Design and evaluation of colon specific drug delivery system containing flurbiprofen microsponges

Orlu, Mine; Cevher, Erdal; Araman, Ahmet

doi:10.1016/j.ijpharm.2006.03.025

Cited by 167 publications

(119 citation statements)

References 66 publications

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“…Sodium chloride as a porogen is inert in terms of the evolution of gas and its high aqueous solubility would facilitate its easy extraction in the outer aqueous phase during the microsponge formation (Orlu, Cevher, Araman, 2006). Therefore, using sodium chloride as porogen, nine formulations (F1-F9) were fabricated and characterized.…”

Section: Methods Development For the Fabrication Of Microspongesmentioning

confidence: 99%

“…The reasons for fabricating microsponge was due to the fact that, drug carrier systems less than 200 μm can efficiently be taken up by the macrophages present in colon tissue, thus exhibit effective localized drug action at the desired site. Apart from being site specific, retention of drug or its carrier system on the colonic surface is yet another important consideration that guided the selection of microsponges as the drug carrier system in the research work (Orlu, Cevher, Araman, 2006). They can also increase the lag time for absorption of drug as these get entrapped on the surface of the colon and thus have the potential for being developed as a colon-targeted drug delivery system.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Enteric coated HPMC capsules plugged with 5-FU loaded microsponges: a potential approach for treatment of colon cancer

Gupta¹,

Tiwari²,

Tiwari³

et al. 2015

Braz. J. Pharm. Sci.

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The work was aimed at developing novel enteric coated HPMC capsules (ECHC) plugged with 5 Florouracil (5-FU) loaded Microsponges in combination with calcium pectinate beads. Modified quasiemulsion solvent diffusion method was used to formulate microsponges based on 3 2 factorial design and the effects of independent variables (volume of organic solvent and Eudragit RS100 content) on the dependent variables (Particle size, %EE & % CDR) were determined. The optimized microsponges (F4) were characterized by SEM, PXRD, TGA and were plugged along with calcium pectinate beads in HPMC capsules and the HPMC capsules were further coated with enteric polymer Eudragit L 100 (Ed-L100) and/ or Eudrgit S 100 (Ed-S 100) in different proportions. In vitro release study of ECHC was performed in various release media sequentially SGF for 2 h, followed by SIF for the next 6 h and then in SCF (in the presence and absence of pectinase enzyme for further 16 h). Drug release was retarded on coating with EdS-100 in comparison to blend of EdS-100: EdL-100 coating. The percentage of 5-FU released at the end of 24 h from ECHC 3 was 97.83 ± 0.12% in the presence of pectinase whereas in control study it was 40.08 ± 0.02% drug. The optimized formulation was subjected to in vivo Roentgenographic studies in New Zealand white rabbits to analyze the in vivo behavior of the developed colon targeted capsules. Pharmacokinetic studies in New Zealand white rabbits were conducted to determine the extent of systemic exposure provided by the developed formulation in comparison to 5-FU aqueous solutions. Thus, enteric coated HPMC capsules plugged with 5-FU loaded microsponges and calcium pectinate beads proved to be promising dosage form for colon targeted drug delivery to treat colorectal cancer. O trabalho teve como objetivo o desenvolvimento de novas cápsulas com revestimento entérico HPMC (ECHC) conectadas com microesponjas carregadas com fluoruracila (5-FU) em combinação com grânuos de pectinato de cálcio. O método de difusão de solvente modificado quasi-emulsão foi usado para formular microesponjas com base no planejamento fatorial 3 2 e determinaram-se os efeitos das variáveis independentes (volume de solvente orgânico e conteúdo Eudragit RS100) sobre as variáveis dependentes (tamanho de partícula, EE% e % CDR). As microesponjas otimizadas (F4) foram caracterizadas por SEM, PXRD, TGA e ligadas aos grânulos de pectinato de cálcio em cápsulas de HPMC e estas foram, ainda, revestidas com polímero entérico Eudragit L 100 (Ed-L100) e/ou Eudrgit S 100 (Ed S 100) em diferentes proporções. No estudo de liberação in vitro de ECHC foi realizada em vários meios de liberação sequencial SGF durante 2 h, seguido de SIF para as próximas 6 h, e, em seguida, em SCF (na presença e na ausência de enzima pectinase por mais 16 h). A liberação do fármaco foi retardada em revestimento com a EDS-100, em comparação com mistura de EDS-100: EDL-100, de revestimento. O percentual de 5-FU liberado de ECHC 3 ao final de 24 h foi 97,83 ± 0,12% em presença de pectinase, enquanto...

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Section: Methods Development For the Fabrication Of Microspongesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Enteric coated HPMC capsules plugged with 5-FU loaded microsponges: a potential approach for treatment of colon cancer

Gupta¹,

Tiwari²,

Tiwari³

et al. 2015

Braz. J. Pharm. Sci.

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“…In 2013, the group of Liu et al 8 firstly put forward a new skin-target drug delivery system containing Paeonol which was extracted from the root of Paeonia suffruticosa, a kind of traditional Chinese medicine. The preparation of Paeonol microsponges is the same as flurbiprofen microsponges, 15 using the quasi-emulsion solvent-diffusion method ( Figure 6). …”

Section: Figure 2 Preparation Of Bpo Microsponges By Quasi-emulsion Smentioning

confidence: 99%

“…3 As a new drug carrier of TDDS, Microsponges are mostly used for topical [4][5][6][7][8][9][10] and oral administration. [11][12][13][14][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.…”

Section: Introductionmentioning

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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“…The surface can be varied from 20 to 500 m 2 /gm and the pore volume range from 0.1 to 0.3 cc/gm [2,3]. Microsponges, which are porous and polymeric microspheres, were mainly used for topical use [3,4], but recently the oral administration was also proposed [5]. Microsponges are designed to deliver a pharmaceutically active ingredient efficiently at the minimum dose and also to enhance stability, reduce side effects and modify drug release [3].…”

Section: Introductionmentioning

confidence: 99%

Evaluation of carvedilol-loaded microsponges with nanometric pores using response surface methodology

Saini

Singh

Verma

2012

Journal of Experimental Nanoscience

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This study demonstrates the use of factorial design for the preparation of microsponges of carvedilol with nanometric pores using the response surface methodology and to establish the functional relationships between two operating variables of Eudragit RS100 and sucrose. The response variables selected for this study were percent drug entrapment (Y1), time taken to release 35% of drug (Y2), percent drug release after 24 h (Y3), percent dissolution efficiency (DE) (Y4) and the angle of repose (Y5). The overall calculated desirability was found to be 0.8065 for the optimised formulation OF1. The response surface analysis of the desirability function with the independent levels indicated that the overall desirability increases with high levels of Eudragit RS100 and sucrose content. The optimum robust formulation (OF1) contains high levels of Eudragit RS100 (400.0 mg) and sucrose (350.21 mg), satisfying the predetermined constraints and goals of all the selected response variables. The scanning electron microscopy of OF1 indicated the spherical shape of microsponges with numerous pores on the surface. The atomic force microscopic study suggested the presence of nanometric pores on the surface of microsponges which may facilitate the release of the drug. Compatibility studies using the Fourier transform infrared spectroscopy, X-ray diffraction and differential scanning calorimeter indicated the absence of any incompatibility between carvedilol and excipients used to prepare microsponges.

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Design and evaluation of colon specific drug delivery system containing flurbiprofen microsponges

Cited by 167 publications

References 66 publications

Enteric coated HPMC capsules plugged with 5-FU loaded microsponges: a potential approach for treatment of colon cancer

Enteric coated HPMC capsules plugged with 5-FU loaded microsponges: a potential approach for treatment of colon cancer

Toward Application of Microsponges in Transdermal Drug Delivery System

Evaluation of carvedilol-loaded microsponges with nanometric pores using response surface methodology

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