Characterizing In Vitro Permeation of Ibuprofen

Objective

To evaluate the uses of Labskin as an alternative to human or animal experimentation when characterizing in vitro permeation of Ibuprofen (IBU).

Method

  • Atatic glass Franz diffusion cells were used to mount Labskin. This was then equilibrated at 32 oC ±1 oC. The receptor phase used PBS. Figure 1.
  • Any excess surface water was removed and TEWL measurements were carried out using an AquaFlux AF200 (Biox Systems).
  • A test was carried out on infinite dose: 1mL of saturated IBU solution in propylene glycol (PG). After each sample receptor fluid was replaced.
  • An addition of finite dose: 3.6 μL of IBU solution (1.5% w/v in 5% PG : 95% isopropyl alcohol) was made to the donor compartment. Fresh PBS replaced the collected 200 μL samples.
  • A period of 24 hours was used to conduct all experiments and samples were assayed by UV-HPLC.

Results

  • Over the time- course of the experiments TEWL for Labskin remained constant. (Figure 2).
  • There was less variability demonstrated for Labskin (Figure 3) than that usually demonstrated by human or porcine skin and other human skin equivalent tissue culture models (Netzlaff, F., et al., European Journal of Pharmaceutics and Biopharmaceutics, 2005. 60: p.167-178)
  • Labskin demonstrated flux values for the infinite dose study (Figure 4) that were roughly 1.5 times higher than with human epidermis (Watkinson, R.M., et al., Skin Pharmacology and Physiology, 2009. 22: p. 225-230)
  • After application the total amount of IBU permeated across Labskin of 3.6 μL of the formulation was 46.2 μg cm-2 compared to 17 μg cm-2 across human epidermis (Figure 5)
Mounting in the receptor compartment of a Franz diffusion cell & Franz diffusion cell final assembly.

Figure 1. Mounting in the receptor compartment of a Franz diffusion cell & Franz diffusion cell final assembly.

TEWL values measured on Labskin, no formulation control for 24h infinite (●) and finite (▲) dose study.

Figure 2. TEWL values measured on Labskin, no formulation control for 24 h infinite () and finite () dose study.

Cumulative amount of ibuprofen permeated from a saturated solution of IBU in PG for 24 h across Labskin at 32 ºC

Figure 3. Cumulative amount of ibuprofen permeated from a saturated solution of IBU in PG for 24 h across Labskin at 32 ºC

Steady-state fluxes of ibuprofen through different membranes from saturated solutions in PG (mean ± SD)

Figure 4. Steady-state fluxes of ibuprofen through different membranes from saturated solutions in PG (mean ± SD)

Cumulative amount IBU permeated from 95:5:1.47 (IPA:PG:IBU) solution over 24 h across Labskin (◼) and human epidermis (◆) at 32 °C (n=5, Mean ± SD)

Figure 5. Cumulative amount IBU permeated from 95:5:1.47 (IPA:PG:IBU) solution over 24 h across Labskin () and human epidermis () at 32 °C (n=5, Mean ± SD)

Summary

Whilst IBU permeated more quickly through Labskin than human skin in vitro, permeability is comparable to porcine ear tissue, which is the closest animal model to human skin.

About Labskin

At Labskin we deliver human skin microbiology services to support your product R&D activities in the cosmetic, personal care, medical device and pharmaceutical sectors. With our sector experience and use of technology, you will be accessing industry-focused services supported by world-leading skin science expertise.

Whether you need rapid, focused analysis or flexible, tailor-made research programs we can help you develop and validate skincare ingredients and products which really work.

Our skin model is a 3D human skin equivalent that incorporates vital biological components to model normal skin function.

Developed over 12 years with more than 30 scientific journal publications, it is made from young keratinocytes (human skin cells) and adult fibroblasts (metabolically-active, collagen-producing human skin cells).

“An ideal platform for basic or applied skin research, testing compounds or formulated products for the cosmetic, pharmaceutical and chemical sectors.”


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Last updated: Oct 28, 2019 at 4:43 AM

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