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NANOTECHNOLOGY: LIPOSOMES

Juan Manuel Serrano Núñez

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•NANOTECHNOLOGY: Definition and Scale

•History

•Fields of Application

•Phospholipids

•LIPOSOMES: Definition, Classification, Benefits, Composition

•LECITHIN: Composition, Properties

•MANUFACTURING PROCESS

•CHARACTERIZATION

•NANOTECH VIDEO

•LIPOSOME PERMEATION: SKIN, HAIR AND NAILS

•ORAL BIOAVAILABILITY: LIPOSOMAL VITAMIN C

•ANTIOXIDATIVE TEST

•EFFICACY OF FREE RETINOL VS LIPOSOMAL RETINOL

•DEGRADATION OF FREE RETINOL VS LIPOSOMAL RETINOL

INDEX

Definition and Scale

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The science and technology which manipulates and controls matter within the nanoscale

The science and technology which manipulates and controls matter within the nanoscale

1nm=1x10-9m (one billionth of a meter) 1.000.000.000nm=1m

Nanotechnology: Liposomes

History

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We have always been surrounded by nanoparticles…

- Carbon nanoparticles from combustion (cars, fires)

- Carbon nanoparticles from car tyres.

- Gold nanoparticles as pigments in windows of churches.

- Virus.

-Molecules,…

We are now surrounded by more nanoparticles ...

Due to the discovery of new tools that allow us to observe, manipulate and producenanoscale structures.


Fields of application

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Phospholipids

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Small spherical vesicles comprised of one or more lipid bilayers.


Definition

Classification

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BenefitsNanotechnology: Liposomes

Their structure is very similar to biological membranes

Biodegradable and non toxic

Prevent oxidation and degradation of the ingredients

Show higher efficiencies at lower concentrations

Can encapsulate hydrophilic and lipophilic substances

Can reach the deepest layers of the skin

Provide a sustained release of the active ingredients

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Liposomes composition


Soy lecithin, organic solvent, surfactant, active ingredient and water

Chemical Composition QUANTITY (%)

Phosphatydilcholine 94

Lysophosphatydilcholine 3

Triglycerides 2

N-Acyl-Phosphatydil Ethanolamine 0,5

Free Fatty Acids 0,5

DL-Alpha-Tocopherol 0,3

Phosphatydil Ethanolamine 0,1

Phosphatydil Inositol 0,1

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Properties of LecithinNanotecnología: valor diferencial en dermocosmética

EPITHELIALIZING: repairs the damaged stratum corneum, enhancing skin barrier function.

ANTI-INFLAMMATORY: reduces swelling in the area.

BACTERICIDE: prevents the proliferation of infections.

SEBUM REGULATING: normalizes skin surface lipids.

WHITENING: linoleic acid has helps to even the skin tone.

Skin diseases such as eczema, psoriasis and acne improve with the use of lecithin.

Slows the aging of the skin when dryness and thinning of the skin occurs.

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Manufacturing ProcessNanotechnology: Liposomes

On one side, soy lecithin is dissolved in an organic solvent and a detergentis added too. Separately, the molecule of interest is dissolved in purifiedwater or saline. Both phases are mixed at constant frequency undervacuum conditions and at a certain temperature (above the phasetransition temperature). Finally, the liposomal suspension is passedthrough a 200nm pore size filter.

The liposomes obtained are unilamellar, stable and homogeneous. Thediameter of the vesicles oscillate between 50 and 200nm.

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Characterization


NANOSIZER (Delsa nano C): Particle Analyzer

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CharacterizationNanotechnology: Liposomes

NANOSIZER (Delsa nano C): Particle Analyzer

The DelsaNano utilizes Photon Correlation

Spectroscopy and Electrophoretic Light Scattering

techniques to determine particle size and zeta

potential of materials

- Size: diameter of liposomes

- Homogeneity: polidispersity index

- Stability: Z potential

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TRANSMISSION ELECTRON MICROSCOPY

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TRANSMISSION ELECTRON MICROSCOPY

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Nanotech videoNanotechnology: Liposomes

NANOTECH English.mp4

NANOTECH English.mp4

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Transdermal PathwaysNanotechnology: Liposomes

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Percutaneous AbsorptionNanotechnology: Liposomes

AIM

Compare the penetration capacity of a liposomal formulation with a conventional one, through humanskin.

Experiment was conducted with the collaboration of the General Hospital of Valencia.

Fluorescein and sodium ascorbate were the molecules chosen.

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METHOD

FRANZ DIFFUSION CELL SYSTEM

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RESULTS

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CONFOCAL MICROSCOPY

Source: General Hospital of Valencia

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CONCLUSIONS

Sesderma® liposomes enhance epidermal penetration and facilitate permeationto the deepest layers of the skin.

Skin penetration depends on the carrier used and the nature of the molecule.

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Transfollicular AbsorptionNanotechnology: Liposomes

Assess the permeation capacity of fluorescein labeled liposomes through hair follicles of human scalp.

AIM

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Fluorescence Microscopy Optical microscopy

Liposomes reached superficial hairs

RESULTS

Source:GeneralHospital ofValencia

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Fluorescence

Microscopy

Optical

microscopy

Liposomes conquered the base of the hair follicle

RESULTS


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Fluorescence Microscopy Optical microscopy

Liposomes are still present in the deepest hairs

RESULTS


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CONCLUSIONS

Sesderma® liposomes penetrate through the follicular canal forming a reservoir and facilitating their way into the dermis

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Transungual AbsorptionNanotechnology: Liposomes

AIM

Assay the penetration capacity of fluorescein loaded liposomes and a solution of free fluoresceinthrough a nail plate.

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The equipment used was a Franz diffusion cell with a coupling device fornails. Fluoresce in liposomes were added to the donor chamber and it wascovered with a film to prevent evaporation. The receptor compartment wasbathed with a pH 7.4 buffered solution (PBS) previously degassed withultrasound. Samples were taken from the receptor chamber at pre-settimes.

The amounts of fluorescein were determined by spectrofluorimetry.

METHOD

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RESULTS

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Fluorescence Microscopy

RESULTS

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The results showed that after two days in contact with the product, the nail reached itsmaximum of absorption for the two fluorescein formulations. We obtained an amount ofaccumulated fluorescein 2.5 times higher for the liposomal preparation (2.96 ± 0.2 mg /cm2) than for the preparation with the free form(1.22± 0.2 mg / cm2).

RESULTS

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CONCLUSIONS

Sesderma® liposomes play an important role in carrying active ingredients inside the nails

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In vivo pharmacokinetics of oral administration of sodium ascorbate liposomes


Compare the pharmacokinetics of two sodium ascorbate formulations:

- Sodium ascorbate solution (extemporaneously prepared).- Sodium ascorbate encapsulated in liposomes.

Experiment was conducted with the collaboration of the General Hospital of Valencia.

AIM

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RESULTS

Plasma concentration versus time after oral administration of 250 mg of sodium ascorbate formulated in an extemporaneous solution (black line) or in liposomes (green line). Mean

± SEM, n = 6.

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CONCLUSIONS

Sesderma® liposomes enable a sustained release of sodium ascorbate, allowing longerblood circulating times. Thus, the intervals for dosing can be increased.

Sodium ascorbate loaded liposomes require a smaller dose to reach the desiredplasma concentration and, therefore, the desired therapeutic effect.

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Antioxidative effectNanotechnology: Liposomes

Source: Bionos

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Retinol


COMPARATIVE STUDY OF RETINOL LIPOSOMES VS FREE RETINOL

Fuente: Bionos

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RetinolNanotechnology: Liposomes

COMPARATIVE STUDY OF RETINOL LIPOSOMES VS FREE RETINOL

Source: Bionos

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RetinolNanotechnology: Liposomes

COMPARATIVE STUDY OF THE DEGRADATION OF RETINOL IN FREE FORM VS RETINOL LOADED LIPOSOMES

PRODUCTO FECHA FABRICACION FECHA ANALISIS % RETINOL PRESENTE % DEGRADACION RETINOL

RETINOL LIBRE 26.06.12

Tiempo 0 84%

30% en 6 meses

54% en 18 meses

6 meses 58%

12 meses

18 meses

36%

30%

RETINOL LIPOSOMADO 9.01.12

Tiempo 0 88%

28% en 1 AÑO

34% en 18 meses

6 meses 79%

12 meses

18 meses

63%

54%

Source: Faculty of Chemistry. University of Valencia

Thanks for your [email protected]

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