Development and In Vitro Evaluation of Pantoprazole-Loaded Microspheres

Çomoğlu, Tansel; Gönül, Nurşin; Doğan, Aydın; Başcı, Nursabah E.

doi:10.1080/10717540802006864

Cited by 27 publications

(14 citation statements)

References 25 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Comoglu et al (30) reported that the encapsulation efficiency of microspheres is affected by drug/polymer ratio. When the amount of the polymer is decreased, there is no sufficient polymer in the media to produce microspheres for the entire drug.…”

Section: Microspheres Prepared With Varying Drug To Es100 Ratiomentioning

confidence: 99%

Influence of Some Formulation Variables on the Optimization of pH-dependent, Colon-targeted, Sustained-release Mesalamine Microspheres

El-Bary¹,

Aboelwafa²,

Sharabi³

2011

AAPS PharmSciTech

View full text Add to dashboard Cite

Abstract. The aim of this work was to understand the influence of different formulation variables on the optimization of pH-dependent, colon-targeted, sustained-release mesalamine microspheres prepared by O/O emulsion solvent evaporation method, employing pH-dependent Eudragit S and hydrophobic pHindependent ethylcellulose polymers. Formulation variables studied included concentration of Eudragit S in the internal phase and the ratios between; internal to external phase, drug to Eudragit S and Eudragit S to ethylcellulose to mesalamine. Prepared microspheres were evaluated by carrying out in vitro release studies and determination of particle size, production yield, and encapsulation efficiency. In addition, morphology of microspheres was examined using optical and scanning electron microscopy. Emulsion solvent evaporation method was found to be sensitive to the studied formulation variables. Particle size and encapsulation efficiency increased by increasing Eudragit S concentration in the internal phase, ratio of internal to external phase, and ratio of Eudragit S to the drug. Employing Eudragit S alone in preparation of the microspheres is only successful in forming acid-resistant microspheres with pulsatile release pattern at high pH. Eudragit S and ethylcellulose blend microspheres were able to control release under acidic condition and to extend drug release at high pH. The stability studies carried out at 40°C/75% RH for 6 months proved the stability of the optimized formulation. From the results of this investigation, microencapsulation of mesalamine in microspheres using blend of Eudragit S and ethylcellulose could constitute a promising approach for site-specific and controlled delivery of drug in colon.

show abstract

Section: Microspheres Prepared With Varying Drug To Es100 Ratiomentioning

confidence: 99%

Influence of Some Formulation Variables on the Optimization of pH-dependent, Colon-targeted, Sustained-release Mesalamine Microspheres

El-Bary¹,

Aboelwafa²,

Sharabi³

2011

AAPS PharmSciTech

View full text Add to dashboard Cite

show abstract

“…Gelatin (Figure 3b) and HPMC (Figure 3c) gave no sharp peaks. The intrinsic peak in the drug appeared with reduced intensity in a physical mixture (Figure 3d), indicating that the drug could not interact with other carriers (Castelli et al, 2001;Comoglu et al, 2008). However, no sharp intrinsic peak appeared in pure valsartan was observed in microcapsule (Figure 3e), suggesting that drug was present as an amorphous state (Li et al, 2008).…”

Section: Resultsmentioning

confidence: 84%

“…About 5 mg of samples were placed in sealed aluminum pans, and DSC analyses were carried out under nitrogen flow of 20 ml/min at a heating rate of 10°C/min from 40-200°C (Castelli et al, 2001;Comoglu et al, 2008). Furthermore, these materials were assessed by X-ray powder diffraction (D/MAX-2500, RIGAKU, Japan) conducted at room temperature using Ni-filtered Cutarget at 40 mA and 40 kV in the region of 10° ≤ 2θ ≤ 50° with an angular increment of 0.02° per second (Venkateswarlu & Manjunath, 2004).…”

Section: Thermal Characteristics and Crystallinitymentioning

confidence: 99%

Development of valsartan-loaded gelatin microcapsule without crystal change using hydroxypropylmethylcellulose as a stabilizer

Li¹,

Yan²,

Oh³

et al. 2010

Drug Delivery

View full text Add to dashboard Cite

To develop a valsartan-loaded gelatin microcapsule using hydroxypropylmethylcellulose (HPMC) as a stabilizer, which could improve the physical stability and bioavailability of valsartan, the gelatin microcapsules were prepared with various ratios of gelatin and HPMC using a spray-drying technique. Their solubility, dissolution, thermal characteristics, crystallinity, and physical stability were investigated. The bioavailability of drug in valsartan-loaded microcapsule was then evaluated compared to drug powder and commercial product in rats. The microcapsule with gelatin and/or HPMC enhanced the solubility and dissolution of drug compared to valsartan powder. Among the formulations tested, the valsartan-loaded gelatin microcapsule at the weight ratio of valsartan/gelatin/HPMC of 1/2/1 gave excellent drug solubility of approximately 2 microg/ml and dissolution of 70% at 1 h. The crystal state of valsartan in this microcapsule was changed from crystalline to amorphous form during the spray-drying process and maintained as an amorphous form at 40 degrees C for at least 3 months, indicating that it was physically stable. HPMC in this microcapsule could inhibit the recrystallization, resulting in stabilizing the amorphous form of valsartan. Furthermore, it improved the oral bioavailability of valsartan compared to valsartan powder and gave the similar AUC, C(max), and T(max) values to commercial product, suggesting that it was bioequivalent to commercial product in rats. Thus, the gelatin microcapsule with HPMC would be a more effective and stable oral delivery system of poorly water-soluble valsartan.

show abstract

“…Microspheres are characteristically free flowing powders consisting of proteins or synthetic polymers which are biodegradable in nature (Cao et al, 2011). Microspheres are defined as ''Monolithic sphere or therapeutic agent distributed throughout the matrix either as a molecular dispersion of particles'' can be defined as structure made up of continuous phase of one or more miscible polymers in which drug particles are dispersed at the molecular or macroscopic level (Comoglu et al, 2008;Modgill et al, 2014). Microspheres can be manufactured from various natural and synthetic materials (Kalia et al, 2014).…”

Section: Rifampicinmentioning

confidence: 99%

Advances in nanotechnology-based carrier systems for targeted delivery of bioactive drug molecules with special emphasis on immunotherapy in drug resistant tuberculosis – a critical review

et al. 2015

View full text Add to dashboard Cite

From the early sixteenth and seventeenth centuries to the present day of life, tuberculosis (TB) still is a global health threat with some new emergence of resistance. This type of emergence poses a vital challenge to control TB cases across the world. Mortality and morbidity rates are high due to this new face of TB. The newer nanotechnology-based drug-delivery approaches involving micro-metric and nano-metric carriers are much needed at this stage. These delivery systems would provide more advantages over conventional systems of treatment by producing enhanced therapeutic efficacy, uniform distribution of drug molecule to the target site, sustained and controlled release of drug molecules and lesser side effects. The main aim to develop these novel drug-delivery systems is to improve the patient compliance and reduce therapy time. This article reviews and elaborates the new concepts and drug-delivery approaches for the treatment of TB involving solid-lipid particulate drug-delivery systems (solid-lipid micro- and nanoparticles, nanostructured lipid carriers), vesicular drug-delivery systems (liposomes, niosomes and liposphere), emulsion-based drug-delivery systems (micro and nanoemulsion) and some other novel drug-delivery systems for the effective treatment of tuberculosis and role of immunomodulators as an adjuvant therapy for management of MDR-TB and XDR-TB.

show abstract

Development and In Vitro Evaluation of Pantoprazole-Loaded Microspheres

Cited by 27 publications

References 25 publications

Influence of Some Formulation Variables on the Optimization of pH-dependent, Colon-targeted, Sustained-release Mesalamine Microspheres

Influence of Some Formulation Variables on the Optimization of pH-dependent, Colon-targeted, Sustained-release Mesalamine Microspheres

Development of valsartan-loaded gelatin microcapsule without crystal change using hydroxypropylmethylcellulose as a stabilizer

Advances in nanotechnology-based carrier systems for targeted delivery of bioactive drug molecules with special emphasis on immunotherapy in drug resistant tuberculosis – a critical review

Contact Info

Product

Resources

About