(Transcript of presentation)

Outline of Lecture

• What is a Delivery System
• Skin Fundamentals
• Physiology and Penetration Pathways
• Why Encapsulate
• Types of Delivery Systems
• Overview
• Next Generation

Definition of a Delivery System

• It’s a way of holding, carrying, and transporting an active to a substrate
• It can control the rate of release from a formulation as well as absorption
• May provide sustained release, controlled release, or release on demand into the substrate
• Any type of vehicle that make an “active” available to a target site

Delivery System

• Ingredients today
• More advanced
• Much more effective
• How do we take advantage of the technology?
• Formulators challenge
• Ability to include more ingredients into one formula
• Ingredients work smarter

Human Skin

• Stratum Corneum

(10-15 µm)

• Living Epidermis

(~ 100 µm)

• Dermis

(2,000-3,000 µm)

Brick and Mortar
Bricks = Corneocytes
Mortar = Lipids

4 Layers of the Epidermis

Stratum Spinosum

Stratum Granulosum

Stratum Corneum

Structure of the SC

Stratum Corneum Anatomy

• Lamellar Bodies – Releases free fatty acids and ceramides
• Corneocyte Shell
• Ceramide Lipids
• Corneodesmosomes
• NMF
• Desquamation

Skin Penetration Pathways

• Intercellular pathway
• The volume of the area is about 5%-30% of the stratum corneum
• Water has been found to penetrate the skin via the intercellular pathway
• Transcellular pathway
• Occurs through the keratinized corneocytes
• Also known as the polar pathway

Skin Penetration Pathways

• The Pilosebaceic pathway
• Occurs via penetration through the hair follicles
• Mainly a route for very lipophilic molecules
• A major route for both charged and large polar molecules
• Available area for diffusion is approx. 0.1% of the total skin area

Skin Penetration Enhancers

• Physical
• Iontophoresis; electric current 15 mA
• Sonophoresis; low-frequency ultrasound, 20 kHz
• Dermal patches
• Micro needles
• Enzymatic
• These inhibit key enzymes of the lipid synthesis
• Alters the critical moral ratio of the stratum corneum lipids
• Vesicular carriers
• Microscopic vesicle spheres or Nanospheres
• Hydrophilic and Lipophilic actives can be incorporated within the carrier

Why Encapsulate

• Improve stability
• Protection from light/air, prolongation of shelf life
• Fluctuating temperature sensitivities
• Modulating skin penetration properties
• Controlled release
• The rate of release
• Sustained release
• The time of release

Why Encapsulate

• Protection from component interactions
• Prevent contact of incompatible ingredients in the formulation
• Change of form (i.e. incorporation of oil into a powder to allow the creation of powdered formulation)
• Multi-benefit products
• Product releases a peptide followed by a skin brightener

Why Encapsulate

• Improve skin tolerance
• Eliminate skin irritation
• Improve efficacy
• Improve safety
• Improved aesthetics
• Consumer appeal
• Color changes
• Eliminate undesired odor

Types of Delivery Systems

• Micro capsules
• Liposomes
• Particles
• Emulsions
• Lyphazomes
• Physical enhancements
• Future models

Micro Capsules

• Proprietary type of polymer
• Delivers a specific ingredient
• Releases when applying
• Not a controlled release
• Releases one ingredient onto the target area
• Carrier oils
• Retinol palmitate
• Vitamin E
• Linoleic acid/Linolenic acid

Liposomes

• Lamellar vesicles
• Size-In the low micro-meter range
• Made up of aqueous compartments and a lipid bilayer

Liposomes

• May be either phospholipids or sterols
• Natural or artificial
• Not all are biodegradable
• Sizes can vary from 25-5000 nm
• Many are loaded by manufacturer
• Fragile structure
• Prone to oxidation

Size Matters

• What is Nano?
• One nanometer is billionth of a meter …Huh?
• A sheet of paper is 100,000 nanometers thick
• If you’re a blond, your hair is approx. 15,000 to 50,000 nanometers in diameter
• If you have black hair, its diameter is likely to be 50,000 to 180,000 nanometers
• There are 25,400,000 nanometers per inch

Nano

• The Roman makers of the Lycurgus Cup knew that if they added tiny particles of gold and silver when making glass it would turn a different color when light shone through it.

Particles

• Micronized titanium dioxide
• Inorganic UVA UVB blocker
• Mineral makeup and some sunscreens
• Micronized zinc oxide
• Inorganic UVA UVB blocker < 200 nm
• Mostly used in physical sunscreens
• Polytrap® Technology
• Porous networks – ideal for lipophilic actives
• Will promptly release the entrapped ingredient

Most common form of delivery – EMULSION

• Emulsion
• Monomer droplet
• Addition of ingredients
• Emulsion before polymerization
• Polymerization to form latex particles

Emulsions

• Can encapsulate many ingredients
• Emulsion often releases when rubbed onto the skin
• Encapsulation breaks down with pH change, temperature change, salts and surfactants
• Emulsion does not always mean a controlled release

Lyphazomes

• Natural and 100% biodegradable
• Made up of phospholipids used by the body
• Stable in regards to pH, temperature, salts and surfactants
• Exhibits a controlled release while in the skin
• Same sized nanospheres 300 nm
• Slight anionic charge to permeate the skin
• Can also carry a cationic charge
• Penetrates to the ceramides with the stratum corneum and localize

Lyphazomes

• Lyphazomes are formed in situ
• Within itself
• Sized to “stick” within the granulosum
• Lyphazomes enhance the stability of the ingredient until released
• Releases all loaded ingredients over time
• >8 hours
• Irritation is minimal

Lipophilic Ingredients

• Vitamin E
• Vitamin A
• Retinol
• Alpha Bisabolol

Hydrophilic Ingredients

• Vitamin C
• Green Tea
• Peptides
• Glycolic Acid
• Hydroquinone

Lyphazome Natural Nanotechnology (Illustration of how nanospheres work with the skin)

• CELAZOME PRODUCT APPLIED TO SKIN
• NANOSPHERE PENETRATION:
• 80% nanosphere CONCENTRATION penetrating within the stratum corneum
• MIGRATION of NANOSPHERES through the stratum corneum
• RESERVOIR of NANOSPHERES between the stratum corneum and stratum granulosum
• TIME-RELEASE OF INGREDIENTS:
• Bioactive/Active ingredients releasing over time within the stratum corneum and deeper epidermal layer
• RELEASED ingredients slowly penetrating into the epidermal layers

Physical Enhancements

• Micro needles
• 192 needles which delicately puncture the epidermis of the skin. This damage begins the release of growth factors which stimulate collagen and elastin production
• Sonophoresis
• Use of ultrasound to enhance topical delivery
• Very low frequency increases the permeability of the stratum corneum
• Iontophoresis
• Device consisting of an anode and a cathode
• Enhancing the penetration rate

Physical Enhancements

• Trans dermal patches
• It requires the user to wear them for 6 to 8 hours at a time…. and sometimes even overnight for the ingredients to travel back to the selected target…..like under the eyes
• Intra dermal patches
• Delivers the ingredients immediately and directly into the deep layers of the skin so you only have to wear them for 45 minutes to get better and more effective results

Brief Overview

• The absorption of actives into the stratum corneum is a complex process
• Today’s market is more demanding for quality, immediate performance
• Delivery systems today means to be much more precise in terms of targeted effects

Overview

• Provides cost-enhanced, cost-effectiveness potential
• A good delivery system is a valuable tool when it comes to maintaining quality
• Using a similar concentration of ingredients will give you an added benefit vs. conventional products
• Added benefits = faster results to the client

Future Methods

• NLP
• Nano Lipidic Particles
• Dial-a-size technology
• Fast release; sustained release all in one formula
• In nutraceutical applications – vitamins & minerals
• Drug applications
• Nano medicine
• Targeting cancer cells