Post on 03-Jun-2020
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.
Nanotechnology: Liposomes
Fields of application
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Nanotechnology: Liposomes
Phospholipids
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Nanotechnology: Liposomes
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Small spherical vesicles comprised of one or more lipid bilayers.
Nanotechnology: Liposomes
Definition
Classification
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Nanotechnology: Liposomes
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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
Nanotechnology: Liposomes
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
Nanotechnology: Liposomes
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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CharacterizationNanotechnology: Liposomes
TRANSMISSION ELECTRON MICROSCOPY
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CharacterizationNanotechnology: Liposomes
TRANSMISSION ELECTRON MICROSCOPY
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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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Percutaneous AbsorptionNanotechnology: Liposomes
METHOD
FRANZ DIFFUSION CELL SYSTEM
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Percutaneous AbsorptionNanotechnology: Liposomes
RESULTS
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Percutaneous AbsorptionNanotechnology: Liposomes
CONFOCAL MICROSCOPY
Source: General Hospital of Valencia
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Percutaneous AbsorptionNanotechnology: Liposomes
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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Transfollicular AbsorptionNanotechnology: Liposomes
Fluorescence Microscopy Optical microscopy
Liposomes reached superficial hairs
RESULTS
Source:GeneralHospital ofValencia
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Transfollicular AbsorptionNanotechnology: Liposomes
Fluorescence
Microscopy
Optical
microscopy
Liposomes conquered the base of the hair follicle
RESULTS
Source:GeneralHospital ofValencia
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Transfollicular AbsorptionNanotechnology: Liposomes
Fluorescence Microscopy Optical microscopy
Liposomes are still present in the deepest hairs
RESULTS
Source:GeneralHospital ofValencia
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Transfollicular AbsorptionNanotechnology: Liposomes
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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Transungual AbsorptionNanotechnology: Liposomes
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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Transungual AbsorptionNanotechnology: Liposomes
RESULTS
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Transungual AbsorptionNanotechnology: Liposomes
Fluorescence Microscopy
RESULTS
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Transungual AbsorptionNanotechnology: Liposomes
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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Percutaneous AbsorptionNanotechnology: Liposomes
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
Nanotechnology: 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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In vivo pharmacokinetics of oral administration of sodium ascorbate liposomes
Nanotechnology: Liposomes
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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In vivo pharmacokinetics of oral administration of sodium ascorbate liposomes
Nanotechnology: Liposomes
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
Nanotechnology: Liposomes
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 attentionj.serrano@sesderma.com