Topical delivery of niacinamide: Influence of neat solvents

Iliopoulos, Fotis; Sil, Bruno C.; Hossain, Amjad; Moore, David J.; Lucas, Robert A.; Lane, Majella E.

doi:10.1016/j.ijpharm.2020.119137

Cited by 24 publications

(21 citation statements)

References 41 publications

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“…The saturation solubility of EA was higher in complex solvent systems with solubility parameters close to those of EA (15.4 ((cal/cm 3 ) 1/2 ). This is consistent with previous findings on EA saturation solubility in neat solvents, as well as with reports on the solubility of other compounds [5,14,15]. For binary solvent systems, EA solubility ranged from 64.4 ± 4.0 mg/mL to 550.4 ± 9.5 mg/mL, while for ternary solvent systems, EA solubility ranged from 104.6 ± 23.6 mg/mL to 340.9 ± 16.4 mg/mL ( Figure 1).…”

Section: Miscibility Of Solvents Solubility Parameter Values and Sosupporting

confidence: 93%

Topical Delivery of 3-O-ethyl l-ascorbic Acid from Complex Solvent Systems

et al. 2020

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3-O-ethyl l-ascorbic acid (EA), an ether derivative of Vitamin C, is widely used in skincare formulations. Previously, we reported the effects of neat solvents on EA percutaneous absorption and observed that 0.6–7.5% of the applied EA was delivered through the skin over 24 h. In this work, we designed complex formulations using combinations of solvents that may act synergistically and examined their impact on EA permeation in porcine skin in vitro under finite dose conditions. Binary combinations of propylene glycol (PG) with propylene glycol monolaurate (PGML) were effective in enhancing skin permeation of EA compared with individual solvents (p < 0.05). Combining PGML with 1,2-hexanediol (HEX) did not result in significantly higher EA permeation compared with the neat solvents (p > 0.05). Addition of the volatile solvent isopropyl alcohol (IPA) to PG solutions also did not improve EA skin delivery compared with neat PG. Ternary solvent systems containing PG:PGML were subsequently prepared by the addition of a lipophilic solvent, either isopropyl myristate (IPM), medium-chain triglycerides (MCT) or isostearyl isostearate (ISIS). The optimum vehicle, PG:PGML:IPM, promoted up to 70.9% skin delivery of EA. The PG:PGML:ISIS vehicles also promoted EA permeation across the skin, but to a significantly lesser extent than the IPM-containing vehicles. No enhancement of EA delivery was noted for the PG:PGML:MCT mixtures. These results will inform the development of targeted formulations for EA in the future.

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Section: Miscibility Of Solvents Solubility Parameter Values and Sosupporting

confidence: 93%

Topical Delivery of 3-O-ethyl l-ascorbic Acid from Complex Solvent Systems

et al. 2020

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“…The HPLC method for the analysis of NIA has been reported and validated in earlier work [ 29 ]. Briefly, analysis was performed using a Luna ® reverse phase column, 250 × 4.60 mm, 5 μm, Phenyl-Hexyl (Phenomenex, Macclesfield, UK), and a universal HPLC guard column (Phenomenex, Macclesfield, UK) packed with a SecurityGuard™ cartridge (Phenomenex, Macclesfield, UK).…”

Section: Methodsmentioning

confidence: 99%

“…Solutions of NIA (3% w / w ) were prepared in three formulations: TC, PG:PGML (0.75:0.25), and PG:PGML:IPM (0.65:0.30:0.05). This concentration of NIA is commonly used in topical preparations [ 26 ], and these formulations are known to promote NIA permeation through skin [ 29 , 32 ]. The selection of TC as a single solvent was based on its reported efficacy in promoting NIA skin delivery compared with other neat solvents [ 29 ].…”

Section: Methodsmentioning

confidence: 99%

“…This concentration of NIA is commonly used in topical preparations [ 26 ], and these formulations are known to promote NIA permeation through skin [ 29 , 32 ]. The selection of TC as a single solvent was based on its reported efficacy in promoting NIA skin delivery compared with other neat solvents [ 29 ]. Prior to the permeation experiments, a section of frozen skin was cut and placed in a basin of distilled water.…”

Section: Methodsmentioning

confidence: 99%

“…At the end of the permeation experiments, mass balance studies were conducted to measure the amounts of NIA on the surface and inside the skin, according to procedures described previously [ 29 , 32 ]. Briefly, the skin surface was washed with three consecutive 1 mL volumes of water:methanol (50:50, v / v ) and was subsequently dried with a cotton swab.…”

Section: Methodsmentioning

confidence: 99%

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Franz Cell Diffusion Testing and Quantitative Confocal Raman Spectroscopy: In Vitro-In Vivo Correlation

2020

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Previously, we reported the use of Confocal Raman Spectroscopy (CRS) to investigate the topical delivery of actives and excipients. We have also correlated the results from CRS with findings from in vitro diffusion studies in human skin. However, until now CRS has only been used as a semi-quantitative method of determining the skin uptake of molecules, with results expressed as arbitrary units of signal intensity. Clearly, this posed challenges for using CRS to determine skin delivery and to assess the drug bioavailability and bioequivalence of topical formulations. In the present work, the permeation of niacinamide (NIA) from various formulations in human skin was studied in vitro using conventional Franz cells and in vivo using a quantitative CRS method under finite dose conditions. The selection of NIA was based on its wide use in pharmaceutical and personal care formulations for many years. This is the first fully quantitative study to compare these methods. The vehicles investigated were neat Transcutol® P (TC); binary combinations of propylene glycol (PG) with propylene glycol monolaurate (PGML); and ternary mixtures of PG, PGML, and isopropyl myristate (IPM). These solvents were selected to encompass a range of physicochemical properties. NIA permeation was evident from all formulations in vitro and in vivo. The vehicles PG:PGML and PG:PGML:IPM delivered comparable amounts across the skin in vitro at 24 h (100.3–106.7 µg/cm2, p > 0.05) that were significantly higher compared with those of TC (1.3 µg/cm2, p < 0.05). An excellent in vitro in vivo correlation (R2 = 0.98) was found following the linear regression of the cumulative amounts of NIA permeated in vitro and the amounts of NIA at 2 μm in the skin measured with CRS. A very good correlation between the cumulative permeation of NIA in vitro and the total amount of NIA that penetrated the stratum corneum (SC) per unit of surface area (μg/cm2) in vivo was also observed, with a Pearson correlation coefficient (R2) of 0.94. The findings support the use of CRS for the quantitative measurement of actives delivered to the skin in vivo. Future studies will focus on exploring the reproducibility and reliability of the method by investigating the delivery of different actives from a wider range of vehicles. Additionally, quantitative CRS will be evaluated further as a method for assessing the bioequivalence of topical formulations.

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A Conformable Ultrasound Patch for Cavitation‐Enhanced Transdermal Cosmeceutical Delivery

Shah

Amiri

et al. 2023

Advanced Materials

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Increased consumer interest in healthy‐looking skin demands a safe and effective method to increase transdermal absorption of innovative therapeutic cosmeceuticals. However, permeation of small‐molecule drugs is limited by the innate barrier function of the stratum corneum. Here, a conformable ultrasound patch (cUSP) that enhances transdermal transport of niacinamide by inducing intermediate‐frequency sonophoresis in the fluid coupling medium between the patch and the skin is reported. The cUSP consists of piezoelectric transducers embedded in a soft elastomer to create localized cavitation pockets (0.8 cm2, 1 mm deep) over larger areas of conformal contact (20 cm2). Multiphysics simulation models, acoustic spectrum analysis, and high‐speed videography are used to characterize transducer deflection, acoustic pressure fields, and resulting cavitation bubble dynamics in the coupling medium. The final system demonstrates a 26.2‐fold enhancement in niacinamide transport in a porcine model in vitro with a 10 min ultrasound application, demonstrating the suitability of the device for short‐exposure, large‐area application of sonophoresis for patients and consumers suffering from skin conditions and premature skin aging.

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Topical delivery of niacinamide: Influence of neat solvents

Cited by 24 publications

References 41 publications

Topical Delivery of 3-O-ethyl l-ascorbic Acid from Complex Solvent Systems

Topical Delivery of 3-O-ethyl l-ascorbic Acid from Complex Solvent Systems

Franz Cell Diffusion Testing and Quantitative Confocal Raman Spectroscopy: In Vitro-In Vivo Correlation

A Conformable Ultrasound Patch for Cavitation‐Enhanced Transdermal Cosmeceutical Delivery

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