Applications of microsponge1

Applications Of Microsponge
Prepare by,
Madhavi A. Kuchekar
Guided by,
Sonali P. Mahaparale
Dr. D.Y. Patil college of pharmacy, Akurdi, Pune

 Contents
Introduction
 Preparation of microsponge
 Release mechanism
 Physical characterization
 Applications of microsponge
 Conclusion
 References

 The Microsponge technology was developed by Won in 1987.
 Microsponges are polymeric delivery systems composed of porous
microspheres.
 They are tiny sponge- particles with a large porous surface which
are spherical in shape having reduce side effects, enhance stability,
modify drug release.
 Microporous beads are unique technology for the controlled
release of topical agents which consists of 10-25 microns in
diameter, loaded with active agent

 uniform, spherical, porous polymeric
microspheres
 particle size range 5-300μm
 a typical 25μm sphere can have up to 250000 pores(Figure 2) and an
internal pore structure equivalent to 10ft in length, providing a total
pore volume of about 1ml/g.
 compatible with most vehicles and ingredients; higher payload (50 to
60%), still free flowing, self-sterilizing as average pore size is 0.25μm
where bacteria cannot penetrate

 Conventional topical preparation releases their active ingredient
upon application and produces highly concentrated layer of drug
which is rapidly absorbed.
Microsponge delivery system can prevent the accumulation of
active ingredient and reduces the irritation at site of application
and also helps in maintaining the efficacy of drug.

 Microsponge delivery system can control the release rate of
actives which is not possible in case of microcapsules, where once
the wall is ruptured the active ingredient will be released.
 Liposome formulations suffer from lower payload, formulation
difficulty, limited chemical stability and microbial instability.
Microsponge delivery system can help to overcome these
problems.
 Microsponge system increases the amount of time for which the
actives remains present on skin surface and reduces its
transdermal penetration.

 Microsponges can absorb oil up to 6 times its weight without drying.
 It provides continuous action up to 12 hours i.e. extended release.
 Improved product elegancy.
 Lessen the irritation and better tolerance leads to improved patient compliance.
 It can also improve efficacy in treatment.
 They have better thermal, physical and chemical stability.
 These are non-irritating, non-mutagenic, non-allergenic and non-toxic.
 MDS allows the incorporation of immiscible products.
 They have superior formulation flexibility.

 Microsponge formulations are stable over range of pH 1 to 11;
 Microsponge formulations are stable at temperature up to 130oC;
 Microsponge formulations are compatible with most vehicles and
ingredients;
 Microsponge formulations are self sterilizing as their average pore
size is 0.25μm where bacteria cannot penetrate;
 Microsponge formulations have higher payload (50 to 60%), still free
flowing and can be cost effective.

 It should be either fully miscible in monomer or capable of being
made miscible by addition of small amount of a water immiscible
solvent.
 It should be water immiscible or at most only slightly soluble.
 It should be inert to monomers.
 It should be stable in contact with polymerization catalyst and
conditions of polymerization.
 should not increase the viscosity of formulation.

liquid-liquid suspension quasi emulsion solvent
polymerization diffusion technique
Based on physico-chemical properties of drug to be loaded.
Drug loading in microsponges
One Step
Process
Two step
Process

In liquid-liquid systems the porous microspheres are prepare
by suspension polymerization method.
The various steps in the preparation of microsponges are-
Monomers + active ingredients dissolved in a suitable
solvent
Solution of monomer and are then dispersed in the
aqueous phase, which consist of additives
polymerization is then initiated by adding catalyst or by
increasing temperature or irradiation.

Reaction vessel for microsponge preparation by liquid-
liquid suspension polymerization

This is the two-step process and microsponge are prepared by
using different polymer amount.
This method consists of two phases:
 External phase: It includes the 40mg polyvinyl alcohol in
200ml distilled water.
 Internal phase: The internal phase consists of drug, ethyl
alcohol, triethyl citrate and polymer. triethyl citrate is used to
facilitate the plasticity and it is added at an amount of 20% of
the polymer.

Method of Quasi-Emulsion Solvent Diffusion

Microsponges Synthesis by Suspension
Polymerization

The release of drug through microsponges can be initiated by
following triggers:
 Solubility: Release can be achieved by diffusion taking into
consideration the partition coefficient of the actives into
microsponges and outside system.
 pH triggered system: The modification in coating of
microsponges can be used to achieve the pH based drug
release.

 Pressure: The release of drug from microsponges can
be achieved by applying the pressure or by rubbing.
 Temperature triggered system: The flow rate and release
of the actives which are too viscous at room
temperature can be increased by increasing the skin
temperature.

1. Particle Size Determination:
Particles larger than 30 μm.
 particles of sizes between 10 and 25 μm.
Particle size analysis of loaded and unloaded microsponges can
be performed by laser light diffractometry or any other suitable
method.
2. Morphology And Surface Topography of Microsponges
SEM of a fractured microsponge particle can also be taken to
illustrate its ultrastructure.

3. Determination of Loading Efficiency And Production
Yield:
 Loading efficiency = Actual Drug Content In Microsponges
Theoretical Drug Content × 100-Eqn no.
 Production Yield (PY)
= Practical Mass of Microsponges
Theoretical Mass (polymer+ drug) × 100-Eqn no.
4. Determination of True Density:
Use ultra- pycnometer under helium gas and was calculated from a
mean of repeated determinations.

5. Compatibility studies:
Thin layer chromatography (TLC)
Fourier Transform Infra-red spectroscopy (FT-IR)
powder X-ray diffraction (XRD)
Differential Scanning Colorimetry (DSC)
6. Polymer/ Monomer Composition:
 Polymer composition of the MDS can affect partition
coefficient of the entrapped drug between the vehicle and
the microsponge system and hence have direct influence
on the release rate of entrapped drug.
 Release of drug from microsponge systems of different
polymer compositions can be studied by plotting
cumulative % drug release against time.

7.Characterization of pore structure:
Use mercury intrusion porosimetry.
8. Resiliency (viscoelastic properties):
Resiliency of microsponges will be studied and optimized as
per the requirement by considering release as a function of
cross-linking with time.
9. Dissolution studies:
 Use of dissolution apparatus USP XXIII with a modified
basket consisted of 5μm stainless steel mesh.

 Microsponge for topical delivery
The Microsponge for Oral Delivery
 Micro sponges for biopharmaceuticals delivery
 Microsponge for Bone and Tissue Engineering
Microspong From Seaweed Use In Diagnose the
Diseases.
Self-Assembling RNAi Microsponges

Applications of microsponge drug delivery system

Microsponge for topical delivery
 The Microsponge system can prevent excessive
accumulation of ingredients within the epidermis and the
dermis.
 Microsponges consisting of non-collapsible structures with
porous surface through active ingredients are released in a
controlled manner.
 Microsponge systems are made of biologically inert
polymers.
 Extensive safety studies have demonstrated that the
polymers are non-irritating, nonmutagenic, non-allergenic,
non-toxic and non- biodegradable
 Eg: Sunscreens, Antidandruff, Anti-acne, Skin de-
pigmentation products

The Microsponge for Oral Delivery
 Increase the rate of Solubilization of poorly water soluble
drugs by entrapping such drugs in the Microsponge system's
pores.
 that the time it takes the Microsponge system to traverse the
small and large intestine is significantly increased thus
maximizing the amount of drug that is absorbed.
 Controlled oral delivery of ibuprofen microsponges is
achieved with an acrylic polymer, eudragit RS, by changing
their intraparticle density.
 Eg; Paracetamol , Ibuprofen

Microsponges for biopharmaceuticals
delivery
 The micro sponge delivery system (MDS) is employed for both
in the delivery of biopharmaceuticals as well as in tissue
engineering.
 Poly (lactic-co-glycolic acid) has been used as a biodegradable
scaffold which was compounded with collagen microsponge to
form a vascular patch material.
 The poly (lactic-co-glycolic acid)–collagen patches with or
without autologous vessel cellularization were used to patch the
canine pulmonary artery trunk.
 Use in cardiovascular surgery and bioengineered material for
promoting in situ cellularization.
 Eg; Poly (lactic-co-glycolic acid)

Microsponge for Bone and Tissue
Engineering
 Bone-substitute compounds were obtained by mixing pre
polymerized powders of polymethylmethacrylate and liquid
methylmethacrylate monomer with two aqueous dispersions
of tricalcium phosphate grains and calcium deficient
hydroxyapatite powders.
 The injection of collagen microsponges incorporating bFGF
induced a significant increase in the blood flow, in the murine
ischemic hind limb, which could never have been attained by
the bolus injection of bFGF.

Microspong From Seaweed Use In
Diagnose the diseases.
 Microsponges derived from seaweed may help diagnose
heart disease, cancers, HIV and other diseases quickly and
at far lower cost than current clinical methods.
 The microsponges are an essential component of Rice
University's Programmable Bio-Nano-Chip (PBNC).
Fig:Programable Bio-nano Cheap

Self-Assembling RNAi Microsponges
 Microsponges that act as both carrier and cargo for the
delivery of gene-silencing RNA (siRNA) into cells.
 The RNAi-microsponge presents a novel materials system in
general owing to its unique morphology and nanoscale
structure within the polymer particle.
 Provides a promising self-assembling material that
spontaneously generates a dense siRNA carrier for broad
clinical applications of RNAi delivery using the intrinsic
biology of the cell.”

Fig:Formulation of siRNA Microsponge

 The microsponge drug delivery technology is widely applicable
to the dermatological drug delivery products.
 The microsponge drug delivery system has properties like
improved stability and enhanced flexibility in formulation.
 MDS is originally developed for topical delivery of drugs like
anti-acne, anti-inflammatory, anti-fungal, anti-dandruffs,
antipruritic, rubefacientsetc. But MDS also expands its
application in oral drug delivery, bone and tissue engineering, in
detecting the diseases and inRNAi silencing.

 Netal A, Bajaj A and Madan M. Development of
Microsponges for Topical Delivery of Mupirocin, AAPS
Pharm. Sci. Tech, 2009;10(2):123-128.
 Jelvehgari M, Siahi-Shadbad MR and Azarmi S.
Themicrosponge delivery system of benzoyl peroxide:
Preparation, characterization and release studies. Int J
Pharm 2006;308:124-13
 Nacht S and Katz M. The microsponge: a novel topical
programmable delivery system. Topical drug delivery
formulations. New York: Marcel Dekker; 1990. pp. 299–325.
 Microsponges from seaweed may save lives Rice University
scientists refine process at heart of diagnostic Bio-Nano-
Chip.

 http://www.microsponge.com/images/microspongepartic
le.jpg
 http://www.pharmainfo.net/files/images/stories/article_images
/ReactionVesselForMicrospong ePreparation.jpg.
 http://www.pharmainfo.net/files/images/stories/article_images
/PreparationOfMicrosponges.jpg.
 Thompson J., Bau H., J Chrom B., 878:228–236, (2010).
 Nature MaterialsFebruary 27, (2012).
 MIT's Paula Hammond on siRNA Delivery Via All-RNA
Microsponges March 01, (2012).

Applications of microsponge1

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