Preparation and in vitro evaluation of modified release ketoprofen microsponges

Çomoğlu, Tansel; Gönül, Nurşin; Baykara, Tamer

doi:10.1016/s0014-827x(02)00007-1

Cited by 82 publications

(42 citation statements)

References 17 publications

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“…SEM of a fractured microsponge particle can also be taken to illustrate its ultrastructure. [23,24] 3. Determination of loading efficiency and production yield: -The loading efficiency (%) of the microsponges can be calculated according to the following equation Loading efficiency = Actual Drug Content in Microsponges X 100…”

Section: Percentage Yieldmentioning

confidence: 99%

Microsponges: Topical Preparation and Its Applications

Sumbria¹

2017

WJPPS

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Microsponges are polymeric delivery systems composed of porous microspheres. They are tiny sponge-like spherical particles with a large porous surface. Moreover, they may enhance stability, reduce side effects and modify drug release favorably. Microsponge technology has many favorable characteristics, which make it a versatile drug delivery vehicle. Microsponge Systems are based on microscopic, polymer-based microspheres that can suspend or entrap a wide variety of substances, and can then be incorporated into a formulated product such as a gel, cream, liquid or powder. The outer surface is typically porous, allowing a sustained flow of substances out of the sphere.Microsponges are porous, polymeric microspheres that are used mostly for topical use and have recently been used for oral administration. More and more developments in delivery systems are being integrated to optimize the efficacy and cost-effectiveness of the therapy.Microsponge technology offers entrapment of ingredients and is believed to contribute towards reduced side effects, improved stability, increased elegance, and enhanced formulation flexibility. In addition, numerous studies have confirmed that microsponge systems are non-irritating, nonmutagenic, non-allergenic, and non-toxic. Microsponges are being used currently in cosmetics, over-the-counter (OTC) skin care, sunscreens and prescription products. One of the best feature of microsponge is it is self-sterilizing. This review is based on method of preparation and applications of microsponges.

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Section: Percentage Yieldmentioning

confidence: 99%

Microsponges: Topical Preparation and Its Applications

Sumbria¹

2017

WJPPS

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“…This could lead to a longer diffusional path, and consequently reduced LGO release rates. 38,39 Moreover, the decrease in the percentage LGO released after 6 hours with increasing the stirring rate might be explained on the basis of decreased porosity of the nanosponges formed at higher stirring rates, as evidenced by the scanning electron microscopy photographs (representative samples shown in Figure 2). According to Mateovic et al 40 larger microspheres exhibit higher porosity and higher release rates.…”

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confidence: 99%

Design and formulation of a topical hydrogel integrating lemongrass-loaded nanosponges with an enhanced antifungal effect: in vitro/in vivo evaluation

Aldawsari¹,

Badr-Eldin²,

Labib³

et al. 2015

IJN

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Lemongrass oil (LGO) is a volatile oil extracted from the leaves of Cymbopogon citratus that has become one of the most important natural oils in the pharmaceutical industry because of its diverse pharmacologic and clinical effects. However, LGO suffers from low aqueous solubility, which could lead to a reduced effect. Moreover, the instability of its major active constituent, citral, could lead to volatilization, reaction with other formulation ingredients, and consequently, skin irritation. To surmount these problems, this research aims to formulate lemongrass-loaded ethyl cellulose nanosponges with a topical hydrogel with an enhanced antifungal effect and decreased irritation. The minimal inhibitory concentration and minimal fungicidal concentration of LGO against Candida albicans strain ATC 100231, determined using the broth macrodilution method, were found to be 2 and 8 μL/mL, respectively. The emulsion solvent evaporation technique was used for the preparation of the nanosponges. The nanosponge dispersions were then integrated into carbopol hydrogels (0.4%). Nine formulations were prepared based on a 3 2 full factorial design employing the ethyl cellulose:polyvinyl alcohol ratio and stirring rate as independent variables. The prepared formulations were evaluated for particle size, citral content, and in vitro release. Results revealed that all the nanosponge dispersions were nanosized, with satisfactory citral content and sustained release profiles. Statistical analysis revealed that both ethyl cellulose:polyvinyl alcohol ratio and stirring rate have significant effects on particle size and percentage released after 6 hours; however, the effect of the stirring rate was more prominent on both responses. The selected hydrogel formulation, F9, was subjected to surface morphological investigations, using scanning and transmission electron microscopy, where results showed that the nanosponges possess a spherical uniform shape with a spongy structure, the integrity of which was not affected by integration into the hydrogel. Furthermore, the selected formulation, F9, was tested for skin irritation and antifungal activity against C. albicans , where results confirmed the nonirritancy and the effective antifungal activity of the prepared hydrogel.

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“…For example, as early as1989, Kawashima 17 had prepared the ibuprofen microsponges by using quasi-emulsion solvent diffusion method, and since then, this kind of method for preparation of microsponge was commonly used. [18][19][20][21] And subsequently, the advantages of microsponges were found and revealed by researches gradually.…”

Section: Initial Discoveriesmentioning

confidence: 99%

Toward Application of Microsponges in Transdermal Drug Delivery System

Hong¹,

Chen²,

Xiang³

et al. 2015

MOJBB

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Abbreviations: TDDS, transdermal drug delivery system; FDA, food and drug administration; EC, ethyl cellulose; BPO, benzoyl peroxide; SEM, scanning electron microscopy; AUC, area under the curve; EE, entrapment efficiency; DSC, differential scanning calorimetry; MED, minimal erythemal dose; SPF, sun protection factor IntroductionCompared with drug dosage forms for oral and parenteral administration, Transdermal drug delivery system (TDDS) can minimize and avoid some restrictions relating to dosage forms effectively. Due to the conventional delivery systems suffering from certain restrictions like Peak and Valley phenomenon i.e., they show fluctuations in plasma drug concentration and cannot render sustained effect.1 However, the TDDS can meet the requirement to keep relatively stable plasma drug concentration and prolong delivery of drug, in a steady-state profile and minimizes the peak-associated side effects, which thus ensures the level of the drug is effective for treatment on the minimal therapeutic concentration. In general, Transdermal drug delivery system, as a controlled drug delivery system, is exceedingly humanized, commodious and prolong the period of time of release of drug, if need arises (e.g. systemic toxicity) with less pain sensation while administrating drug candidates. Additionally, TDDS permits the permeation of drugs across the skin and into the systemic circulation which avoids the hepatic first-pass effect observed in the course of oral administration and inconvenience of frequent parenteral administration. As a new drug carrier of TDDS, Microsponges are mostly used for topical 4-10 and oral administration. 11-15 For other topical delivery systems, the traditional delivery systems are required of frequent dosing to keep relatively stable local concentrations of effective constituent for therapeutic effectiveness because of low effectiveness.Thus to avoid this defect it is indispensable to design a new drug delivery system to prolong the residual time of drug in the epidermis or the dermis, while reduce its penetration into the body. For this reason, as a porous polymeric microsphere, Microsponges can fulfill such aims uniquely.4 Microsponges are porous, polymeric microspheres (Figure 1) which are invariably used for topical delivery system; 4-5,7-10 its inside are full of lacunas and its particle size is 5~300μm in diameter. AbstractTransdermal drug delivery system (TDDS) is a dosage form designed to deliver drug through skin by topical route of administration to the systemic circulation or for local treatment. As a new type of dosage form, TDDS has a number of special merits, but inevitably at the same time it possess some distinct disadvantages, such as low permeability and the drug mostly enter the systemic vascular. Microsponges are a kind of micro-sized and polyporous particles which can entrap effective constituents, and are biologically safe. And Microsponges also exhibit distinctive advantage at the aspect of drug release. The TDDS can enhance drug stability, decrease side effec...

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Preparation and in vitro evaluation of modified release ketoprofen microsponges

Cited by 82 publications

References 17 publications

Microsponges: Topical Preparation and Its Applications

Microsponges: Topical Preparation and Its Applications

Design and formulation of a topical hydrogel integrating lemongrass-loaded nanosponges with an enhanced antifungal effect: in vitro/in vivo evaluation

Toward Application of Microsponges in Transdermal Drug Delivery System

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Preparation and in vitro evaluation of modified release ketoprofen microsponges

Cited by 82 publications

References 17 publications

Microsponges: Topical Preparation and Its Applications

Microsponges: Topical Preparation and Its Applications

Design and formulation of a topical hydrogel integrating lemongrass-loaded nanosponges with an enhanced antifungal effect: in vitro/in&nbsp;vivo&nbsp;evaluation

Toward Application of Microsponges in Transdermal Drug Delivery System

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Design and formulation of a topical hydrogel integrating lemongrass-loaded nanosponges with an enhanced antifungal effect: in vitro/in vivo evaluation