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Advantages of Microsponges
Microsponges have several advantages which are explained
below:
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Preparation of Microsponges
Drug loading in microsponges can take place in
two ways, by one-step or two-step process; based on
physico-chemical properties of drug to be loaded. If the
drug is typically an inert non-polar material, it will create
the porous structure which is called as porogen. Porogen
drug, which neither hinders the polymerization nor become
activated by it and stable to free radicals is entrapped with
one-step process.
Formulation Considerations
Actives entrapped in microsponge delivery system
can then be incorporated into many products such as
creams, lotions, powders and soaps. While formulating the
vehicle, certain considerations are taken into account in
order to achieve desired product characteristics. These are
as follows:
1. The solubility of actives in the vehicle must be limited.
Otherwise the vehicle will deplete the microsponges
before the application.
2. To avoid cosmetic problems; not more than 10 to 12%
w/w microsponges must be incorporated into the
vehicle.
3. Polymer design and payload of the microsponges for
the active must be optimized for required release rate
for a given time period.
There remains equilibrium between microsponge
and vehicle, and microsponge releases drug in response to
the depletion of drug concentration in the vehicle. Drug
concentration in the vehicle is depleted by absorption of the
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.Equ. (2)
Determination of True Density
The true density of microsponges can be measured
using an ultra-pycnometer under helium gas and can be
calculated from a mean of repeated determinations.
Characterization of Pore Structure
Pore volume and diameter are vital in controlling
the intensity as well as duration of effectiveness of an active
ingredient. Pore diameter also affects the migration of active
ingredients from microsponges into the vehicle in which the
material is dispersed. Mercury intrusion porosimetry can be
employed to study effect of pore diameter and volume on
rate of drug release from microsponges. Porosity parameters
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....Equ. (4)
Where P is the pressure (psi); V the intrusion
volume (mL g1); Vtot is the total specific intrusion volume
(mL g1). The average pore diameter (Dm) is calculated by
using equation,
....Equ. (5)
Envelope (bulk) density (se) of the microsponges is
calculated by using equation,
....Equ. (6)
Where Ws is the weight of the microsponge sample (g); Vp
the empty penetrometer (mL); VHg is the volume of mercury
(mL). Absolute (skeletal) density (sa) of microsponges is
calculated by using equation,
....Equ. (7)
Where Vse = the volume of the penetrometer minus the
volume of the mercury (mL). Finally, the percent porosity
of the sample is obtained from equation,
....Equ. (8)
Pore morphology can be characterized from the intrusion
extrusion profiles of mercury in the microsponges.
Compatibility Studies
Compatibility of drug with reaction adjuncts can be
studied by thin layer chromatography (TLC) and Fourier
Transform Infra-red spectroscopy (FT-IR). Effect of
polymerization on crystallinity of the drug can be studied by
powder X-ray diffraction (XRD) and Differential Scanning
Calorimetry (DSC) [6].
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Manufacturer
Ortho-McNeil
Pharmaceutical, Inc.
Dermalogica
Biomedic
Avon
Skin Medica Inc.
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Sports cream
RS and XS
Retinol 15
Night Cream
Micro Peel
Plus/Acne Peel
Salicylic Peel
20 and 30
Oil Control
Lotion
Lactrex 12%
Moisturizing
Cream
Dermalogical
Oil Control
Lotion
Ultra Guard
hydroquinone and retinol. The microsponges release these ingredients into the
skin gradually throughout the day. This provides the skin with continuous
exposure to hydroquinone and retinol over time, which may minimize skin
irritation. EpiQuin Micro is a prescription moisturizing fading cream that
reduces the impact of these conditions known as melasma, post inflammatory
hyper pigmentation or solar lentigines. Also help in Age spots, Sun spots and
Facial discoloration.
Topical analgesic-anti-inflammatory and counterirritant actives in a
Microsponge Delivery System (MDS) for the management of
musculoskeletal conditions.
A night time treatment cream with Microsponge technology using a stabilized
formula of pure retinol, Vitamin A. Continued use of Retinol 15 will result in
the visible diminishment of fine lines and wrinkles, a noticeable improvement
in the skin discolorations due to aging, and enhanced skin smoothness.
The MicroPeel Plus procedure stimulates cell turnover through the
application of salicylic acid in the form of microcrystals using Microsponge
technology. These microsponges target the exact areas on the skin that need
improvement. The MicroPeel Plus aggressively outperforms other
superficial chemical peels by freeing the skin of all dead cells while doing no
damage to the skin.
Salicylic acid 20%, microsponge technology has excellent exfoliation and
used for stimulation of the skin for more resistant skin types or for faster
results. It will considerably improve pigmentation, fine lines and acne
concerns. Salicylic acid moves easily through the pores, clearing them out
while reducing inflammation. This treatment effectively combats acne leaving
an amazingly smooth and clear complexion.
A feature-light lotion with technically advanced microsponges that absorb oil
on the skin's surface during the day, for a matte finish. Eliminate shine for
hours with this feature-weight lotion, formulated with oil-absorbing
Microsponge technology and hydrating botanicals. The naturally- antibiotic
Skin Response Complex soothes inflammation and tightness to promote
healing. Acne-Prone, oily skin conditions.
Lactrex 12% Moisturizing Cream contains 12% lactic acid as the neutral
ammonium salt, ammonium lactate. Microsponge technology has been
included for comfortable application and long lasting moisturization.
Lactrex also contains water and glycerin, a natural humectant, to soften and
help moisturize dry, flaky, cracked skin.
Exclusive skin response complex soothes and purifies, provides effective skin
hydration, without adding excess oil; eliminate shine for hours with
dermalogical Oil Control Lotion. Oil Control Lotion is a feather-light lotion,
formulated with oil absorbing Microsponge technology and hydrating
botanicals. The naturally antiseptic Skin Response Complex helps soothe and
purify the skin.
Microsponge system that contains dimethicone to help protect a baby's skin
from diaper rash. The new wipe contains a skin protectant that helps keep
wetness and irritants from the baby's skin. The solution is alcohol-free,
hypoallergenic and contains dimethicone, an ingredient found in baby creams,
lotions and skin protectants.
Biomedic
Biophora
Fountain Cosmetics
SDR Pharmaceuticals,
Inc., Andover , NJ ,
U.S.A.
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Aramis
Fragrances
Aramis Inc.
Fig 5. Microsponges
Polymerization
Synthesis
by
Suspension
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