NEW TECHNOLOGY IN TRANSDERMAL DELIVERY

THE CHALLENGE

The continual market increase in the transdermal and topical delivery of drugs makes cutaneous drug delivery exploration all the more attractive for scientists.

The key in the delivery of drugs to the skin is bypassing its natural barrier, i.e. the stratum corneum, comprised of corneocytes surrounded by lipid regions, which functions as a protective skin layer against exogenous substances and poses as the fundamental obstacle for product formulators.

As most solutions applied onto the skin permeate along the lipid domains, the organisation and composition of the lipid component is considered to be very important for the skin barrier function. To overcome the challenge of skin permeation faced, Liposomes have emerged as a advantageous technique.

Pro-Liposomes have a bilayer of phospholipids with the ability to fuse/absorb into the cellular membranes when applied topically, followed by the transfer of active ingredients into cells.

LIPOSOMES

Liposomes are microscopic vesicles composed of a bilayer of phospholipids that encapsulate medicines. They are a novel drug delivery system that release the medication at a predetermined rate, according to need, pharmacological aspects, drug profile, physiological conditions of the body area, etc. But liposomes exhibit poor stability and this problem leads to issues relating to their storage.

To circumvent this problem, Pro-liposomes (PLs) were originated.

DERMCLAR PRO-LIPOSOMES

Pro-liposomes, as utilised in Dermclar Liposome Solutions, are free flowing granular products composed of active ingredients and phospholipid precursors.

Dermclar Pro-liposomes have a natural affinity for skin lipids, avoiding stratum corneum hindrance and thus enhancing the ingredient permeation and diffusion within the tissue, and leads to a more sustained action of the entrapped nutrients.

CLINICAL REFERENCES

The four mechanisms proposed by which vesicular systems deliver drugs into skin have previously been reviewed (Elsayed et al., 2007; Dubey et al., 2007; Nounou et al., 2008; El Maghraby et al., 2008; El Maghraby and Williams, 2009) and include (i) intact drug-laden vesicle penetration into the different layers of the skin; (ii) lipid vesicles acting as penetration enhancers via their skin lipid fluidising property; (iii) direct carrier-skin drug exchange by “collision complex transfer” between the drug intercalated in the lipid bilayer and the surface phase of the stratum corneum; and (iv) lipid vesicle-mediated enhanced transdermal drug delivery via appendageal pathways (e.g., hair follicles and sweat ducts).

DERMCLAR CELLULITE LIPOSOME CLINICAL EFFICACY TEST

PERCUTANEOUS ABSORPTION

Dermclar Liposomes Cellulite formulation favours epidermal penetration as was demonstrated by the fact that caffeine penetration is increased almost 5 fold and escin penetration is increased almost 8 fold. The encapsulation of the actives also enables a more efficient release, as proven by determinations at 16 hours, where caffeine showed to have absorbed 3 times more than standard caffeine.

Absorption

INHIBITION OF ADIPOCYTE MATURATION

An in-vitro cell culture model of human preadipocytes were stimulated to differentiate to adipocytes. Lipid droplets were visualised by phase contrast microscopy and quantified image analysis.

Results indicate that Liposomes Cellulite is a strong inhibitor of adipocyte maturation with microscopy photographs showing a dramatic decrease in adipocyte formation.

Microscopy

ACTIVATION OF MICRO-CIRCULATION

An in-vivo test involving 20 adult female patients proved the properties of Liposomes Cellulite as
an activator of microcirculation.

Video capillaroscopy images show an improvement in the structure of microcapillaries and a decrease in microhemorrhages. This appears as a rosier complexion, less evident presence of nodules and an improvement in skin colour.

Skin

TREATABLE INDICATIONS

The current, treatable indications include:

Additional Pro-Liposome solutions coming soon.

TREATMENT COMPATIBILITY

Dermclar Pro-Liposome Solutions are compatible with a broad range of treatment modalities where active ingredient penetration is advantageous, including:

  • Microneedling
  • Ultrasound
  • Electroporation, Iontophoresis, virtual meso, etc.
  • Radio frequency
  • Simple topical application