Optimising product performance through the combination of innovative formulations and

cutting edge technology

InnoCosmetics Europe Thursday 7th October 2010

Dr Mark I EdwardsDirector Biosciences and Idea Evolution,

GSK Consumer Healthcare

Optimising product performance through the combination of innovative formulations and cutting

edge technology

InnoCosmetics Europe Thursday 7th October 2010

Dr Mark EdwardsDirector Biosciences and Idea Evolution,

GSK Consumer Healthcare

This talk will:

• Include examples of innovative high performance and effective formulations

• Demonstrate the use of cutting edge technology to driving new product development and formulation

• Show the importance of choosing the right ingredients for the targeted benefit

Overview

Optimising product performance through innovative formulation:

Dental erosion is commonly defined as the chemical dissolution of dental hard tissues by methods other than those involving bacterial acid production, the role of dietary acids as a major contributor to this process is well established 1,2. Enamel is the hard, protective coating of the tooth, when the enamel is worn away, the dentine underneath is exposed, which may lead to pain and sensitivity.

Enamel loses mineral content

and becomes surface softened

Saliva neutralizes and slowly replaces

mineral

However frequent attack by dietary

acids leads to significant surface

softening

Formulation Goal – To Reduce Enamel & Dental Erosion

DentalErosion

1. Zero DT, Lussi A: Erosion – chemical and biological factors of importance to the dental practitioner. Int Dent J 55:285-290, 2005.2. Lussi A. (Ed.) Dental Erosion: From Diagnosis to Therapy. Monographs in Oral Science Vol 20. Pub: Karger, Basel, 2006.

Abrasion e.g. brushing

& Attrition e.g.

tooth grindingresult in enamel

loss

Once enamel is lost it can

not be replaced

Intake of acidic

food or drink

Optimising Product Performance

Pronamel does this by maximising the ‘free’ or available fluoride in the formulation. This is important because:

• Tooth enamel is composed of hydroxyapatite (HAP), Ca10(PO4)6(OH)2

• Fluoride treatment creates fluorapatite Ca10(PO4)6F2 • Fluorapatite is harder and more resistant to acid attack that HAP.• The greater the amount and depth of fluorapatite formed the

more resistant the tooth is to enamel softening and loss on exposure to dietary acids.

Formulation Optimisation

The formulation is optimised for ‘free’ or available fluoride by:

• minimising interaction with other ingredients in the formulation:– Abrasive system– Detergent– Thickening agents

• Using sodium fluoride as the source of fluoride in the formulation

• Ingredients: Aqua, sorbitol, hydrated silica, glycerin, potassium nitrate, PEG-6, cocamidopropyl betaine, aroma, xanthan gum, sodium saccharin, sodium fluoride, titanium dioxide, sodium hydroxide, limonene, anise alcohol.

• sodium fluoride (1450 ppm fluoride), potassium nitrate (5% w/w)

Optimising product performance through cutting edge technology – Dynamic Secondary Ion Mass Spectroscopy

(DSIMS)

• Semi quantitative information about depth of F penetration into enamel

1400ppm Fluoride1000ppm Fluoride

0ppm Fluoride

Measuring Fluoride Penetration via DSIMs - Dose Response Study

DSIMS - Dose Response Study

Plot of SIMS ratio [(F/F+P) x2000] vs. Fluoride dose

0

200

400

600

800

1000

1200

1400

0 200 400 600 800 1000 1200 1400 1600

Fluoride Dose (ppm)

SIM

S R

atio

(F/F

+P) x

2000

Poster Presentation: International Association Dental Research, General Meeting, New Orleans, March 21 st - 24th 2007

Formulation –The Effect of Different Fluoride Salts on Fluoride Penetration into Enamel using DSIMS

• All fluoride containing toothpastes leads to fluoride penetration and incorporation into the surface of enamel.

• Fluoride penetration was significantly greater (49-150%) for pastes containing sodium fluoride alone vs. those based on Amine Fluoride, Stannous Fluoride or Sodium Fluoride in combination with pyrophosphate.

A: Paste 1 treated (NaF) B: Paste 2 treated (NaF + Sodium Pyroposphate)

C: Paste 3 treated (NaF + KNO3) D: Paste 4 treated (SnF2)

E: Paste 5 Treated (AmF)

Correlating Physical Properties (Rehardening) of Enamel to Fluoride Uptake Using DSIMS Imaging

Fluoride incorporation was deeper in samples treated with the new formulation (~60mm* vs. 5mm).

The degree of fluoride incorporation into enamel corresponded with the extent of rehardening of surface softened enamel.

Fluoride-freeControl toothpaste

Commercial toothpasteNew Formulation toothpaste

Overlay Image for new testdesensitising toothpaste (F- red, C2H- blue)

Poster Presentation: IADR Pan European Federation Meeting, Dublin , 2006

Nanometer = one billionth of a meter

* Micron = one millionth of a meter

Incorporating polymers optimise product performance in a mouthwash formulation

• Maximises the ‘free’ or available fluoride in the formulation

• Tri-Hydra™ a three polymer system - xanthan gum, carboxymethyl cellulose, copovidone

• These polymers provide greater enamel fluoride uptake

Ingredients: aqua, glycerin, sorbitol, poloxamer 3381, PEG-60 hydrogenated castor oil, VP/VA copolymer2, potassium nitrate, sodium benzoate, cellulose gum, aroma, sodium fluoride, methylparaben, propylparaben, cetylpyridinium chloride, sodium saccharin, xanthan gum, disodium phosphate, sodium phosphate, CI 42090, sodium fluoride

1. Polyethylene-Polypropylene Glycol

2. Polyvinylpyrrolidone/Vinyl Acetate (VP/VA) Copolymer

Fluoride layer

300 ppm F + 3 Polymer System

Distance (µm) Distance (µm)

16O-19F-12C21H31P

300 ppm F

DSIMS to Measure Enhancement of Fluorideby the Three Polymer System

Optimising product performance through cutting edge technology - White Light Interferometry Non Contact Surface Profiling

Quantitative assessment of shape, texture and topography (nm height resolution)

Enables acid based enamel surface damage/damage prevention to be determined

White Light Interferometry - Untreated Human Enamel

White Light Interferometry - Human Enamel Treated with 1% Citric Acid pH3.8 for 5 Minutes

Water

300ppm F + 3 Polymer System

3 Polymer System

300ppm F

White Light Interferometry to Measure Erosion Inhibition

Poster Presentation: International Association Dental Research, General Meeting Miami Florida, April 1-4 2009

Publications:

• Pronamel toothpaste and mouthwash have been used as examples of innovative high performance and effective formulations

• The use of new technology to driving new product development and formulation has been shown by: • DSIMS • White light inferometry• Tri-Hydra™ three polymers system used in Pronamel

mouthwash

• Sodium fluoride: an example showing the importance of choosing the right ingredients for the targeted benefit

• Pronamel toothpaste and mouthwash demonstrate the importance of careful formula ingredient choice to ensure optimal final performance of the product

Summary

Acknowledgements:

• Dr Chris Fowler, GSK Consumer Healthcare• Dr Charles Parkinson, GSK Consumer Healthcare• Dr Louise Gracia, GSK Consumer Healthcare• Dr Alan Brown CERAM, Stoke-on-Trent• Dr Simon Shenton CERAM, Stoke-on-Trent

Vielen DankThank you

Questions?

Carbopol Xanthan

Sodium Lauryl Sulphate Tego Betaine