Dynamic in-situ eutectic formation for topical drug delivery

Fiala, Sarah; Brown, Marc; Jones, Stuart A.

doi:10.1111/j.2042-7158.2011.01346.x

Cited by 11 publications

(4 citation statements)

References 26 publications

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“…Another important physicochemical drug characteristic in transdermal drug delivery is the melting point of the applied compound [36,37]. Substances with low melting points exhibit a high solubility in epidermal lipids, which in turn provides a higher thermodynamic activity for percutaneous permeation.…”

Section: Discussionmentioning

confidence: 99%

Microneedle pretreatment enhances the percutaneous permeation of hydrophilic compounds with high melting points

Stahl

Wohlert

Kietzmann

2012

BMC Pharmacol Toxicol

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BackgroundTwo commercially available microneedle rollers with a needle length of 200 μm and 300 μm were selected to examine the influence of microneedle pretreatment on the percutaneous permeation of four non-steroidal anti-inflammatory drugs (diclofenac, ibuprofen, ketoprofen, paracetamol) with different physicochemical drug characteristics in Franz-type diffusion cells. Samples of the receptor fluids were taken at predefined times over 6 hours and were analysed by UV–VIS high-performance liquid-chromatography. Histological examinations after methylene blue application were additionally performed to gather information about barrier disruption.ResultsDespite no visible pores in the stratum corneum, the microneedle pretreatment resulted in a twofold (200 μm) and threefold higher (300 μm) flux through the pretreated skin samples compared to untreated skin samples for ibuprofen and ketoprofen (LogKow > 3, melting point < 100°C). The flux of the hydrophilic compounds diclofenac and paracetamol (logKow < 1, melting point > 100°C) increased their amount by four (200 μm) to eight (300 μm), respectively.ConclusionCommercially available microneedle rollers with 200–300 μm long needles enhance the drug delivery of topically applied non-steroidal anti-inflammatory drugs and represent a valuable tool for percutaneous permeation enhancement particularly for substances with poor permeability due to a hydrophilic nature and high melting points.

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Section: Discussionmentioning

confidence: 99%

Microneedle pretreatment enhances the percutaneous permeation of hydrophilic compounds with high melting points

Stahl

Wohlert

Kietzmann

2012

BMC Pharmacol Toxicol

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“…We selected the column Gemini ® C18 because of its low polarity, moderate hydrophobicity and stability at extreme pH conditions (1-12). This column is ideal for the separation of basic compounds at high pH and probably for this reason it has been widely used in the analysis of local anesthetics (Fiala et al, 2008;Moraes et al, 2009;Fiala et al, 2010;Fiala et al, 2011).…”

Section: Methods Developmentmentioning

confidence: 99%

A simple and high‐resolution HPLC‐PDA method for simultaneous quantification of local anesthetics in in vitro buccal permeation enhancement studies

Couto

Cubayachi

Lopez

et al. 2015

Biomedical Chromatography

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A simple, isocratic, high-resolution and prompt HPLC-PDA method was developed and validated for the simultaneous quantification of prilocaine (PCL) and lidocaine (LCL) hydrochlorides in in vitro buccal iontophoresis-driven permeation studies. A reversed-phase C18 column (250 mm x 4.6 mm, 3μm, 110Å) was used for the chromatographic separation. The mobile phase contained acetonitrile: 0.1M sodium phosphate buffer, pH 7.0 (1:1, v/v), plus 0.05% (v/v) diethylamine. The isocratic flow rate was set at 1 mL/min and the detection wavelength was 203 nm. PCL and LCL eluted in 8.9 min and 13 min, respectively, and the system suitability parameters varied within an acceptable range. The method was selective, sensitive, precise, accurate and robust, producing a linear plot at the concentration range of 0.25 to 10 µg/mL. The application of this method was demonstrated by a significant enhancement of the permeation of PCL and LCL with the application of iontophoresis (1 mA/cm(2) per 1 h) through isolated porcine esophageal epithelium. The amount of the drug retained in the epithelium also increased with the application of an electrical current. Copyright © 2015 John Wiley & Sons, Ltd.

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“…Mixtures with a eutectic composition are important in many industries including pharmaceutical, thermosetting resins formulation, or metallic alloys as lower solid-to-liquid temperature enables better processability [21][22][23][24][25].…”

Section: Scheme 1 Functionalization Of Ddsq-oh 4 With Dichlorosilanesmentioning

confidence: 99%

Phase Behavior of Selected Condensed Double-Decker Shaped Silsesquioxane Compounds

Vogelsang

Maleczka

Lee

2021

Preprint

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Bisfunctional dichlorosilanes were reacted with tetrasilanol of double-decker shaped octaphenylsilsesquioxane (DDSQ) to form fully condensed DDSQ compounds. The crystallographic and thermal characteristics of these compounds were examined. For compounds capped with dichlorosilanes bearing linear aliphatic moieties, as the number of carbon increases from methyl to n-butyl (from 1 to 4) the melting temperature, Tm, dropped from 546 K to 416 K. While for compounds capped with cycloaliphatic, as the moiety changes from cyclopentyl to cyclohexyl, the value of Tm increases from 533 K to 555 K. Surprising, the highest Tm observed was that when capping was done using diisopropyl dichlorosilane. A Tm of around 565 K was observed, which was even higher as compare to diphenyl dichlorosilane capped DDSQ, which had Tm of about 526 K. Phase behavior of binary and ternary mixtures of these condensed DDSQ was also investigated. To our surprise, mixtures of these compounds form eutectic. The eutectic points were calculated based on ideal binary and ternary eutectic from the thermal properties of pure components. Depending on the crystallography, experimental observations of eutectic match well with calculated values.

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Dynamic in-situ eutectic formation for topical drug delivery

Cited by 11 publications

References 26 publications

Microneedle pretreatment enhances the percutaneous permeation of hydrophilic compounds with high melting points

Microneedle pretreatment enhances the percutaneous permeation of hydrophilic compounds with high melting points

A simple and high‐resolution HPLC‐PDA method for simultaneous quantification of local anesthetics in in vitro buccal permeation enhancement studies

Phase Behavior of Selected Condensed Double-Decker Shaped Silsesquioxane Compounds

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