Influence of Vehicles and Penetration Enhancers on the Permeation of Cinnarizine Through the Skin

Objectives: The aim of this study was to determine the influence of vehicles and penetration enhancers on the penetration and permeation of cinnarizine (CNZ) through the skin. Materials and Methods: Topical formulations based on hydrogel, o/w emulsion and oleaginous cream were prepared. After determination of physical properties of formulations, the penetration and permeation of CNZ through the stratum corneum and full-thickness skin was investigated by an ex vivo study. Results: The cumulative amount of CNZ permeated from the base hydrogel formulation was about 5 times higher than the base o/w emulsion and base oleaginous cream formulations. The incorporation of penetration enhancers to the base hydrogel and o/w emulsion formulations generally increased CNZ penetration through the skin. Transcutol® was confirmed to provide the highest penetration in the hydrogel formulation. Propylene glycol was found to be the most suitable penetration enhancer for CNZ in the oleaginous cream. Glycerol and oleic acid displayed the highest effect in the o/w emulsion. Conclusion: It was concluded that the hydrogel containing Transcutol® provided the highest penetration through the skin among all formulations and this formulation could be an alternative to the oral route in the treatment of Ménière's disease and motion sickness. Thus, the risk of systemic side effects caused by oral medication can be reduced or eliminated.

Development of monolithic matrix type transdermal patches containing cinnarizine: Physical characterization and permeation studies

To overcome the problems associated with bioavailability and systemic side effects of the drug by oral administration, monolithic matrix type transdermal patches containing cinnarizine (CNZ) were developed. For this purpose, films based on hydroxypropyl methylcellulose and polyvinylpyrrolidone as matrix-forming polymers were designed. Physical characteristics of transdermal films and drug-excipient compatibility were investigated. Factors affecting in vitro drug release and ex vivo skin penetration and permeation of the drug were studied. It was confirmed that films displayed sufficient flexibility and mechanical strength for application onto the skin for a long time period. Ex vivo penetration experiments gave satisfactory results for transdermal drug delivery through rat skin. The parameters determining good skin penetration were also evaluated. The highest drug permeation rate was obtained with incorporation of Transcutol® (0.102 mg/cm2/h) into the base CNZ formulation, followed by propylene glycol (0.063 mg/cm2/h), menthol (0.045 mg/cm2/h), and glycerin (0.021 mg/cm2/h) as penetration enhancers (p < 0.05). As a result, the developed transdermal patches of CNZ may introduce an alternative treatment for various conditions and diseases such as idiopathic urticarial vasculitis, Ménière's disease, motion sickness, nausea, and vertigo. Thus, the risk of systemic side effects caused by the drug can be reduced or eliminated

Therapeutic potential of drug delivery by means of lipid nanoparticles: reality or illusion?

BACKGROUND: Solid lipid nanoparticles (SLN) are colloidal drug carrier systems that contribute several properties required from a sophisticated drug delivery system for increasing drug bioavailability and providing effective therapy. Many advantages of SLN have been reported over traditional dosage forms and their colloidal counterparts in the studies since the early 1990s. They were optimized for oral drug delivery for the first time. The first SLN formulations were produced by reducing the particle size of solid lipid microparticles by spray congealing technique in the late 1980s. Then, studies have been continued investigating for their different administration routes else including parenteral, transdermal, ocular, nasal, respiratory etc. METHODS: Their foremost qualifications such as their biocompatible nature and high drug entrapment efficiency make them promising colloidal drug carrier systems for the effective treatment of serious disasters like genetic disorders and cancer. CONCLUSION: In this review, therapeutic potential of drug delivery of SLN and nanostructured lipid carriers (NLC, the second generation of SLN) are summarized considering researches and patents on their administration via different routes and their preparations in the pharmaceutical market.