Microsponge Delivery System Research Articles

Formulation of microsponges of anti-fungal drugs and their pharmacokinetic and in vitro analysis

Microsponges are uniform, spherical, porous polymeric microspheres having myriad interconnected voids of particle size range 5-300 μm. These microsponges have the capacity to entrap a wide range of active ingredients such as emollients, fragrances, essential oils, sunscreens and anti-infective, etc. and then release them onto the skin over a time in response to a trigger. Microsponge Delivery System (MDS) can be used to resolve the problem associated with these conventional approaches. The drug entrapped microsponges can be incorporated into a formulated product, such as a gel, cream, liquid or powder. Microsponge is as tiny as a particle of talcum powder. Although they are microscopic in size, these systems are too large to pass through the stratum corneum thus preventing excessive accumulation of drugs within the epidermis and dermis, and hence systemic entry of the drugs. They increase the rate of solubilization of poorly water soluble drugs by entrapping such drugs in pores of the microsponges. In this study, Flutrimazole and Oxiconazole nitrate microsponge were prepared by quasi-emulsion solvent diffusion method. The microsponges thus prepared, were evaluated for production yield, loading efficiency, particle size analysis, SEM, IR, DSC, PXRD, characterization of pore structure, in-vitro release study of microsponges, and stability. Then, gels loaded with microsponge and plain drug were formulated and evaluated for rheology, diffusion, skin irritation and antifungal activity. Antifungal activity of Flutrimazole and Oxiconazole nitrate containing microspongic gels were compared with marketed formulations. The microsponges showed good production yield, loading efficiency and particle size. All characteristic peaks of the drugs were concordant with IR spectra of pure drugs. PXRD and DSC studies revealed amorphization of drugs. SEM images showed that styrene microsponges prepared by suspension polymerization were finely spherical and uniform, while Eudragit microsponges prepared by quasi-emulsion solvent diffusion method were comparatively less spherical. According to intrusion and extrusion curves, majority of the pores present in Eudragit microsponges were spherical type, whereas the pores of styrene microsponges were mainly cylindrical-hole type. BET multipoint adsorption isotherm studies revealed that the percent of porosity of styrene microsponges is comparatively higher than Eudragit based microsponges. During the storage of drug-entrapped microsponges at 40±2°C and 75±5% RH for 6 months, surface morphology and release of drug showed no notable changes. Viscosity determination of gel showed that gels loaded with microsponge are more viscous than gel loaded with plain drug. The controlled drug release was observed with all the microspongic gels. Antifungal activity of gels containing microsponge entrapped Flutrimazole and Oxiconazole nitrate showed that antifungal activity of drugs was retained even after entrapment in microsponges and it was higher as compared with the gel containing free drug and marketed formulation. Gels containing drugs entrapped in microsponges.

Microsponges: A Neoteric approach for the effective management of Osteoarthritis.

A microsponge delivery system (MDS) is a cutting-edge and distinctive method of structured medication delivery. Regulated drug distribution is now possible with the use of microsponge technology. Techniques for drug release are created specifically to distribute medications to the body's various locations. As a result, pharmacological therapy becomes more effective, and patient compliance significantly affects the health care system. MDS consists of porous microspheres with a substantially porous structure and a very small spherical shape, ranging in size from 5 to 300 microns. MDS is typically used to administer medications through topical channels, but new research has demonstrated the promise of this technique for parenteral, oral, and ocular drug delivery. Topical formulations are an attempt to manage diseases like osteoarthritis, rheumatoid arthritis, psoriasis, etc. While reducing the drug's side effects, MDS can readily change the pharmaceutical release shape and enhance formulation stability. Reaching the highest peak plasma concentration in the blood is the main goal of microsponge medication delivery. The ability of MDS to self-sterilize is by far the most notable quality. In countless studies, MDS is employed as an anti-allergic, anti-mutagenic, and nonirritant. This review covers the overview of microsponges along with their release mechanism. The article focuses on the marketed formulation of microsponges and patent data of the same. This review will be helpful for researchers working in MDS technology.

MICROSPONGES: AN INNOVATIVE TECHNIQUE FOR BIOMEDICAL RESEARCH

A microsponge delivery system (MDS) is a cutting-edge and distinctive method of structured drug delivery. Controlled drug delivery is now possible with the use of microsponge technology. MDS consists of porous microspheres with a substantially porous structure and a very small spherical shape, ranging in size from 5 to 300 microns. MDS is typically used to administer medications through topical channels, but new research has demonstrated the promise of this technique for parenteral, oral, and ocular drug delivery. While reducing the drug's side effects, MDS can readily change the pharmaceutical release shape and enhance formulation stability. Reaching the highest peak plasma concentration in the blood is the main goal of microsponge medication delivery. The most notable quality of MDS is their ability to self-sterilize. MDS is employed in countless studies as an anti-allergic, anti-mutagenic, and non-irritant. This review discusses formulation, eligibility requirements for medications to be included in MDS, formulation processes, evaluation criteria, and the function of MDS in the treatment of various illnesses. In the future, while researching MDS in other illnesses, this review will be quite helpful.

Microsponges as Drug Delivery System: Past, Present, and Future Perspectives.

Microsponges are polymeric delivery devices composed of porous microspheres that range in size from 5 to 300 micrometers. These have been explored for biomedical applications such as targeted drug delivery, transdermal drug delivery, anticancer drug delivery, and bone substitutes. The purpose of this study is to conduct a comprehensive analysis of recent developments and prospects for a microsponge-based drug delivery system. The current study analyzes how the Microsponge Delivery System (MDS) is made, how it works, and how it can be used for a wide range of therapeutic purposes. The therapeutic potential and patent information of microsponge-based formulations were systematically analyzed. The authors summarize various effective techniques for developing microsponges, such as liquid-liquid suspension polymerization, quasi-emulsion solvent diffusion method, water-in-oil-in-water (w/o/w) emulsion solvent diffusion, oil-in-oil emulsion solvent diffusion, lyophilization method, porogen addition method, vibrating orifice aerosol generator method, electrohydrodynamic atomization method, and ultrasound-assisted microsponge. Microsponge may reduce the side effects and increase drug stability by positively altering drug release. Drugs that are both hydrophilic and hydrophobic can be loaded into a microsponge and delivered to a specific target. The microsponge delivery technology offers numerous advantages over conventional delivery systems. Microsponges, which are spherical sponge-like nanoparticles with porous surfaces, have the potential to increase the stability of medications. They also efficiently decrease the undesirable effects and alter drug release.

A CONCISE LITERATURE REVIEW ON STUDY OF MICROSPONGES FROM ANCIENT TO RECENT

Polymeric microspheres enclosing an extremely porous surface are termed as microsponges. Microsponges are drug loaded microporous beads having 10-25 micron diameter. These may augment stability, ease side effects and amend drug release. Microsponge systems have capability to capture ample drug substances and are then formulated into various products like gel, cream, liquid or powder. Several research studies corroborated that microsponge entities possess non-irritant, non-mutant, non-allergic and non-toxicity features. Suitable analytical techniques for characterization of microsponges can be illustrated for suitable characteristic properties such as thickness, particle size and its distribution, surface and pore properties. Many problems such as repulsive odor, greasiness and skin exasperation are resolved by MDDS (microsponge drug delivery system). MDDS generates prolonged release and site specific action. In this review article, a concise outline of MDDS covering the principle, methods of formulation and characterization have been discussed. Microsponge delivery system (MDS) is primarily utilized for topical and oral formulations but it is also being explored for cosmetic formulations.

Microsponge Drug Delivery System: Emerging Technique in Novel Drug Delivery System and Recent Advances

A number of advancements have been made in the drug delivery system in order to achieve the goals of improved efficacy and cost-effectiveness in therapy. Controlling the rate of release of active drugs to a predetermined site in the human body has been one of the pharma industry's most challenging tasks. Microsponges are porous cross-linked, non-collapsible microspheres with a size range of 5-300µm that can entrap a variety of drugs and then be incorporated into a formulated product like gel, cream, powder, or liquid. Controlled release of drugs onto the epidermis with the confidence that the drug remains primarily localized and does not enter the systemic circulation in substantial amounts is a field of research that the microsponge delivery system is progressively exploring. In order to remove systemic exposure and minimize local cutaneous reaction to active drugs, microsponge technology has been introduced in topical drug products to facilitate the controlled release of the active drugs into the cell. Also, numerous studies have shown that microsponge systems are non-irritating, non-mutagenic, non-allergenic, and non-toxic. MDDS technology is being used currently in cosmetics, over-the-counter (OTC) skin care, sunscreens, and prescription products and has recently been used in oral drugs as well as biopharmaceuticals (protein, peptides, and DNA based therapeutics) drug delivery. The purpose of this article is to provide information about microsponges such as the method of preparation, mechanism of drug release from microsponges, characterization, applications of microsponges, and information about microsponges updated research.

Review on Microsponges a Novel Drug Delivery System

Bottom of Form Microparticulate drug delivery systems have shown a good interest within the pharmaceutical space. they permit the rise of drug therapeutic effectiveness and therefore the reduction of aspect effects. during this context, microsponges represent a brand new model of porous uu microspheres, which permit the defense of a good vary of active agents. Microsponge drug delivery system (MDS) was developed to deliver the pharmaceutical ingredients efficiently at the positioning of administration at a restricted dose. MDS is predicated on pore size of sponges. The action of microsponges lasts up to 12 hours. A microsponge's delivery system could be a extremely cross-linked, porous, chemical compound microsphere, chemical compound system consisting of porous microspheres that may entrap and unleash them into the skin over long amount. This delivery system provides extended release with reduced irritation, higher tolerance, improved thermal, physical and chemical stability. Microsponges area unit ready by many technique utilization emulsion system or by suspension chemical process into a liquid-liquid system. Microsponges will entrapped numerous style of drug and incorporated in formulation like cream, powder, gels, and lotions. Topical preparation have some disadvantages like unpleasant odour, oiliness and skin irritation and fail to achieve the circulation this drawback is overcome by microsponges delivery system.

An Innovative Strategy, Current Status and Future Prospects for Microsponge Technology

In the rapidly evolving field of novel drug delivery technology, microsponges are at the forefront Scientist have become increasingly intrigued by microsponge drug delivery technology because it holds great promise for achieving the goal of controlled and specific drug delivery, and it has thus captured the interest of many researchers. The microsponge delivery system, an innovative technology for controlled drug delivery, is a polymeric delivery system that contains porous microsphere range in size from 5 to 300μm. Microsponge structure is not irritating, non-mutagenic, non- allergic or toxic, as shown by multiple studies. This article provides a comprehensive explanation of the microsponge delivery system, as well as a theoretical and practical overview. In this section, the basic principle of particle size distribution, surface morphology and porosity are discussed as appropriate analytical techniques to characterize microsponges. They are also discussed in term of the recent advancements in microsponge delivery systems and their future prospects.

Microsponge Mediated Targeted Drug Delivery System for the Treatment of Fungal Infection

The microsponge delivery system is a profoundly cross-connected permeable, polymeric microsphere, polymeric system comprising of permeable microspheres that can capture and delivery them into the skin throughout a significant stretch of time. This system furnishes broadened discharge with diminish disturbance, better resistance, worked on warm, physical and compound steadiness. The principal objective of any prescription transport structure is to achieve needed gathering of the medicine in blood or tissue, which is therapeutically incredible and non-noxious for a somewhat long period in this review different strategy for planning of microsponge drug delivery system are considered. Different benefits are likewise given which shows the significance of this strategy for the delivery of medication over the other medication delivery system. An ever increasing number of advancements in delivery system are being coordinated to enhance the adequacy and cost viability of the treatment. Microsponge innovation offer entanglement of fixing and is accepted to contribute towards lessen incidental effects, further developed strength, expanded style, and improved plan adaptability. Furthermore various examinations have affirmed that microsponge systems are not bothering, non-mutagenic, non-allergenic and non-harmful Microsponge delivery innovation is being utilized at present in beauty care products, over the counter, healthy skin, and sunscreen and remedy items.

Formulation and Evaluation of Luliconazole Microsponges Loaded Gel for Topical Delivery

Microsponge containing Luliconazole (LCZ) with different proportion of drug:polymer (Ethyl cellulose and Eudragit RS 100) were obtained efficiently using Quasi-emulsion solvent diffusion method. Luliconazole is an anti-fungal drug used for the topical delivery. The purpose of the microsponge formulation is to control the release of LCZ drug to the skin through Microsponge Delivery System (MDS) known to be the novel technique which overcome the maximum concentration of active ingredient, frequency doses, and skin irritation. The prepared microsponges were examined using drug content, % production yield, % entrapment efficiency and in-vitro drug release. The formulation were subjected to in-vitro drug release studies for 6 hr in which it was concluded that Ethyl cellulose microsponges formulated by drug:polymer (1:1) and Eudragit RS 100 microsponges formulated by drug:polymer (1:3) showed maximum controlled release i.e., Increase in drug:polymer ratio (1:1 to 1:9) increased the production yield and entrapment efficiency of microsponges using Ethyl cellulose with no significant effect for Eudragit RS 100.Therefore, both formulation F1 and F2 was dispersed in carbopol gel preparation for controlled delivery of LCZ to the skin. Various physical parameters like pH, spreadability, viscosity and in-vitro drug diffusion studies were evaluated for the prepared gel formulations. Microsponge gel formulation i.e., FG1 showed better results for controlled release of 89.40% as compared to FG2 i.e., 92.18% over the period of 12 hrs which is performed in Franz Diffusion Cell. On basis of in-vitro diffusion studies for LCZ gel formulation, microsponges using Ethyl cellulose (FG1) was found to be best for its controlled release of LCZ for 12 hrs and followed zero order kinetics. Hence, formulated LCZ loaded gel have potential to treat fungal infections i.e., tinea pedis, tinea cruris and tinea corporis.

Formulation and Evaluation of Eudragit Rl100 Polymeric Drug Loaded Microsponge for Ophthalmic Use

Aims: The aim of this work is the formulation of Eudragit RL100 polymeric microsponges. The Microsponge Delivery System is a patented technique in which there is a polymeric system consisting of porous particles.
 Methodology: The ratio of Diclofenac sodium and eudragit RL100 varied from 1:1 to 13: 1 to formulate microsponge. Dichloromethane was used as internal phase and polyvinylalcohol was used as an external phase. The formed microsponges were characterized for particle size, entrapment efficiency, drug content, in vitro drug release and SEM.
 Results: With increase in drug: polymer ratio there is increase in production yield from 20.04% to 72.14%, and entrapment efficiency from 20.11% to 70.77%. Drug content of formed microsponge varied between 50.18% to 91.09% whereas particle size ranged from 1.41 µm to 17.66 µm. Microsponge formulations F3, F4 and F5 showed desired particle size hence studied for further evaluation. Formulation F3, F4 and F5 showed controlled release of 89.54%, 98.5% and 98.76% respectively up to 6 hr. F3 showed more controlled release at the end of 6 hr. The drug release from microsponges was best fitted to Higuchi’s diffusion kinetics for all microsponge formulations with non-Fickian diffusion mechanism. The formed microsponge particles have spherical porous structure.
 Conclusion: Study showed significance of Microsponge Delivery System for ophthalmic administration.

Microsponges: A Novel Strategy to Control the Delivery Rate of Active Agents with Reduced Skin Irritancy

Microsponges are particulate system which is composed by porous polymeric material. As compare to Conventional topical formulations, microsponge provide controlled release of the drug in the epidermis, it is to ensure that the drug is mainly localized and does not unduly entering the systemic circulation, it is a new area of research. The active ingredient needs to maximize the time to stay on the skin, while reducing transdermal penetration. Apart from this, there is a problem of unethical vehicles that can be viscous sticky deformation and skin irritation. One of the biggest challenges of now a days is to control irritability for a predetermined site of active agents in the human body. Microsponges delivery system is a unique technique for controlled release with low irritant involving many triggers of Mechanism for the release of drugs. The Microsponge Delivery system is a polymeric porous microspheres, which can trap a wide range of effective elements such as anti-fungus, anti-infected, anti- inflammatory agent, fragrance and essential agent. This review includes different techniques used to prepare microsponges, formulation consideration, safety consideration, drug release mechanism, and challenges with microsponge drug delivery system along with their advantages, disadvantages and applications. In the current review, we summarize the updated application and capacity of Microsponge as an effective drug-delivery system to reduce skin irritation.
 Keywords: Microsponges; quasi-emulsion solvent diffusion; Porous microspheres; Controlled release.

Microsponges: A Promising Novel Drug Delivery System

Microsponge is recent novel technique for control release and target specific drug delivery system. More and more developments in drug delivery systems are being integrated to optimize the efficacy and cost-effectiveness of the therapy. Microsponges are polymeric delivery system containing porous microspheres having a size range from 5 to 300µm. Microsponge Delivery System (MDS) is a unique technology for controlled drug delivery. This review article mainly deals with Microsponge drug delivery along with its method of preparation, characterization, advantages and release mechanism of MDS. Microsponges are characterized by particle size, entrapment efficacy, true density, % drug content and % yield, dissolution studies, Resiliency, compatibility studies and in-vitro studies. Wide range of applications is also preferred to develop drug with enhanced safety and efficacy.
 Keywords: Microsponge, Porous microspheres, Control release, Colon.

Studying the effect of variables on baclofen floating microsponge

The aim of the present work was to develop a microsponge delivery system of baclofen to control its release and thereby reducing dosing frequency and enhancing patient compliance. The microsponge was produced by oil in oil emulsion solvent diffusion method. The effects of drug/polymer ratio, stirring time and type of Eudragit polymer on the physical characteristics of microsponges were investigated. The prepared microsponges was characterized for production yield (PY), loading efficiency (LD), particle size, surface morphology, and in vitro drug release. The results showed that the microsponge formula with Eudragit RS100 had optimum physical properties with PY % equal to 97 %, and LD % equal to 81% and controlled drug release (75% of drug release in 8 hours) when compared with other formulas and pure BFN. Therefore, the non-‎aqueous emulsion solvent diffusion method is a promising method to produce baclofen microsponges.‎

A Review on Microsponge Delivery System

Microsponge is recent novel technique for control release and target specific drug delivery system. Microsponge technology has been introduced in pharmaceutical industry to provide the controlled release of active drug ingredient for the application into the skin in order to decrease systemic exposure and reduce local cutaneous reactions to active drugs. Microsponges comprises of microporous beads, typically 10-25 microns in diameter, loaded with active agent. The microsponge releases its active ingredient on a time mode, when applied to the skin, and also in response to other stimuli that are used mostly for topical and recently for oral administration. Microsponge technology has many favourable characteristics which make It all around suitable as drug delivery vehicle. Microsponge systems can suspend or entrap a wide variety of substances, and then be incorporated into a formulated product such as a gel, cream, liquid or powder. The outer surface is mostly porous, allowing the sustained flow of substances out of the sphere. Microsponge drug delivery system causes increased efficacy for the topically active agents with enhanced safety and product stability for a longer period of time with reduction in side effects. In addition their non-allergenic, non-irritating, non-mutagenic and nontoxic behaviour makes them the suitable dosage form. The present review emphasis Microsponge drug delivery system along with its release mechanism. Keywords: Novel drug delivery system, Microsponges, Microsponge drug delivery system, Quasi-emulsion solvent diffusion method.

MICROSPONGES AS A NEOTERIC CORNUCOPIA FOR DRUG DELIVERY SYSTEMS

Microsponges (MSPs) are at the forefront of the rapidly developing field of novel drug delivery systems which are gaining popularity due to their use for controlled release and targeted drug delivery. The microsponge delivery system (MDS) is a patented polymeric system consisting of porous microspheres typically 10-25 microns in diameter, loaded with an active agent. They are tiny sponge-like spherical particles that consist of a myriad of interconnecting voids within a non-collapsible structure with a large porous surface through which active ingredient is released in a controlled manner. Microsponge also hold a certification as one of the potential approaches for gastric retention where many oral dosage forms face several physiological restrictions due to non-uniform absorption pattern, inadequate medication release and shorter residence time in the stomach. This type of drug delivery system which is non-irritating, non-allergic, non-toxic, can suspend or entrap a wide variety of substances, and can then be incorporated into a formulated product such as gel, cream, liquid or powder that is why it is called as a “versatile drug delivery system”. It overcomes the drawbacks of other formulations such as frequency of dosing, drug reaction, incompatibility with environmental condition. These porous microspheres were exclusively designed for chronotherapeutic topical drug delivery but attempt to utilize them for oral, pulmonary and parenteral drug delivery were also made. The present review elaborates about the multifunctional microsponge technology including its preparation, characterization, evaluation methods along with recent research and future potential.

Studying the Effect of Variables on Acyclovir Microsponge

The aim of the present investigation was to develop a microsponge delivery system of acyclovir to control its release when applied topically thereby reducing dosing frequency and enhancement patient compliance. The microsponges were produced by the oil in oil emulsion solvent diffusion method. The effect of different formulation and process variables such as internal phase volume, polymer type, drug-polymer ratio, stirring speed and stirring duration on microsponge production yield, loading efficiency, particle size and in-vitro drug release was evaluated. The result showed that the microsponge F2 prepared from Eudrajet RS polymer had optimum physical properties regarding the loading efficiency of 99.71_+ 0.7% and production yield which was 85%. Also, F2 showed 66% drug release within 8 hours. Accordingly, the oil in oil emulsion solvent diffusion method is an effective technique to formulate microsponges with maximum production yield and loading efficiency for acyclovir.

INNOVATIVE AND NOVEL STRATEGY: MICROSPONGES FOR TOPICAL DRUG DELIVERY

Microsponge type of drug delivery is the latest technology which has been introduced in topical skin care, drug products to facilitate the controlled release of the active medicament into the skin in order to reduce systemic exposure and control local cutaneous reactions to active drugs. Microsponge can be loaded into a topical route of drug delivery system for the residue of dosage form of skin and thus controlled release drug delivery system is achieved and in return improving the patient compliance by providing target drug delivery system and prolonging dosage intervals. Microsponge is polymeric delivery systems composed of porous microspheres. They are tiny sponge-like spherical particles and posses large porous surface area. Furthermore, they may enhance stability, reduce side effects, improve patient compliance and modify drug release. Microsponges are the polymer-based microspheres system that has the capacity to entrap a wide variety of substances, and can then be incorporated into a different formulation.
 Keywords: Microsponge Delivery System, Quasi- emulsion solvent diffusion.

A Review on Novel Drug Delivery System: Microsponges

Recent research on idealizing drug delivery system which is progressing at a prodigious rate and aims at development of drug delivery system (DDS), with maximum therapeutic advantages of drug delivery, thus resulting in safe and effective management of disease. More and more developments in delivery systems are being integrated to optimize the efficacy and cost effectiveness of the therapy. New classes of pharmaceuticals, biopharmaceuticals are fueling the rapid evolution of drug delivery technology. Microsponge technology has been introduced in topical drug products to facilitate the controlled release of active drug into the skin in order to reduce systemic exposure and minimize local cutaneous reactions to active drugs. Microsponge consists of microporous beads loaded with active agent. When applied to the skin, the microsponge releases its active ingredient on a time mode and also in response to other stimuli (rubbing, temperature, pH etc.) that are used mostly for topical and recently for oral administration Microsponges are porous, polymeric microspheres that are mostly used for prolonged topical administration. Microsponges are designed to deliver a pharmaceutically active ingredient efficiently at minimum dose and also to enhance stability, reduce side effects, and modify drug release profiles. Microsponges are prepared by several methods utilizing emulsion system or by suspension polymerization in a liquid–liquid system. The most common emulsion system used is oil-in-water (o/w), with the microsponges being produced by the emulsion solvent diffusion (ESD) method. Microsponge delivery system (MDS) can provide increased efficacy for topically active agents with enhanced safety, extended product stability, enhanced formulation flexibility, reduced side effects and improved aesthetic properties in an efficient and novel manner. In addition these are non-irritating, non-mutagenic, non-allergenic, and nontoxic. The present review introduces microsponge technology in great detail.

Microsponges: An Overview

Microsponge and Nanosponge delivery System was originally developed for topical delivery of drugs can also be used for controlled oral delivery of drugs using water soluble and bioerodible polymers. Microsponge delivery system (MDS) can entrap wide range of drugs and then release them onto the skin over a time by difussion mechanism to the skin. It is a unique technology for the controlled release of topical agents and consists of nano or micro porous beads loaded with active agent and also use for oral delivery of drugs using bioerodible polymers.