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Microsponge drug delivery system as an innovation in Cosmetic world: A Review

Microsponge drug delivery system as an innovation in Cosmetic world: A Review

Based on the literature surveyed, it may be concluded that simple production, various innovative applications with a programmable release makes Microsponge drug delivery system unique, novel and versatile and extremely attractive in cosmetic world for delivery of drugs like anti-acne, anti- inflammatory, anti-fungal, anti-dandruffs, antipruritics, antifungal ,rubefacients etc. and also expands its application in oral ,biopharmaceutical drug delivery & tissue engineering. Thus Microsponge technology has got a lot of potential and is a very emerging field which is needed to be explored for patient compliance provides the improved efficiencies of various types of pharmacotherapies with novel product development therefore it is easy to say that it has potential to create new era in cosmetic world.

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MICROSPONGE DRUG DELIVERY SYSTEM: AN OVERVIEW

MICROSPONGE DRUG DELIVERY SYSTEM: AN OVERVIEW

Microsponges are porous microspheres that having myriad of interconnected size ranging voids of particle from 5-150 μm. Microsponge delivery systems (MDS) that can precisely control the release rates or target drugs to a specific body site have an enormous impact on the health care system. The microsponge drug delivery technology is widely applicable to the dermatological drug delivery products.MDS expands application in oral drug delivery, bone and tissue engineering, in detecting the diseases and in RNAi silencing .The area of drug delivery technology is being rapidly and becoming highly competitive day by day.The microsponges have the ability to entrap a wide range of active ingredients such as emollients, fragrances, essential oils, sunscreens and anti-infective, etc. are used as a topical carrier system.Microsponges are designed to deliver a pharmaceutical active ingredient efficiently at the minimum dose and also to enhance stability, reduce side effects, and modify drug release .

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A NEW ERA IN TOPICAL FORMULATIONS – MICROSPONGE DRUG DELIVERY SYSTEM

A NEW ERA IN TOPICAL FORMULATIONS – MICROSPONGE DRUG DELIVERY SYSTEM

Microsponge delivery systems are used to improve the safety, effectiveness and quality of topical prescription, over-the-counter and personal care products. Microsponges can be used in variety of applications. It is used mainly for topical and now a days for oral administration. It can be used as an excipient due to its high loading capacity and sustained release ability. It offers the manufacturer a range of alternatives to develop drug and cosmetic products. Microsponges are designed to deliver a pharmaceutical active ingredient efficiently at the minimum dose and they also enhance stability, reduce side effects and modify drug release. Over-the-counter products that incorporate microsponge drug delivery system include numerous moisturizers, specialized rejuvenated products, and sunscreens.

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DEVELOPMENT AND EVALUATION OF MICROSPONGE DRUG DELIVERY SYSTEM OF INDOMETHACIN

DEVELOPMENT AND EVALUATION OF MICROSPONGE DRUG DELIVERY SYSTEM OF INDOMETHACIN

In the present study controlled release formulation of Indomethacin microsponges were prepared by using Carbopol 940, PVA. Microsponges were prepared by Quasi emulsion solvent diffusion method by changing drug polymer ratio (1:0.5-1:4) and process was optimized. Microsponges were evaluated by micromeritic properties, drug content, encapsulation efficiency, and particle size. Characterization of Indomethacin microsponges were done by FT-IR spectroscopy,. In-vitro dissolution study indicated that the release of Indomethacin varied according to the concentration of matrix forming polymer, drug release mechanism was found to be super case II transport Therefore, Indomethacin microsponges prepared in thus study are promising as being more useful than conventional formulation intherapy.

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Designa and Evaluation of Microsponge Drug Delivery of Psoralen - Isolated from Psoralea Corylifolia

Designa and Evaluation of Microsponge Drug Delivery of Psoralen - Isolated from Psoralea Corylifolia

water which contained different concentration(0- 2 %) of Poly Vinyl Alcohol (PVA) as emulsifying agent. The mixture was stirred for 6 hours, at 25 °C. The formed Microsponge were filtered and washed with distilled water before being tray-dried at room temperature. For the evaluation of the effect of drug: polymer ratio on the physical characteristics of Microsponge, different weight ratios of drug to Ethyl Cellulose (EC) (1:0.5, 1:1, 1:1.5) were employed. In all these formulations, the total amount of drug was kept constant. To optimize the particle size, size distribution and the drug release from the Microsponge, an individual formulation was selected and a series of the Microsponges were prepared using different stirring rates. However, for optimizing the preparation method and the characteristics of the prepared Microsponge were evaluated 10 .

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MICROSPONGE DRUG DELIVERY STSTEM FOR TOPICAL DELIVERY-A REVIEW

MICROSPONGE DRUG DELIVERY STSTEM FOR TOPICAL DELIVERY-A REVIEW

period of time. Conventional dermatological and personal care products typically provide active ingredients in relatively high concentrations but with a short duration of action. This may lead to a cycle of short-term overmedication followed by long-term under medication. Rashes or more serious side effects can occur when active ingredients penetrate the skin. In contrast, microsponge technology allows an even and sustained rate of release, reducing irritation while maintaining efficacy. Microsponges are capable to absorb skin secretions consequently, reducing oiliness and shine from the skin. Microsponge particles are extremely small, inert, indestructible spheres that do not pass through the skin. To a certain extent, they accumulate in the tiny nooks and crannies of skin and slowly release the entrapped drug, as the skin needs it. The microsponge system can also avoid unnecessary accumulation of ingredients within the epidermis and the dermis. Potentially, they can reduce considerably the irritation of effective drugs without reducing their efficacy. Resembling a true sponge, each microsphere consists of an innumerable of interconnecting voids within a non-collapsible structure with a large porous surface. When it is applied to the skin, the drug release can be controlled through diffusion. This controlled release of active ingredient onto skin over time is an enormously important tool for providing the benefits of enhanced product efficacy, tolerability, mildness and lessen the irritation usually associated with powerful therapeutic agents like retinoids or benzoyl peroxide etc. and extended wear to a wide range of skin therapies. This system has been utilized for the improvement of performance of topically applied drug. MDS technology is now being presently used in cosmetics, over-the-counter (OTC) skin care, sunscreens and prescription products very popularly.

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NOVEL APPROACH: MICROSPONGE DRUG DELIVERY SYSTEM

NOVEL APPROACH: MICROSPONGE DRUG DELIVERY SYSTEM

In recent years, there has been considerable emphasis given to the development of microsponge base novel drug delivery systems, in order to modify and control the release behavior of the drugs. By incorporation into a carrier system, it is possible to alter the therapeutic index and duration of the activity of drugs. Microsponges are porous microspheres, biologically inert particles that are made of synthetic polymers and the particles serve to protect the entrapped drug compound from physical and environmental degradation. Their high degree of cross-linking results in particles that are insoluble, inert and sufficient strength to stand up to the high shear commonly used in manufacturing of creams, lotions, and powders. Their characteristic feature is the capacity to adsorb or “load” a high degree of active materials into the particle and on to its surface and it is delivered to skin via controlled diffusion.

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 FORMULATION AND EVALUATION OF MICROSPONGE DRUG DELIVERY SYSTEM USING INDOMETHACIN

 FORMULATION AND EVALUATION OF MICROSPONGE DRUG DELIVERY SYSTEM USING INDOMETHACIN

In the present study controlled release formulation of Indomethacin microsponges were prepared by using Eudragit RS 100, pH independent release retardant polymer and PVA, stabilizer or emulsifier. Microsponges were prepared by Quasi emulsion solvent diffusion method by changing drug polymer ratio (3:1, 4:1, 5:1) and process was optimized. Microsponges were evaluated by micromeritic properties, drug content, encapsulation efficiency, and particle size. Characterization of Indomethacin microsponges were done by FT-IR spectroscopy, Differential scanning calorimetry, X-ray diffractometry and Scanning electron microscopy for pure drug, polymer, physical mixture and formulation. In-vitro dissolution study indicated that the release of Indomethacin varied according to the concentration of matrix forming polymer. Therefore, Indomethacin microsponges prepared in thus study are promising as being more useful than conventional formulation in therapy.

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THE MICROSPONGE DRUG DELIVERY SYSTEM: AN OVERVIEW

THE MICROSPONGE DRUG DELIVERY SYSTEM: AN OVERVIEW

diffusion of the stratum corneum. and liposomes. Microcapsules cannot usually control the release rate of actives. Once the wall is ruptured the actives contained with in microcapsules will be released. Liposomes suffer from lower payload, difficult formulation, limited chemical stability and microbial instability. While microsponge system in contrast to the above systems are stable over range of pH 1 to 11, temperature up to 130 o C; compatible with most vehicles and ingredients; self sterilizing as average pore size is 0.25µm where bacteria cannot penetrate; higher payload (50 to 60%), still free flowing and can be cost effective. Most liquid or soluble ingredients can be entrapped in the particles. Actives that can be entrapped in microsponges must meet following requirements,

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A REVIEW ON MICROSPONGE DRUG DELIVERY SYSTEM

A REVIEW ON MICROSPONGE DRUG DELIVERY SYSTEM

Free-flowing powders with fine aesthetic attributes are possible to obtain by controlling the size of particles during polymerization. Particle size analysis of loaded and unloaded microsponges can be performed by laser light diffractometry or any other suitable method. The values (d50) can be expressed for all formulations as mean size range. Cumulative percentage drug release from microsponges of different particle size will be plotted against time to study effect of particle size on drug release. Particle larger than 30 μm can impart gritty feeling and hence particles of sizes between10 and 25 μm are preferred to use in final topical formulation. The most widely used procedures to visualize microparticles are conventional light microscopy (LM) and scanning electron microscopy (SEM). Both can be used to determine the shape and outer structure of microparticles. LM provides a control over coating parameters in case of double walled microparticles. Conflocal fluorescence microscopy is used for the structure characterization of multiple walled microparticles. Laser light scattering and multi size coulter counter other than instrumental methods, which can be used for the characterization of size, shape and morphology of the microparticles (microsponges). Morphology and surface topography of microsponges: 28

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RECENT TRENDS AND ADVANCES IN MICROSPONGE DRUG DELIVERY

RECENT TRENDS AND ADVANCES IN MICROSPONGE DRUG DELIVERY

Microsponges are microscopic spheres capable of absorbing skin secretions, therefore reducing oiliness and shine from the skin. Spherical particles composed of clusters of even tinier spheres are capable of holding four times their weight in skin secretions. Microsponge particles are very small, inert, indestructible spheres that do not pass through the skin. Rather, they collect in the tiny nooks and crannies of the skin and slowly release the entrapped drug, as the skin needs it. The microsponge system can prevent excessive accumulation of ingredients within the epidermis and the dermis. Potentially, the microsponge system can significantly reduce the irritation of effective drugs without reducing their effectiveness. The empty spheres are then washed away with the next cleansing. The microsponge delivery system (MDS) fulfills these requirements and has resulted in a new generation of very well-tolerated and highly efficacious, novel products. These products are typically presented to the consumer in conventional forms like creams, gels or lotions and they enclose a relatively high concentration of active ingredients. [5]

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To control the delivery rate of active agents to a predetermined site in the human body has been one of the biggest challenges faced by Pharmaceutical scientists. Several predictable and reliable systems have been developed for systemic delivery of drugs under the heading of transdermal delivery system (TDS) using the skin as portal of entry. It has improved the efficacy and safety of many drugs that may be better administered through skin. But TDS is not practicable for delivery of materials whose final target is skin itself. Controlled release of drugs onto the epidermis with assurance that the drug remains primarily localized and does not enter the systemic circulation in significant amounts is a challenging area of research. Microsponges consist of non-collapsible structures with porous surface through which active ingredients are released in controlled manner. Depending upon the size, the total pore length may range up to 10 ft. and pore volume up to 1 ml/g. When applied to the skin, the microsponge drug delivery system (MDS) releases its active ingredient on a time mode and also in response to other stimuli such as rubbing, temperature, and pH Microsponges have the capacity to adsorb or load a high degree of active materials into the particle or onto its surface. Its large capacity for entrapment of actives up to 3 times its weight differentiates microsponges from other types of dermatological delivery systems [4] .

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A Review on Microsponge as Emerging Drug Delivery System

A Review on Microsponge as Emerging Drug Delivery System

A microsponge delivery system will entrap a wide variety of active pharmaceutical ingredients and then release them onto the skin over a time and additionally in response to different stimuli including rubbing, moisture, pH, friction, or ambient skin temperature. It can also be used for controlled oral delivery of drugs using water-soluble, water-insoluble and bio-erodible polymers. The primary aim of any drug delivery system is to provide a therapeutic quantity of drug to the suitable site in the body, to punctually achieve and retain the desired drug concentration. The elemental application of the microsponge technology arises as of the difficulty experienced with predictable formulations in release active ingredients over an extended period of time. Microsponges also enhanced bioavailability of active ingredient and increase the solubility of the poorly water-soluble drug. Microsponge is providing some advantages like controlled release and extended release of active agents by using different polymers. They become a reduced irritation and improved thermal, physical, and chemical stability of the product. The pre sent review describes microsponge technology including its method of preparation, characterization, programmable parameters and release mechanism of microsponge drug delivery system. Microsponges can be designed to programmable release of drug by using different triggers li ke solubility triggered systems, pressure triggered systems, temperature triggered systems and pH triggered systems.

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FORMULATION AND EVALUATION OF MICROSPONGE BASED DRUG DELIVERY SYSTEM OF LEVONORGESTREL

FORMULATION AND EVALUATION OF MICROSPONGE BASED DRUG DELIVERY SYSTEM OF LEVONORGESTREL

Recently the drug delivery systems use to treat contraception are pills ,vaginal ring , the Patch ,Shot/Injection ,Implantable Rods ,Intrauterine Devices ,Sterilization Implant , Surgical Sterilization were still acceptable, such dosage form are no longer sufficient to overcome the various contraception methods. Which are conventionally use from many years, which also have number of limitations out of these limitation the most important is residence time of drug at the site of application. To overcome these limitations there is need to find some innovative featured microsponge drug delivery in the contraception method.

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DEVELOPMENT & CHARACTERIZATION OF EMTRICITABINE LOADED MICROSPONGES

DEVELOPMENT & CHARACTERIZATION OF EMTRICITABINE LOADED MICROSPONGES

The rationale of this study was to develop, optimize and characterize microsponge drug delivery system for antiviral delivery. Antiviral compound, emtricitabine was selected as a model drug. The microsponges were prepared by emulsion solvent diffusion method and optimize for various formulation parameters. The formulation (F1- F6) were characterized in terms of particle size, drug entrapment efficiency (DEE), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and zeta potential measurement. The drug release from the microsponge loaded gel was studied by modified Franz diffusion cell. F2 released 50.85% of drug at 8 hours. Diffusion exponent (n) value of F2 formulation was found to be 0.912 suggesting that the Ficks law of diffusion was not followed. The F2 formulation followed Zero order kinetics in its in vitro drug release. This study provides future insights for developing delayed release microsponge based gels for treatment of skin infections and disorders. K eywords: Microsponge, Solvent diffusion method, Emtricitabine, Scanning electron microscopy, Differential scanning calorimetry.

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FORMULATION AND IN-VITRO EVALUATION OF ETODOLAC ENTRAPPED IN MICROSPONGE BASED DRUG DELIVERY SYSTEM

FORMULATION AND IN-VITRO EVALUATION OF ETODOLAC ENTRAPPED IN MICROSPONGE BASED DRUG DELIVERY SYSTEM

Drug delivery systems (DDS) can control the release rate of drug and targets drug moiety to a specific site in the body and has huge impact on the human health care system. Microsponge drug delivery system is an exclusive technology that has been used for the controlled release of topically active agents. It is a highly cross-linked, porous, polymeric system usually 10-25 microns in diameter which can entrap wide range of active substances and releases them over a period of time and in response to trigger. When it is applied, microsponges releases the active substance based on its time mode and in response to other stimuli like temperature and pH. It has been used in prescription products, over the counter skin care products, cosmetics and sunscreens. It offers entrapment of ingredients and increased stability, elegance, flexibility in formulation and reduced side effects. These are stable in the pH of 1 to 11 and temperature up to 130 0 C. They are self sterilizing in

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FORMULATION DEVELOPMENT OF MICROSPONGE BASED DELAYED RELEASE DOSAGE FORM OF LANSOPRAZOLE

FORMULATION DEVELOPMENT OF MICROSPONGE BASED DELAYED RELEASE DOSAGE FORM OF LANSOPRAZOLE

This developed dosage form may be a cost effective as the numerous coatings involved in the process is reduced and prepared by simple diffusion of drug in polymer by means of microsponge structure. Production yield and Loading efficiency has encouraged for further development. Developed dosage form behaves similar to the marketed formulation in OGD and USP recommended dissolution media. It is recommended to have in-vitro in-vivo correlation using convolution and deconvolution technique for the optimized formulations.

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Fabrication and characterization of sertaconazole nitrate microsponge as a topical drug delivery system

Fabrication and characterization of sertaconazole nitrate microsponge as a topical drug delivery system

Pore related parameters like total specific surface area, % porosity, average pore diameters, total cumulative value, bulk and apparent density were determined by using mercury intrusion porosimetry. Pressure was gradually applied in a cell in which a small sample of the microsponge was placed under mercury. With increasing pressure more mercury was forced to enter even smaller pores of the microsponge, resulting in an apparent reduction in the volume of mercury in the cell that was measured [5,14] .

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Formulation, development and evaluation of Microsponge loaded Topical Gel of Nystatin

Formulation, development and evaluation of Microsponge loaded Topical Gel of Nystatin

All the microsponge formulations were subjected to drug content estimation, the low SD values indicates drug content was uniform and reproducible in all the formulations. All the microsponge formulations were subjected for loading efficiency and the results were found to be reproducible.The IR spectral analysis suggested that there was no interaction between the drug and formulation additive. The drug exists in original form and available for the biological action.From dissolution studies it was found out that microsponge batch no. F3 gave maximum drug release.

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POLYSACCHARIDE MICROSPONGE BASED MATRIX TABLET FOR COLON TARGETING OF KETOPROFEN: IN VITRO AND IN VIVO EVIDENCE

POLYSACCHARIDE MICROSPONGE BASED MATRIX TABLET FOR COLON TARGETING OF KETOPROFEN: IN VITRO AND IN VIVO EVIDENCE

ABSTRACT: The present research was aimed to formulate erosion based matrix tablets of ketoprofen micro-sponges for spatial-colon targeting. For the optimization, the effects of independent variables like solvent volume and concentration of chitosan were studied on the mean particle size, percent entrapment efficiency (% EE) and in vitro drug release. Scanning Electron Microscopy (SEM) image of the micro-sponge formulation revealed that the surface of the micro-sponge was nearly spherical and porous. Optimized micro-sponge formulation was further formulated into erosion based matrix tablet and evaluated for quality control parameters. In vitro release studies revealed that both the micro- sponge formulation and micro-sponge matrix tablet (MST) had restricted the drug release of ketoprofen in gastric pH followed by gradual release up to 12 hr. The release kinetics data, after fitting into various models revealed that both formulations were best fitted to zero order, indicating controlled release property. The pharmacokinetic evaluation of colon targeted MST in rats revealed the presence of drug in plasma after lag time of 4 hr, t max of 4 ± 0.23, AUC (0-12hr) of 33.10 ± 3.68 with t 1/2 3.85

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