (SLNs) with the ability to load lipophilic drugs and nanosize were developed. The SLNs were manufactured by a microemulsion technique in which glyceryl monostearate (GMS), glyceryl behenate (Compritol ® 888; Gattefossé), and glyceryl palmitostearate (Precirol ® ATO 5; Gattefossé) were used as the solid lipid phases, Tween ® and Cremophor ® series as the surfactants, and propylene glycol as the cosurfactant to construct ternary phase diagrams. The skin of nude mice was used as a barrier membrane, and penetration levels of TB of the designed formulations and a commercial product, Lamisil ® Once™ (Novartis Pharmaceuticals), in the stratum corneum (SC), viable epidermis, and dermis were measured; particle sizes were determined as an indicator of stability. The optimal SLN system contained a ,5% lipid phase and .50% water phase. The addition of ethanol or etchants had no significant effect on enhancing the amount of TB that penetrated the skin layers, but it was enhanced by increasing the percentage of the lipid phase. Furthermore, the combination of GMS

Recent advances in topical formulation carriers of antifungal agents

“…[27,28] The amount of terbinafine penetrating deep into the skin and reaching the dermis was higher for solid lipid nanoparticles compared to the marketed Lamisil ® cream. [29] Similar results were obtained with solid lipid nanoparticles of econazole. [30] Moreover, solid lipid nanoparticles of griseofulvin were shown to exhibit good skin permeation effect as manifested by the complete mycological and clinical cure in Microsporum canis infected guinea pigs upon administration of griseofulvin solid lipid nanoparticles gel twice daily for 8 days.…”

Evaluation of the Permeation and Penetration of Two Formulations of Terbinafine Chlorhydrate Incorporated in Liposomes (Cream 1%) vs. a Conventional Formulation (Cream 1%), in an <i>in Vitro-ex Vivo</i> Model

“…All the pharmacokinetic processes of absorption, distribution and elimination require the passage of the molecules of the drug through membranes (biological or synthetic). In vitro permeation studies are commonly used in trials that evaluate the delivery of drugs via topical [25] [26].…”

Superficial Dermatophytosis across the World’s Populations: Potential Benefits from Nanocarrier-Based Therapies and Rising Challenges

“…The aforementioned formulation exhibited enhanced permeability, thereby enabling a decrease in the frequency of dosage and mitigation of adverse effects. Consequently, the utilization of this particular mode of drug administration amplifies the safety, cost-efficiency, and tolerability of antifungal treatment Figure illustrates several other advantages of drug delivery systems utilizing nanocarriers in comparison to conventional treatments.…”