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CHITIN NANOFIBRILS A NATURAL COMPOUND TO BE USED AS DRUG

By Monica Bell,2014-05-15 16:55
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CHITIN NANOFIBRILS A NATURAL COMPOUND TO BE USED AS DRUG

    Chitin Nanofibrils :An Innovative Cosmetic Delivery

    System

    P. Morganti

    Professor of Applied Cosmetic Dermatology, II University of Naples

    Visiting Professor of China Medical University Shenyang

    Head of R&D, Mavi Sud s.r.l

    Mavi Sud s.r.l.

    Via dell’Industria 1,04011 Aprilia (LT)- Italy morganti@mavicosmetics.it

CHITIN NANOFIBRILS

    BIOLOGICAL SIGNIFICANCE

    In chemical terms chitin is a natural polysaccharide, present in scrub and shrimp shells

    formed by glucosamine and N-acetyl glucosamine, linked in a glycoside structure.

    (Muzzarelli RAA, et al., 1999; Muzzarelli R.A.A. and Muzzarelli C. 2005)

    Its alfa-nanocrystalline form separated by a patented process, is used as nanofibril of

    240x5x7 nm in dimension. These nanocrystals, exhibiting an exceptionally high surface

    (up to 400 m2/gr), have demonstrated a relevant biological significance. Thus they are able to activate fibroblast proliferation and cytokine production, favoring the giant cell

    migration, macrophage activation and neovascolarization. Due to its molecular

    conformation and its particular chemical-physical activity, the chitin nanofibril (CN) is

    capable not only to establish ionic bond with a great quantity of water, just as yaluronic

    acid (YA), but also to form complexes with different active ingredients delivering them

    to different site of the skin for different periods of time, in depending of the selected

    vehicle used. (Morganti P. et al., 2007).

CHEMICAL ACTIVITY

    Having CN the same backbone of YA, it is strongly hydrophobic and capable to attract

    and bind many molecules of water, establishing also stable ionic bonds with the

    negative sulfate location of the

    glycosaminoglycans (GAG). CN, in fact, is a

    polysaccharide strongly positively charged.

    can be selected to obtain a local or global

    activity at level of lipid bilayer membranes, or

    the extracellular matrix rich in GAGs.

    Therefore, the outmost layer of the stratum

    corneum (SC) (sunscreens), the whole SC or

    the intercorneocitary lipids (lipid lamellae) or

    the corneocytes themselves within the SC

    (moisturizing ingredients),the viable epidermis

    and the dermis (anti-aging and antioxidant Fig.1 - Different skin penetrability compounds), but also structural entities such as hair follicle (hair grow promoting

    agents), sebaceous or eccrine glands (anti-perspirant agents) or specific cell types such

    as melanocytes (depigmenting agents), Langerhans or Mast cells (immunostimulant and

    antiinflammatory compounds), can be targeted (Fig.1).

    So far, differently from drugs, it can be safely stated that the majority of current functional skin ingredients, and, first of all CN, are delivered to either the outer layer of the skin, viable the epidermis or dermis (i.e cosmetic dermal delivery) and not to the systemic circulation (i.e transdermal cosmetic delivery), being particularly safe for its cosmetic use. (Morganti P et al., 2007; Wiechers J.W, 2008; Biagini et al., 2008). At this purpose the natural chitin nanofibril (CN), processed and patented worldwide from MAVI Sud (MAVI SUD Int. Pat, 2005), seems to play many supporting roles in the cosmetic/personal care/pharmaceutical markets both as delivery system and active compound (Morganti P, 2007; Morganti et al., 2008; Mezzana P., 2008).

CLINICAL EFFICACY

    What is interesting to underline is the capacity the nanofibril has to increase the clinical efficacy of the active ingredients (Muzzarelli RAA, et al. 1999; ), positively affecting their partition coefficient between formulation and skin, when used in the right way and in the right emulsion (Morganti P, 2008).

    The prevalent amino groups of these rod-like and positively charged chitin crystallites, embedded in water form hydrogen and ionic

    bonds with different kind of molecules,

    originating innovative skin-friendly

    complexes contributing to the stability of

    the final suspension also (Fig. 2). These new

    obtained chitin-complexes reorganize

    theirselves spontaneously into large

    domains, easily emulsifying different class

    of lipids. In depending of the different

    quantity and quality of CN, CN-complexes

    and of other active compounds (natural and

    synthetic lipids, polymers and amphiphilic Fig.2 Chitin Nanofibrils at SEM molecules), the emulsifiers selected and all

    the manufacturing process used, it is

    possible to obtain different tipology of

    emulsions (vesicular or lamellar, micro or

    nano) solubilization systems and gel

    systems (Fig.3).

    Moreover, the CN-complexes can be chosen

    from a wide variety of active compounds

    both idro and lipo-soluble to meet the needs

    of the application as well as the clinically

    efficacy of the final cosmetic formulation

    (Morganti et al., 2008; Mezzana P., 2008).

     Fig.3 - different tipology of emulsions BIO-AVAILABILITY

    However, to increase the efficacy, safety and bio-availability of all the active ingredients applied to the skin, the interaction between vehicle/active ingredient, the capacity the vehicle has to produce changes in skin structure, and the doplet size of the vehicle, should be critically controlled. The small size ensures a closer contact with the SC and thus, the amount of incorporated active ingredients within the carrier reaching the programmed site of action will be notably increased. CN seems, in fact, to have the ability to induce the creation of a monolayer lipidic film on the SC, thereby

    increasing the skin penetration of all the active compounds, avoiding the excessive water evaporation and thus increasing skin hydration also.

    Moreover, when directly in contact with the stratum corneum, the emulsified CN may be hydrolized by the skin’ enzymes and transformed in dimeric and/or tretrameric units.

    Thus, oligomers may penetrate throughout the skin layers together with the eventually bonded active compounds.

    However, the influence of formulation design, the selected ingredients used together with CN, and the manufacturing process are other important factor to obtain a correct skin penetration.

    Therefore the CN, used alone or in combination with natural antioxidant and immunomodulant compounds may found interesting application, leading to a new generation of skin anti-aging and wound

    healing products.

OBTAINED RESULTS

    Thus, our R&D group verified the cosmetic

    activity of CN by different studies both in

    vitro and in vivo ((Morganti et al. a, 2008;

    Morganti et al. b, 2008).

    These studies have stressed the influence

    CN has to increase the active compounds’

    penetration through the stratum corneum

    and, thereby the viable skin (Fig. 4).

    As matter of fact, in vivo skin hydration Fig.4 Chitin Nanofibril into the skin increase from 40 (only CN vehicle) to 80% (CN + active compounds) (Tab.1), and surface skin-lipids increase also from 35 to 68%(Tab.2).

    On the other side TEWL decrease from about 50 to 72% and lipid peroxides from 35% to66% (Tab.3). It is interesting to underline the whitening activity CN seems to have also strongly decreasing the age spots appearance (Tab. 4). On the other hand the in vitro studies demonstrates as CN is capable to increase both fibroblast proliferation and the relative collagen production. Naturally the ATP production is also seems to increase by the activity of CN (Tab.5).

    Tab. 2 Tab. 1

     Tab. 4 Tab.3

    CONCLUSION

    These examples underline the activity CN

    seems to have as innovative cosmetic

    delivery , allowing particular bonds and

    connections between water, active molecules

    and the cells of both stratum corneum and

    viable skin. These CN bindings, seem to be

    mediated by a group of non covalent

    attractions (ionic and hydrogen bonds) that

    are individually quite weak, but whose

    energies can sum to create an effective force Tab. 5 between two or more separate molecules. CN, as a natural polysaccharide recognized from the cell components, may have

    different fates. Part, totally hydrolized may be used as monomer subunits to construct

    the giant polymeric macromolecules of the cell, such as large polysaccharides. Others,

    may act as energy sources and therefore, broken down and transformed into small

    molecules, in a maze of intracellular metabolic pathways. It is to remember that both

    glucosamine and acetyl-glucosamine are fundamental molecules of our body. In

    conclusion CN, as sugar- like compound , may be considered a safe molecule that, for

    its particular characteristics to easily bond water and other molecules, and to penetrate

    the different skin layers, may be useful not only as skin carrier, but also as an active

    component to formulate innovative cosmetic and pharmaceutical products. Many other

    seem also the possibilities of its use as, for example, to make innovative fibers for

    biofunctional textiles (Morganti P, 2008). For better understanding this fascinating

    rediscovered molecule it will be necessary to make further multidisciplinary studies,

    introducing new technology useful for ameliorate the general wellbeing. This is our

    challenge for the future.

References

    Biagini G., Zizzi A., Giantomassi F., Orlando F., Lucarini G., Mattioli Belmonte M., TucciM.G. and Morganti P., 2008, Cutaneous Absorption of Nanostructured Chitin

    Associated with Natural Synergistic Molecules (Lutein) Journal of Applied Cosmetology 26:69-80

MAVI SUD International Patent, 2005, PCT/IB2005/053576

    Mezzana P., 2008, Clinical efficacy of a new chitin-nanofibrils based gel in wound healing . In print on: Acta Chirurgiae Plasticae

    Morganti P, Lee Yuanhong, Morganti G., 2007, Nano-structured products: technology and future, J. Appl. Cosmetol., 25:161-178

    .

    Morganti P., 2007, Where nutriceuticals meet cosmecuticals, J. Appl. Cosmetol., 25:111-120

    Morganti P., Fabrizi G., Palombo P., Palombo M., Ruocco E. Cardillo A and Morganti G., 2008, a. Chitin-nanofibrils: a new active cosmetic carrier. Journal of Applied Cosmetology 26: 105-120

Morganti P, 2008, Unpublished data

    Morganti P., Morganti G., Fabrizi G. and Cardillo A, 2008, b. A new sun to rejuvenate the skin. In print on: Journal of Applied Cosmetology

    Morganti P., 2008, Leather & Textile Chemicals Chitin nanofibrils in textiles. Speciality Chemicals Magazine 28 (n.9) :26

    Muzzarelli RAA, Mattioli-Belmonte M, Pugnaloni A and Biagini G., 1999, Biochemistry, histology and clinical uses of chitins and chitosans in wound healing. In: Chitin and and Chitinases P.Jollés and RAA Muzzarelli, eds. Birkhaüser Verlag Basel/Swizterland, p. 251-264

    Muzzarelli R.A.A. and Muzzarelli C., 2005, Chitin nanofibrils. In: Chitin and Chitosan: Research Opportunities and Challenges P.K. Dutta and RAA Muzzarelli, eds. New Age International, New Dehli, India

    Wiechers J.W 2008 Science and application of skin delivery systems. Allured Ed, Carol Stream, IL,USA

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