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Table of Contents
REVIEW ARTICLE
Year : 2021  |  Volume : 10  |  Issue : 2  |  Page : 108-111

Microsponge: An advanced drug delivery system


1 Department of Pharmacy, R V Northland Institute, Greater Noida, Uttar Pradesh, India
2 Saraswathi College of Pharmacy, Hapur, Uttar Pradesh, India

Date of Submission26-Mar-2019
Date of Decision01-Jun-2019
Date of Acceptance18-Jan-2020
Date of Web Publication17-Jul-2021

Correspondence Address:
Kumari Nidhi
Research Scholar, Department of Pharmacy, R V Northland Institute, G B Nagar, Dadri, Greater Noida, Uttar Pradesh - 203207
India
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/JCSR.JCSR_42_19

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  Abstract 


Microsponge drug delivery system (MDS) was developed to deliver the pharmaceutical ingredients efficiently at the site of administration at a limited dose. MDS is based on pore size of sponges. The action of microsponges lasts up to 12 hours. MDS is also dependent on the physicochemical properties of the drug. These are used in bone tissue engineering, for reducing skin irritation and have a self-sterilisation property. This review provides an overview regarding the characteristics, methods of preparation, properties, evaluation, applications and limitations of MDS.

Keywords: Marketed formulation, microsponge, patents, recent advancements, stability


How to cite this article:
Nidhi K, Verma S, Kumar S. Microsponge: An advanced drug delivery system. J Clin Sci Res 2021;10:108-11

How to cite this URL:
Nidhi K, Verma S, Kumar S. Microsponge: An advanced drug delivery system. J Clin Sci Res [serial online] 2021 [cited 2021 Aug 3];10:108-11. Available from: https://www.jcsr.co.in/text.asp?2021/10/2/108/321698




  Introduction Top


The microsponge drug delivery system (MDS) was developed in 1987.[1] MDS, a patented polymeric system consists of porous microspheres. These are minute sponge like spherical particles along with numerous interconnecting voids in a non-collapsible structure. The large porous surface facilitates controlled release of active ingredient. The size of pores varies from 5-300 μm. The internal pore structure can measure upto 10 feet in length, and pore volume of 1 ml/g. This creates in a large pool of storage.This microsponge formulation contains an active ingredient which is released in a controlled manner Microsponge drug delivery consists of quite small, inactive, sphere formulations which do not cross the skin membrane. These formulations are developed to deliver the pharmaceutical ingredients efficiently at the site of administration at minimum dose. These formulations are enhancing stability, modify drug release and reduce side effects.[1],[2]

MDSs is based on the microscopic and polymer-based system. Microspheres are capable of appending or entrap varieties of substances, and they have incorporated in the forms of gel, cream, liquid or powder.[3] MDS is used as an application on the skin and its effect is evident by applied pressure. The microsponge formulations can also contain water-soluble substances (antiseptics/antiperspirants).[4]


  Characteristics Top


Microsponges can have a continuous (extended-release) action for up to 12 hours.[5] The pore size is 0.25 μm and these have a self-sterilising property.[6] These formulations are stable at 130 °C.,[6] are non-toxic, non-allergenic, non-irritating and non-mutagenic.[7] Microsponges do not require addition of preservatives.[8]

MDDS can reduce irritation therby improvingpatient's compliance.[9] These have the ability to improve formulation flexibility[4] and can facilitate extended-release formulations.[4] However,absorption of residual monomers may cause a toxic effect.The preparations of microsponge mostly use organic solvents and some may be highly inflammable and they can cause environmental hazards.[10]


  Methods of Preparation Top


This system is based on physicochemical properties of the drug molecules used in the formulations. The two methods of preparation of MDS can be one-step (liquid–liquid suspension polymerisation method) or two-step process (quasi-emulsion solvent diffusion method).[11]

Liquid–liquid suspension polymerisation method

Liquid–liquid suspension polymerisation method contains two phases. In the first phase active ingredients form solution i.e., non-polar solution. The second phase (aqueous phase) is addition of surfactant or dispersing agents. In this method, the first phase is dispersed in the second phase and this is done by polymerisations process with the help of catalyst,increased temperature or irradiation process The steps involved include selection of active ingredients or monomers; formation of monomer chain as the polymerisation takes place; and formation of spherical particles of microspheres (agglomeration). This results in bunches of microspheres and these bunches are joined together to form microsponges.[11],[12],[13]

Quasi-emulsion solvent diffusion method

Quasi-emulsion solvent diffusion method is a two-step process and increases the sensitivity of the drug release. This method uses different amounts of polymer. This consists of two phases i.e., internal phase and external phase.The internal phase consists of polymer such as Eudragit RS-100 (low permeability). This polymer is cationic and non-biodegradable and entrapment efficiency was found to increase with increased amount of Eudragit RS-100. The external phase consists of polyvinyl alcohol (PVA) with distilled waterInternal phase containing Eudragit RS-100 is dissolved in a solvent like ethyl alcohol at 35 °C under ultrasonication so that the internal phase is dispersed in the external phase containing PVA solution in water. The solution is stirred and 1 hour andis filtered to obtain the solid microsponges. This solid microsponge is dried in an oven at 35 °C- 40 °C for 12 hours. before use[14],[15],[16]


  Evaluation of Microsponge Top


Evaluation of microspnge is done by dissolution drug-release studies using USP basket apparatus at 37 °C ± 0.5 °C.[14] The USP Basket has a stainless steel mesh of 5 μm pore size. The rotation speed of basket is 150 rpm. The surface characteristics and the morphology of the microsponge are evaluated by scanning electron microscopy. Particle size of microsponges can be determined by laser light diffractometry. True density determination is done by an ultra-pycnometer under helium gas.[17],[18],[19],[20] Microsponge pore diameter can be calculated using the Washburn equation.[21]

Compatibility studies of microsponge are done using thin-layer chromatography and infra-red spectroscopy. Viscoelastic properties need to be defined according to the microsponge requirements for producing caplet that is flexible or crippled. In vitro diffusion studies of microsponge are done using a Keshary–Chien diffusion cell (cellophane membrane). In this, a receptor compartment is used i.e., 100 mL of phosphate buffer and 500 mg gel loaded 10 mg of a drug are dispersed on the cell membrane. Then, this is maintained at 37 °C ± 0.5 °C temperature for a predetermined time interval stirring the solution using Teflon-coated magnetic bars at. Five mL of solution is now removed from the compartment and 5 mL of fresh phosphate buffer is added. Finally, the drug concentration is measured by using spectro-photometrically with comparing blank solution. This process is repeated three times.[22],[23],[24]


  Applications of Microsponge Systems Top


MDS is used for enhancing the safety profile and efficacy of the over-the-counter drugs. Microsponge has microscopic spheres and these are capable of getting absorbed into skin secretions and also have a function to reduce oil from the skin and they provide shine to the skin. When used in anti-acne agents, they have a function to reduce or decreased irritation from the skin. This drug delivery technology is used in bone tissue engineering.[25],[26]


  Recent Advances in Microsponge Formulation Top


Advances in technology developed by adapting the methods to form nanosponges and porous micro pellets include Cyclodextrin (CD) based nano-sponges for drug delivery. These advanced drug delivery systems are utilized for oral administration of various drugs such as dexamethasone, flurbiprofen, doxorubicin hydrochloride, itraconazole, This This β-CD molecule is cross-linked by reacting the β-CD with biphenyl carbonate and these form the nanosponges as advanced formulation. Researchers have observed that the addition of a cytotoxic substance as the carrier system in the formulation that can be increased the drug potency and can be used in targeting the cancer cells and also as carriers for the delivery of gases.[27]

Topical anti-inflammatory gels of naproxen entrapped in Eudragit based microsponge delivery system has recently become available. In recent research, naproxen containing Eudragit RS-100, carbopol and PVA has been developed by quasi-emulsion method.[28],[29] Design and in vitro characterisation of betamethasone microsponge loaded topical gel is arecent develpement in betamethasone microsponges formulation for topical anti-inflammatory action by using Quasi-emulsion method.[30] Recent research has also made available, microsponge formulation containing controlled release risperidone used in the treatment of schizophrenia and schizoaffective disorders.[31]

Formulation, optimisation, development, and evaluation of microsponge gel of fluconazole has also been described.[32] Ther are many market preparations uqing MDS[33],[34],[35],[36],[37] [Table 1].
Table 1: Marketed formulations of Microsponge

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Microsponges were successfully prepared by a quasi-emulsion solvent diffusion method using Eudragit Rs 100 and PVA with distilled water and liquid–liquid suspension polymerisation method. These have a potential for improved stability, enhanced formulation flexibility reduction in side effects while maintaining their therapeutic efficacy.

Financial support and sponsorship

Nil.

Conflicts of interest

There are no conflicts of interest.



 
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Draize JH, Woodard G, Calvery HO. Methods for the study of irritation and toxicity of substances applied topically Khopade AJ, Jain sanjay, Jain NK. “The Microsponge”. Eastern Pharmacist, 1996, 49-53.  Back to cited text no. 25
    
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Leyden JJ, Shalita A, Thiboutot D, Washenik K, Webster G. Topical retinoids in inflammatory acne: A retrospective, investigator-blinded, vehicle-controlled, photographic assessment. Clin Ther 2005;27:216-24.  Back to cited text no. 26
    
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Trotta F, Cavalli R, Tumiatti W. Cyclodextrin-based nanosponges for drug delivery. J Inc Phenom Macrocyclic Chem 2006;56:209-13.  Back to cited text no. 27
    
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Rajurkar VG, Tambe AB, Deshmukh VK. Topical Anti-Inflammatory Gels of Naproxen Entrapped in Eudragit Based Microsponge Delivery System. J Adv Chem Eng 2015;5:1-6.  Back to cited text no. 28
    
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30.
Mohanty D, Bakshi V, Rashaid MA, Reddy TV, Dholakia NA, Babu AM. Design and in-vitro characterization of betamethasone microsponge loaded topical gel. Int J Pharma Res Health Sci 2016;2:1124-9.  Back to cited text no. 30
    
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Bhandare CR, Katti SA. Formulation of microsponges of risperidone HCL. Int J Res Pharm Chem 2016;6:518-27.  Back to cited text no. 31
    
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Kumar R, Kumar M, Babita, Saini N, Kumari N, Kumar R. Formulation, optimization, development, and evaluation of microsponge gel of fluconazole. Int J Sci Eng Appl Sci 2016;2:15-22.  Back to cited text no. 32
    
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Lee JB, Hong J, Bonner DK, Poon Z, Hammond PT. Self-assembled RNA interference microsponges for efficient siRNA delivery. Nat Mater 2012;11:316-22.  Back to cited text no. 33
    
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