Microemulsions Containing Medium-Chain Glycerides as Transdermal Delivery Systems for Hydrophilic and Hydrophobic Drugs

Hosmer, Jaclyn; Reed, Rachel; Bentley, Maria Vitória Lopes Badra; Nornoo, Adwoa O.; Lopes, Luciana B.

doi:10.1208/s12249-009-9251-0

Cited by 60 publications

(50 citation statements)

References 29 publications

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“…18,25 , or SLS at concentrations ranging from 0.15% to 5% (v/v) in the cell culture medium. PBS was used as the negative control at 1% concentration (v/v), while SLS was used as the positive control for all assays.…”

Section: Evaluation Of Cellular Viabilitymentioning

confidence: 99%

“…43 The ability of a microemulsion to improve the transport of drugs to and across the skin is mainly affected by the composition and concentration of the microemulsion components, as well as the internal structure and type (o/w, w/o, or bicontinuous systems) of the microemulsion used. 25 Oleic acid is one of the most frequently selected oils in microemulsions, and it has been demonstrated that microemulsions containing oleic acid increased the penetration of lipophilic drugs through the skin. 44 The permeation-enhancing effect of oleic acid has been reported to be more pronounced in oil in water (o/w)-type microemulsions, and the superiority of oleic acid to increase the release of lipophilic drugs from microemulsions has been shown.…”

Section: Figurementioning

confidence: 99%

See 1 more Smart Citation

Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations

Erdal¹,

Özhan²,

Mat³

et al. 2016

IJN

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In topical administration of antifungals, the drugs should pass the stratum corneum to reach lower layers of the skin in effective concentrations. Thus, the formulation of antifungal agents into a suitable delivery system is important for the topical treatment of fungal infections. Nanosized colloidal carriers have gained great interest during the recent years to serve as efficient promoters of drug penetration into the skin. Microemulsions are soft colloidal nanosized drug carriers, which are thermodynamically stable and isotropic systems. They have been extensively explored for the enhancement of skin delivery of drugs. This study was carried out to exploit the feasibility of colloidal carriers as to improve skin transport of naftifine, which is an allylamine antifungal drug. The microemulsions were formulated by construction of pseudoternary phase diagrams and composed of oleic acid (oil phase), Kolliphor ® EL or Kolliphor ® RH40 (surfactant), Transcutol ® (cosurfactant), and water (aqueous phase). The plain and drug-loaded microemulsions were characterized in terms of isotropy, particle size and size distribution, pH value, refractive index, viscosity, and conductivity. The in vitro skin uptake of naftifine from microemulsions was studied using tape stripping technique in pig skin. The drug penetrated significantly into stratum corneum from microemulsions compared to its marketed cream ( P <0.05). Moreover, the microemulsion formulations led to highly significant amount of naftifine deposition in deeper layers of skin than that of commercial formulation ( P <0.001). Microemulsion–skin interaction was confirmed by attenuated total reflectance – Fourier transformed infrared spectroscopy data, in vitro. The results of the in vivo tape stripping experiment showed similar trends as the in vitro skin penetration study. Topical application of the microemulsion on human forearms in vivo enhanced significantly the distribution and the amount of naftifine penetrated into the stratum corneum as compared to the marketed formulation ( P <0.05). The relative safety of the microemulsion formulations was demonstrated with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide viability test. This study indicated that the nanosized colloidal carriers developed could be considered as an effective and safe topical delivery system for naftifine.

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Section: Evaluation Of Cellular Viabilitymentioning

confidence: 99%

Section: Figurementioning

confidence: 99%

Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations

Erdal¹,

Özhan²,

Mat³

et al. 2016

IJN

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show abstract

“…For retention studies, the tape stripping method [13][14][15] was performed. The skins derived after 6 h and 12 h of permeation assay were cleaned using soft paper.…”

Section: Proof Of Concept Of the Formulations By Drug Release Drug Smentioning

confidence: 99%

Surfactant-based Transdermal System for Fluconazole Skin Delivery

Silva¹,

Luz²,

Satake³

et al. 2014

J Nanomed Nanotechnol

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The development of a controlled-release dosage form of antifungals is of crucial importance in view of the side-effects of conventional oral and intravenous treatments of Sporotrichosis. In this study, systems composed of polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol (PPG-5-CETETH-20) as a surfactant, oleic acid as an oil phase, and water were developed as a possible fluconazole transdermal drug delivery system. The systems were characterised by polarised light microscopy (PLM), SAXS, and rheological analysis, followed by cellular and histological analyses, in vitro release assays, and ex vivo skin permeation and retention studies using porcine ear tissue and a Franz diffusion cell. PLM and SAXS results indicated that the mixtures of surfactant, oil and water formed micellar and lamellar phases. The incorporation of fluconazole in these systems was greater than in water and conventional dosage forms. Micellar systems behave as Newtonian fluids, being more viscous than elastic in rheological analysis, and lamellar phases behave as pseudoplastic fluids with high elastic moduli. In vitro and in vivo biological assays showed that the formulations did not affect normal cell macrophages and did not promote skin irritation. The release profile indicated that fluconazole could be released in a controlled manner. It was found that the systems enhanced drug permeation and skin retention by changing only the composition of the components in the formulations. Therefore, PPG-5-CETETH-20-based systems have great potential as transdermal systems with different structural and rheological characteristics for Sporotrichosis treatment using antifungal drugs.vehicles. Surfactants are able to stabilise mixtures of components with different polarities, thus creating additional regions for hydrophilic and lipophilic solubilisation of drugs. The drug can be protected against the dissolution medium due to the interfacial membrane, which is composed of the surfactant layer that the drug must pass through to be released. In this manner, surfactant systems also confer reservoir properties. The phase behaviour of surfactants enable the formation of microemulsions and liquid crystals, which is extremely attractive for nanotechnology because these structures are organised on the nanometric scale. In addition to the advantage of increased stability, their production can be scaled up easily. Varying the composition and proportions of surfactant, oil, and aqueous phase, it is possible to control the viscosity and texture of the systems above, which could lead to the immobilisation or localisation of the formulation at specific sites in the body and routes of administration. Therefore, surfactant systems have great potential as transdermal nanostructured drug delivery systems [6].Recently, our research group has demonstrated that the surfactant polyoxypropylene (5)

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“…Various strategies have been employed to achieve delivery of drugs into skin. Among these strategies, microemulsions have been suggested to serve as efficient promoters of drug localization to skin [2][3][4] .…”

Section: Introductionmentioning

confidence: 99%