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Microsponges -A Review on its Applications in Topical Sustained Drug

delivery

Preprint · April 2020

DOI: 10.13140/RG.2.2.16502.75848

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Microsponges – A Review on its Applications in Topical Sustained Drug
delivery
Arjun Sai Sreekar Aeila
GITAM Institute of Pharmacy; GITAM (Deemed to be University); Visakhapatnam, Andhra
Pradesh, India.

Abstract
Microsponges was initially formulated for topical delivery of drugs. They are said to be
colloidal carriers which were recently designed and proposed for creating a novel drug
delivery system as their use can solubilize hydrophobic drugs that provide prolonged release
and improving the bioavailability of drugs. They are also being used to modify
pharmacokinetic parameters. In this review we tried to brief about the evolution of
microsponges as effective Drug delivery systems and their recent evaluation parameters
which were designed to use for topical purposes are discussed.
Keywords: Microsponges; Sustained-release; Polymerization; Quasi-emulsion
Introduction:[1-3]
Idea of micro sponge was developed by Won in the year 1987. micro sponge is a polymeric
sponge porous spherical particle consisting the drug. They are used for releasing the drug in a
controlled manner.
The size of microsponges range from 5 to 300 μm in diameter. Microsponges are stable at a
pH range of 1-11 with stand a temperature upto 1300 °C
Microsponges act as self-sterilising agents because bacteria cannot penetrate into them as
their pore size is 0.25 mm. A typical 25mm sphere will have approximately 2,50,000 pores.
The main objective of using microsponge delivery system is to achieve desired concentration
of drug in blood or skin gradually.
Microsponges are used in topically applied drugs to improve their performance. There are
interstitial spaces between the pores that can entrap wide range of active ingredients.
Properties of Microsponges:[4-6]
• When microsponges are given topically, the active pharmaceutical ingredient releases
into the skin progressively and response to a stimuli such as rubbing, temperature, pH.
• Microsponges have good compatibility with many vehicles and excipients.
• They are self-sterilising due to their smaller pore size.
• They provide extended release upto 12 hours.
• Microsponges can absorb oil 6 times in weight.
• They have 50-60% entrapment of drug in their pores.
• They can be easily incorporated into many formulations like creams, lotions, gels,
ointments, tablets.
Advantages:[6-10]
• Microsponges increase the stability of the drug. They improve the efficiency of
treatment
• They improve the efficiency of treatment.
• Microsponges are used in absorbing skin secretions and oiliness.
• They improve the bioavailability of the drug.
• Microsponge delivery system is easy to formulate, they are non-allergic and non-
toxic.
• Microsponges are useful to reduce irritation.
• They can’t penetrate into the skin but they arrange themselves in nooks and corners of
skin and slowly release the entrapped drug.
• Microsponges enhance the performace of the formulation
Properties of active drug loading into microsponge:[11,12]
• The drug or active ingredient should be completely miscible in a monomer or it
should be able of being made miscible by adding a small amount of water immiscible
solvent.
• It should be immiscible or least souluble in water.
• It should not increase the viscosity of the mixture during formulation
• The active ingredient must be stable during polymerization.
• The spherical structures of microspheres should not get collapsed.
• The microsponges should be limited to 10 – 12% w/w of the vehicle otherwise, the
vehicle will deplete the microsponge.
Formulation of microsponges:[15]
There are two methods employed for the preparation of microsponge drug delivery system.
They are :
1. Liquid-liquid suspension polymerization.
2. Quasi emulsion solvent diffusion.
These methods are based on phyisco-chemical properties of drug to be loaded.

Liquid-liquid suspension polymerization:[16-20]

• In this process, the active ingredient and the monomers are dissolved in a suitable
solvent and dispersed into aqueous phase consisting of surfactants or suspending
agents that are used for formation of a suspension.
• Then the polymerization is started by adding a catalyst or by increasing the
temperature until a system with spherical structures are formed.
• After polymerization process, the solvent is removed, isolating the microsponges. The
isolated microsponges are filtered and dried at 40ᵒC for 12 hours.
Fig1: Preparation of Microsponges by Liquid-Liquid Suspension Polymerisation
Quasi emulsion solvent diffusion:[16-20]
In this method, first the inner phase and outer phase are prepared.
To prepare the inner organic phase the polymer is dissolved in a suitable solvent followed by
drug addition and dissolved under ultrasonification at 35°C.
The outer phase is a mixture of polyvinyl alcohol solution in water.
The inner organic phase is poured into the outer phase. After mixing, the mixture is filtrated
to separate the developed microsponges.
The separated microsponges are then subjected to drying in an hot air oven at a temperature
suitable for the polymer.
The active ingredient can be entrapped into the microsponge either in time of preparation or
can be post-loaded after the microsphere structure has been pre-formed. This process is done
when the drug is thermo-labile to withstand the polymerization conditions.

Fig2: Quasi-emulsion
Mechanism of drug release from Microsponges:[21,22]
In topical preparations like gel, cream, or a lotion, when they are applied to the desired area
on the skin, the active ingredients get dispersed out of the globule into the vehicle and
reaches to the target site. Once the equilibrium is reached, the vehicle becomes saturated.
And when applied to the skin, the vehicle becomes unsaturated due to depletion in the
vehicle. This will start a flow of active ingredients from microsponge particle to vehicle and
from it to the skin, until the vehicle is either dried or absorbed.
Even after that, the microsponges on the surface of the skin will continue to gradually release
the active ingredient to the skin for sustained release.
The release can be initiated or triggered by increase in skin temperature or triggering pH
release or due to applied pressure and with water miscibility.
Evaluation of Microsponges :[23-25]
1. Determination of loading efficiency and production yield The loading efficiency (%) of
the microsponges was calculated in accordance to the following equation.
Loading efficiency = (Actual amount of drug present in microsphere / theoretical amount of
drug) × 100
Loading efficiency is the effective amount of active ingredient to be loaded into the
microsponges.
The production yield of the nano and micro particles would be determined by calculation of
the initial weight of the raw materials and the final weight of the nano and microsponges
obtained .
Production yield = (practical mass/theoretical mass)×100
2. Compatibility studies Compatibility of drug with reaction adjuncts would be studied by
thin layer chromatography (TLC) and Fourier Transform Infra-red spectroscopy. Effects of
polymerization on crystalline nature of the drug was studied by powder X-ray diffraction
(XRD) and Differential Scanning Colorimetry (DSC).
3.Morphology and surface topography of microsponges For morphology and surface
topography, the prepared microsponges was coated with gold–palladium under an argon
atmosphere at room temperature and then the surface morphology of the nano and
microsponges was studied by scanning electron microscopy (SEM) .
4. Determination of true density The true density of microsponges is calculated using an
ultra-pycnometer under helium gas and was calculated from a mean repeated determinations.
Selection of monomer is identified both by ultimately to be entrapped and by the vehicle into
which it would be dispersed . Polymers with changing electrical charges or degrees of
hydrophobicity or lipophilicity was prepared to provide flexibility in the production of active
ingredients. Many monomer combinations would be screened for their suitability with the
drugs by studying their drug release profile.
5. Resiliency Resiliency of sponges was reportedly modified to produce beadlets that was
softer in accordance to the needs of the final formulation. Enhanced crosslinking tends to
slow down the rate of release.
6. Particle size determination Free-flowing powders with fine aesthetic attributes were
possible to obtain by regulating the size of particles during polymerization. Particle size
analysis of loaded and unloaded microsponges was performed by laser light diffractometry.
Cumulative percentage drug release from microsponges of different particle size was plotted
against time inorder to study the effect of particle size on drug release. Particles of sizes
between 10 and 25 m were preferred to be used in final topical formulation to avoid
grittiness.
7. Dissolution tests Dissolution profile of microsponges was studied in-vitro by use of
dissolution apparatus USP XXIII with a modified basket consisting of 5m stainless steel
mesh along with a speed of the rotation 150 rpm. The dissolution medium was selected by
considering solubility of active ingredients to intensify sink conditions. Samples from the
dissolution medium was analysed by suitable analytical method.
Applications of Microsonges:[26,27,28]
Microsponge based delivery systems have been one of the key technologies investigated in
the last few years. These systems display a strong rationale for cosmetic and dermal
applications, in order to enhance the therapeutic performance of active molecules, with
improved patient compliance. For effective topical application, the selected preparation
method should result in optimum size range, with uniform distribution of microsponges.
Various polymers used in fabrication of microsponges for topical application result in
formation of a microsponge ‘cage’. In view of the structure and physiology of human skin,
microsponges offer enhanced efficacy of dermatological agents, as well as reduced local
adverse effects. There are other applications of microsponges like Sunscreens,Anti-acne and
Anti-Inflammatory drugs.
Recent advancements in oral microsponge drug delivery :[29,30]
The Microsponge system is effective to hold active ingredients in gastric environment and
provide sustained release delivery of oral medication to the lower gastrointestinal (GI)
tract,the active ingredient will be released upon reacting to specific enzymes in the colon.
New polymers for the delivery of small and large molecule drugs, which includes proteins
and peptides, can also be formulated which, if successful can be used in giving micrisponges
in systemic drug delivery
Conclusion:
Microsponge based delivery systems are one of the key technologies investigated in the last
few years. These systems showed a strong rationale for cosmetic and dermal applications, in
order to enhance the therapeutic performance of active drug molecules, with improvised
patient compliance. Microsponges reportedly offer many advantages in relation to mutagenic
and irritation of drugs. These microsponges show a great potential in future and has a wide
scope in development of sustained- release topical formulations.
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