Overcoming Aesthetic Limitations in Formulating Natural
Ingredients and Enhancing Their Performance with Encapsulation Technology
Aesthetic
considerations may be a limiting factor in incorporating vitamins and other
natural ingredients into natural topical formulations. Implementing
encapsulation technology can modulate undesirable effects such as color and
odor common to vitamins and other natural ingredients. Diminishing such
undesired side effects makes it highly desirable to increase concentration of
such ingredients in natural topical formulations while enhancing their
performance.
Undesirable
side effects of vitamins and natural ingredients such as odor and color can be
modulated by encapsulation technology such as
q micro-encapsulation,
q nano-encapsulation,
q complexing.
Encapsulation
of vitamins and natural ingredients can enhance their performance.
Disclaimer
The
following text and statements are not legal or medical advice nor are they
intended to reflect the ideas of or represent the Food and Drug Administration.
The sole purpose is to stimulate a discussion and point out issues of concern
in this field.
The Following Pages are Provided to Clarify Terminology
1.
What are “topical formulations”?
2.
What are “natural ingredients”?
3.
What is “encapsulation technology”?
4.
What is “micro-encapsulation”?
5.
What is “nano-encapsulation”?
6.
What are “aesthetic considerations”?
a.
What is “odor modulation”?
b.
What is “color modulation”?
7. What is “enhanced performance”?
1. What are “topical formulations”?
Topical
formulations (TF) include liquids, creams, lotions, pastes, that are formulated
to be applied onto the skin.
Legal definitions
of drugs and cosmetics.
TF
can be divided into two legal categories: pharmaceutical preparations and
cosmetic preparations. The legal categories are defined by the Food and Drug
Administration (FDA). Cosmetic preparations are sub-categorized as preparations
that have brief contact with the skin, such as soaps and detergents, and
preparations that are made for a prolonged stay on skin, such as skin care
products.
After
TF are applied onto skin they can penetrate into the skin or remain on top of
the skin. TF claiming to be trans-dermal will most likely be treated as a drug.
TF claiming to remain on top of the skin or penetrate into dead skin layers can
be treated as cosmetics.
TF that remain on top of the skin after application may not be different than protective clothes or sun glasses and won a court case against the FDA which was then overturned on appeal.
Actual performance
of preparations categorized as
“cosmetics”
Legal
definitions of pharmaceutical and cosmetic preparations relate to claims and
label regulations and not to actual performance of TF as long as the TF does
not include any ingredient that is specifically categorized as a drug.
Statistically significant, well-designed studies on TF therapeutic performance
can be regarded as scientifically valid. However, scientific validation is not
sufficient ground for legal acceptance of a TF as a drug unless FDA protocol
was applied.
The discrepancy between “actual performance” and “legal performance” of TF is the creative space in which “cosmeceuticals” flourish.
2. What are “natural ingredients”?
The
term “natural ingredients” is not well defined and there are many guidelines
and many levels of adherance to the different guidelines. Example: some believe
that cold-pressed oil from a grain is not natural and only the whole grain
qualifies for the term “natural”. Others believe that any ingredient that
exists in nature is natural even if it was not extracted from a natural source
but was rather synthetized, as long as it is identical to that natural
ingredient.
In
reality, manufacturers and consumers of natural ingredients alike experience
similar constraints of cost and availability which may affect their definition
range of “natural ingredients”
Natural
ingredients often
q
are immiscible in the media in which they are
intendent to be formulated;
q
are too poisonous if they are distributed throughout
the body;
q
have unpleasent distinctive and vivid odors
q
have distinct colors that may affect the overall
formula color.
In
natural skin care the final formula is many times as important as individual
beneficial natural ingredients within that formula delivering their benefits.
There is growing literature and experience indicating that ingredients do not
perform the same when formulated in different preparations. Many natural skin
care products specify benefits that can be derived from certain “natural
ingredients”. However, by legal definition cosmetic preparations claims can
only relate to their moisturizing effects. Thus, ingredients can legally have
only moisturizing activity. Any other claim will categorize the preparation as
a drug.
In reality, cosmetic preperations can have beneficial properties for skin other than mosturizing but these cannot be claimed. Such benefits are not the least due to some of their natural ingredients. Though such claims cannot be made, innovative formulation of natural ingredients into skin care formulations can be very potent. Many natural skin care products are formulated that perform similarly or better than a medicinal preparation.
3. What is “encapsulation
technology”?
Encapsulation
technology is insertion of active ingredients into protective boundaries that
can insolate, disperse, mobilize, enhance activity, and transport these
ingredients via immiscible media and barriers. Inserting active ingredients
into capsules is the art of encapsulation.
Encapsulation’s
effect on ingredients’ performance can be rated by the following criteria:
q
transport them across biological obsticals,
q
increase their active life time,
q
improve ingredients’ solubility in desired media,
q
protect the body from possible poisonous side
effects of ingredients, and
q
concentrate active ingredients in the desired
biological target area.
4. What is
“micro-encapsulation”?
Micro-encapsulation
is encapsulation of ingredients in micrometer size range capsules. Normally,
this would apply to encapsulation of a multitude of ingredients per individual
capsule. An example of micro-capsules is liposomes.
5. What is
“nano-encapsulation”?
Nano-encapsulation
is encapsulation of ingredients in nanometer size range capsules. Normally,
this would apply to encapsulation of a single or several ingredient molecules
per individual capsule. An example of nano-capsules is cyclodextrin.
6. What are “aesthetic
considerations”?
Aesthetic
considerations relate to side effects which are in the eyes of the beholder.
What may be a desirable effect to one may be an undesirable effect to the
other.
Example:
Nano-encapsulation of Vitamin A with a vehicle of the cyclodextrin family may
increase Vitamin A activity against wrinkles. At the same time the dark brown
color and the vivid medicinal odor of Vitamin A are great deterrents. Color and
odor are important manufacturing concerns. Less than effective concentrations
of Vitamin A in anti-wrinkle or anti-aging skin care are therefore used in many
preparations. Encapsulation of Vitamin A in that vehicle drastically reduces
color and odor of a formula enriched with Vitamin A. The benefits may be
triple:
q
increased activity of vitamin A,
q
increased concentration of vitamin A, and
q increased asthetic performance.
How
does encapsulation modulate odor, color, and performance?
c. How is “odor modulation”
achieved?
Odor
is an inherited characteristic of ingredients. A small amount of molecules
which vaporize from a jar can sometimes deliver very perceptible odor.
Encapsulation of such ingredients reduces their evaporation which translates to
odor reduction.
d. How is “color modulation”
achieved?
Color
too, is an inherited characteristic of ingredients. Encapsulation of colored
ingredients can affect their physical characteristics. Color can be quenched by
high concentration of ingredient molecules in the capsule. Hydrogen bonds and
hydrophobic interactions may stabilize the molecules in a certain physical
state reducing color effects. Capsules can mask the color of encapsulated
molecules.
7. What is “enhanced performance”?
Encapsulated
ingredients may undergo a sterochemical change of an active ingredient site of
action. In some cases this will result in increased reactivity of the active
ingredients’ site of action and enhanced activity. Steric hindrance may be
removed at the proximity of the active site of an encapsulated ingredient. This
can enable its activity on molecular targets that are normaly resistant to that
same ingredient in a non-encapsulated state.
Encapsulation may affect active ingredients’ shape and reactivity so that they gain accesability to molecular sites of action and synergistic activity with other active ingredients.
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