30 PRESERVATIVES
used as a natural antimicrobial and anti- inflammatory agent especially in preparations for the hair and the mouth. For several years it has been possible only to source a synthetic nature-identical form of this molecule. However, GreenPharma has now
brought to the market a sustainable and environmental-friendly product, which makes use of waste material of the tree. In fact, the Hiba cedar wood, also known as Aomori Hiba or Asunaro, is an ornamental tree grown in Japan for its valuable wood, which is durable and scented. Using the sawdust produced when
working the tree for human activities seemed a sensible solution aimed at the valorisation of a by-product which is still rich in the molecule of interest, while, in the meantime, helping preserve a precious natural resource. Besides its antimicrobial properties,
Hinokitiol has also been shown to: l Reduce matrix metalloproteinase expression by inhibiting Wnt/ß-Catenin signalling in vitro and in vivo7
l Be a promising and potent agent to inhibit UVB-induced MMP-1 and MMP-3 gene expression in skin fibroblasts8
l Inhibit UVB-induced apoptosis in keratinocytes9 In order to deliver optimised efficacy,
Hinokitiol has been combined with levulinic acid, a well-known and widely used antimicrobial substance which also possesses proven skin-penetration-enhancing properties.10
Levulinic acid is obtained from
biofermentation of sugar cane. Hinoline (now referred to as ‘the
upcycled antimicrobial’) has undergone various studies demonstrating its skin benefits, for example: l Increase of collagen III in both normal and UVB-irradiated skin (the upcycled antimicrobial used at 0.1% in a topical cream), Figure 1.
l Increase of hyaluronic acid levels in both normal and irradiated skin (the upcycled antimicrobial used at 0.1% in a topical cream), Figure 2.
l Anti-acne properties (questionnaire- based user trial, 22 volunteers, 18-40 y.o., 4 weeks; the upcycled antimicrobial used at 2% in a topical cream; results not shown in the present article).
Strain tested
E. Coli S. Aureus
P. Aeruginosa C. Albicans
A. Brasiliensis
MIC (%) of substances used individually
Hinokitiol 0.0050 0.0050 0.0500 0.0010 0.0030
PERSONAL CARE EUROPE
Levulinic Acid 0.31 0.63 0.50 1.25 1.25
Figure 2: Effect of Hinoline on hyaluronic acid (Hyaluronic Acid in blue, 40X, coloration, quantification by number of green pixels).
Broad-spectrum antimicrobial properties Both hinokitiol and levulinic acid show antimicrobial properties that are complementary: while the former displays good strength against fungi and yeasts, the latter is stronger against bacteria. Even though it is known that the so-
called MIC, i.e. the Minimum Inhibitory Concentration, of a substance does not necessarily reflect its performance in a more complex system, such as, for example a cosmetic product, Table 1 clearly shows that the MIC of the two substances combined in the upcycled antimicrobial is much lower than the MIC of the same substances taken individually. In other words, not only do hinokitiol
and levulinic acid complement each other to form a broad spectrum antimicrobial mixture, but they act synergistically lowering each other’s MIC. Ultimately, this enables formulators to use the upcycled antimicrobial on its own to efficaciously preserve a wide range of cosmetic and personal care products. The upcycled antimicrobial has been
widely tested in a variety of systems aimed at simulating real cosmetic products, e.g. emulsions, water-based gels, etc. Such
Table 1: MIC of Hinokitiol and Levulinic Acid used individually and combined in Hinoline.
MIC (%) of substances combined in individually
Hinokitiol 0.0038 0.0038 0.0150 0.0005 0.0019
Levulinic Acid 0.038 0.038 0.150 0.005 0.019
tests were designed to demonstrate its efficacy when both used alone and in combination with other substances, e.g. preservatives (as per Annex V of EC/1223/2009), multifunctionals, etc. AMITA UK (exclusive distributors of the
upcycled antimicrobial in the UK) are performing additional tests to help formulators optimise the use of this ingredient in a variety of cosmetic products. For example, when used at 2% as the sole anti-microbial in an O/W emulsion at pH around 5.5-6.0, a neat Category A pass was obtained when performing PET according to ISO11930. This is summarised by the plots shown in Figure 3.
Conclusions Hinoline is a patented multifunctional ingredient which shows properties of interest for a wide variety of cosmetic and personal-care products. Beside its proven broad-spectrum anti-
microbial and preservative-boosting properties, which make it an ideal ingredient to be used for all preservation needs, Hinoline has also been clinically proven to have anti-acne properties and a positive impact on collagen III and to increase skin levels of hyaluronic acid (ex vivo studies). Moreover, it is produced through green
chemistry processes including the use of waste materials, thus representing an ideal choice for those formulators who take particular care of the environment.
Notes Hinoline (invented by Philippe Bernard, GreenPharma) is exclusively distributed in the UK by AMITA UK.
PC September 2020
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