| How Rosacea Works...
Q: Who Does Rosacea Affect?
A: Rosacea is a chronic disease
which afflicts over 16 million North Americans. Rosacea is most
commonly found in adults between the ages of 30 and 65 but rosacea
has been known to afflict even children. The people who are
the most prone to acquiring Rosacea are fair skinned adults
and especially women.
Q: What is Rosacea?
A: Rosacea is a hereditary, chronic
(meaning long term) skin disorder that most often affects the
nose, forehead, cheekbones, and chin. In its beginning stages
this common skin disease, which causes subtle redness in the
center of the face, may come and go on its own. But, if left
untreated, Rosacea may develop into some inflammation, accompanied
by skin eruptions, and may gradually become chronic and even
permanent. Furthermore, the skin tissue can swell and thicken
and may be tender and sensitive to the touch. About half of
Rosacea sufferers also complain of symptoms with their eyes,
also known as Ocular Rosacea.
The Medical Breakdown of Rosacea
Rosacea is caused by the dilation of tiny blood vessels close
to the surface of the skin. This causes the skin to break out
with blotchy red areas called papules. A papule is a red solid
elevated inflammatory skin lesion without pus (unless the papule
is severe). These papules have three classifications; minor,
moderate and severe. A minor Rosacea papule is the size of a
small measles lesion. A moderate Rosacea papule is the size
of a pencil eraser. A severe papule is the size of a coin and
also contains pustules (pus-filled inflammatory bumps).
How Our Acne Rosacea Treatment System
Works (Details)
Most pharmaceutical companies involved in transdermal product
line are focused on contraception, hormone replacement therapy
and smoking cessation. However our company, through extensive
literature study, dedicated effort, and many year's experience
in herbal treatments, realized the importance of the skin as
an organ and sought to provide relief for many of the common
diseases that constitute sever health problems to people and
often lead to chronic overwhelming illness.
Topically applied remedies provide controlled release of herbs
directly into the bloodstream through the skin. They provide
a number of advantages over conventional methods of herbal administration,
including:
• Enhanced efficacy.
• Increased safety.
• Greater convenience
• By delivering a steady flow of herbs into the bloodstream
over an extended period of time, transdermal systems can avoid
the "peak and valley" effect of a oral therapy and
can enable more controlled, effective treatment.
• By avoiding first pass metabolism through the gastrointestinal
tract and the liver, the therapeutically equivalent dosage for
the transdermal delivery of certain compounds can be significantly
less than the corresponding oral dosage, potentially reducing
dosage related side-effects.
• Easy to terminate dosing if adverse reaction occurs.
Skin Support - Rosacea Treatment Delivery System:
• The concentration and solubility of the active ingredients:
high concentration or solubility penetrate better (high concentration
gradient)
• Vehicle viscosity: viscosity reduces diffusion coefficient.
• Vehicle composition: non-aqueous solvents increase penetration.
• Penetration enhancers: disrupt skin surface causing
faster penetration.
• Area for absorption: increased area causes increased
absorption.
Physiological conditions in skin:
• Dead cells and lipid accumulation in the stratum corneum
decreases initial transport.
• Sebum-pH, amount and composition alter passage.
• Hydration of the skin ( differ according to the person's
age and skin location): increased hydration usually increases
penetration rate.
• Thickness of the skin: Thin skin causes increased penetration
rate e.g. the skin behind the ear is very thin while that of
palm of hand is very thick.
• Injury- open cuts and grazes increase penetration rate.
• Temperature: Theoretically, a positive relation is expected
between skin temperature and the percutaneous penetration of
topically applied substances. Studies showed that temperature
effect with the highest penetration is at 38.2 degrees C (4).
Skin Permeation Enhancers
One literature review found more than 275 chemical compounds
cited as skin penetration enhancers (5).
Most of those compounds were generally recognized as safe (GRAS)
ingredients that would often be considered inert by a formulator.
Complete texts concerning pharmaceutical skin penetration enhancement
are available and they provide excellent descriptions and critical
reviews of this subject (6,7,8).
Although there are many strategies to enhance skin permeation,
some of them include the use of chemical skin penetration enhancers.
We use natural additives that:
• Alter the solubility of the active ingredient in the
formulation (including supersaturation), to increase its delivery
through the skin
• Optimize the ionization state of the active ingredients
in the topical remedies (using buffered gel with the proper
pH).
• Enhance the skin permeation (adding natural skin permeation
enhancers).
Topical products often contain many components that are considered
inert excipients with respect to the pharmacology:
• Solvents and cosolvents are used to alter drug solubility
or ease of processing.
• Emulsifiers and gelling agents provide the consistency
and properties expected of creams, lotions, and gels.
• Antioxidants and preservatives are provided to extend
shelf life or ensure quality.
• Skin permeation enhancers are added to the topical treatments
to increase skin permeability by reversibly altering the physiochemical
nature of the stratum corneum to reduce its diffusional resistance
(8).
We use the natural skin enhancers which include:
• Iontophoresis: uses electrical potential to carry drug
through the skin, by using active ingredients in buffered gel.
• Linoleic acid and alpha-linolenic: It has been found
that polyunsaturated fatty acids PUFA--Linoleic (LA), alpha-linolenic
(ALA) and arachidonic acids-enhance skin permeation stronger
than monounsaturated fatty acids. The enhancement effects of
fatty acids on penetration through the stratum corneum are structure-dependent,
associated with the existence of a balance between the permeability
of pure fatty acids across stratum corneum and the interaction
of the acids to skin lipids (9).
• Oleic acid: Oleic acid has been studied as a skin penetration
enhancer for topically applied medications, primarily via its
action mainly on the stratum corneum lipid structure. It has
been found to increase the epidermal permeability through a
mechanism involving the stratum corneum lipid membrane. It is
incorporated into skin lipid, disrupt molecular packing and
alter the level of hydration and allow drug penetrates faster
(10).
• Cod-liver-oil The enhancing effect of the marine products
could generally be associated with their content of free unsaturated
fatty acids (11).
• Menthol derivatives as potential skin penetration enhancers
Studies showed that the permeation enhancing effect of l-menthol
is significantly high with short lag time (12). The promoting
activity of the ethyl ether derivative of Menthol is the greatest
of all menthol derivatives. Studies showed that it is the most
promising compound which has the greatest action and relatively
low skin irritancy (13,14). A study has been made to elucidate
the mechanism of skin permeation enhancement and it was concluded
that the increase in skin flux, to eight times the base line,
could be attributed to the effect of menthol on the skin barrier
properties (15). The mechanism of permeation enhancement of
menthol has been studied by some other investigators and they
concluded that it could involve its distribution preferentially
into the intercellular spaces of stratum corneum and the possible
reversible disruption of the intercellular lipid domain. They
suggested the use of menthol as effective penetration enhancer
(16).
• Squalene: Squalene was found to be a very effective
skin permeation enhancer. 12% of the human sebum is composed
of Squalene to which is attributed the natural moisturizing
effect of the sebum. Studies also showed the skin soothing effect
of Squalene (17).
• Glycerol derivatives: Studies concluded that glycerol
monoethers derived from linear saturated fatty alcohols are
very effective permeation enhancers (18).
• Herbal ingredients: have the ability to penetrate the
skin fast. In vivo skin penetration studies of the Chamomile
flavones apigenin, luteolin and apigenin 7-O-beta-glucoside
were carried out with nine healthy, female volunteers. During
seven hours the decline of flavonoid concentration in a saturated
aqueous alcoholic solution filled in application chambers were
repeatedly measured by spectrophotometry at fixed time periods.
It was concluded, that the flavonoids are not only adsorbed
at the skin surface, but penetrate into deeper skin layers.
This is important for their topical use as antiphlogistic agents
(19).
Another study has been done to investigate the permeability
of natural herbal compounds of different range of lipophilicity
through hairless mouse skin and the effect of certain herbal
extract called Senkyu(Ligustici Chuanxiong Rhizome )ether extract
(SEE) as permeability enhancer. It has been found that (Senkyu)
ether extract (SEE) enhanced the permeability of the herbal
ingredient that have moderate permeability rate. The effect
of SEE in vivo was similar to that obtained in the in vitro
experiment. It was concluded that the natural compounds having
high lipophilicity sufficiently permeated into the hairless
mouse skin owing to their accumulative property, and the Senkyu
ether extract enhanced the permeability of the moderately lipophilic
compounds into the skin (20).
By using combination of buffered gel and skin permeation enhancer
in addition to the easily permeable herbal ingredients, extracted
by natural solvents, further increases the flux through the
epidermis. It has been concluded after several studies that
Iontophoresis in combination with enhancers (e.g. linolenic
acid ) transformed the highly compact cells of the Stratum corneum
into a looser network of filaments, disrupted the keratin pattern,
and resulted in swelling of Stratum corneum cell layers of human
epidermis, thus increases the flux of medication through human
epidermis (21).
Our scientists are and will always be appreciating the trust
of their customers all over the world. They will always make
use of their unique creative feature in developing the best
of the topical herbal remedies to protect their customers from
the side effect of the long term use of pharmacological drugs.
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