The study of drug release from microspheres adhered on pig vesical mucosa

Burjak, Matejka; Bogataj, Marija; Velnar, M; Grabnar, Iztok; Mrhar, Aleš

doi:10.1016/s0378-5173(01)00748-7

Cited by 35 publications

(22 citation statements)

References 7 publications

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“…These include the use of polymers of both natural and synthetic type, such as chitosan, carbomers, polycarbophil gelatin, polyethylene glycol, poly(methylidene malonate‐2.1.2), and cellulose derivatives . In a comparative study, chitosan was found to exhibit greater mucoadhesion to the bladder wall than carboxymethylcellulose (CMC) and polycarbophyl, thus resulting in a slower drug release and prolonged residence time …”

Section: Application Specific Requirementmentioning

confidence: 99%

Innovative Methods and Applications in Mucoadhesion Research

Mackie

Goycoolea

Menchicchi

et al. 2017

Macromolecular Bioscience

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The present review is aimed at elucidating relatively new aspects of mucoadhesion/mucus interaction and related phenomena that emerged from a Mucoadhesion workshop held in Munster on 2-3 September 2015 as a satellite event of the ICCC 13th-EUCHIS 12th. After a brief outline of the new issues, the focus is on mucus description, purification, and mucus/mucin characterization, all steps that are pivotal to the understanding of mucus related phenomena and the choice of the correct mucosal model for in vitro and ex vivo experiments, alternative bio/mucomimetic materials are also presented. Then a selection of preparative techniques and testing methods are described (at molecular as well as micro and macroscale) that may support the pharmaceutical development of mucus interactive systems and assist formulators in the scale-up and industrialization steps. Recent applications of mucoadhesive systems (including medical devices) intended for different routes of administration (oral, gastrointestinal, vaginal, nasal, ocular, and intravesical) and for the treatment of difficult to treat pathologies or the alleviation of symptoms are described.

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Section: Application Specific Requirementmentioning

confidence: 99%

Innovative Methods and Applications in Mucoadhesion Research

Mackie

Goycoolea

Menchicchi

et al. 2017

Macromolecular Bioscience

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“…To overcome this situation, frequent treatments with repeated catheterizations are required, leading in many cases to irritation during voiding, bladder fibrosis, and infections. 4 Hence, there is a need for the development of sustained intravesical drug delivery systems, which can provide prolonged contact between the drug and the affected tissues and can reduce the chance of recurrence of the disease. 5 Gemcitabine hydrochloride (Gem-HCl) is a deoxycytidine analog with a broad spectrum of antitumor activity.…”

Section: Introductionmentioning

confidence: 99%

Design and evaluation of an intravesical delivery system for superficial bladder cancer: preparation of gemcitabine HCl-loaded chitosan–thioglycolic acid nanoparticles and comparison of chitosan/poloxamer gels as carriers

Şenyiğit¹,

Karavana²,

İlem-Özdemir³

et al. 2015

IJN

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This study aimed to develop an intravesical delivery system of gemcitabine HCl for superficial bladder cancer in order to provide a controlled release profile, to prolong the residence time, and to avoid drug elimination via urination. For this aim, bioadhesive nanoparticles were prepared with thiolated chitosan (chitosan–thioglycolic acid conjugate) and were dispersed in bioadhesive chitosan gel or in an in situ gelling poloxamer formulation in order to improve intravesical residence time. In addition, nanoparticle-loaded gels were diluted with artificial urine to mimic in vivo conditions in the bladder and were characterized regarding changes in gel structure. The obtained results showed that chitosanthioglycolic acid nanoparticles with a mean diameter of 174.5±3.762 nm and zeta potential of 32.100±0.575 mV were successfully developed via ionotropic gelation and that the encapsulation efficiency of gemcitabine HCl was nearly 20%. In vitro/ex vivo characterization studies demonstrated that both nanoparticles and nanoparticle-loaded chitosan and poloxamer gels might be alternative carriers for intravesical administration of gemcitabine HCl, prolonging its residence time in the bladder and hence improving treatment efficacy. However, when the gel formulations were diluted with artificial urine, poloxamer gels lost their in situ gelling properties at body temperature, which is in conflict with the aimed formulation property. Therefore, 2% chitosan gel formulation was found to be a more promising carrier system for intravesical administration of nanoparticles.

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“…Microspheres were prepared by the solvent evaporation method and matrix polymer was Eudragit RS. 7,8) The stirring rate of emulsion system is one of the frequently studied process parameters in solvent evaporation procedure. The effect of this parameter on biopharmaceutical properties of microspheres containing drug and matrix polymer was often observed.…”

mentioning

confidence: 99%

The Influence of Chitosan on in Vitro Properties of Eudragit RS Microspheres.

Kriznar

Mateović

Bogataj

et al. 2003

CHEMICAL & PHARMACEUTICAL BULLETIN

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Eudragit RS microspheres containing chitosan hydrochloride were prepared by the solvent evaporation method using acetone/liquid paraffin solvent system and their properties were compared with Eudragit RS microspheres without chitosan, prepared in our previous study. Different stirring rates were applied (400-1200 rpm) and drug content, Higuchi dissolution rate constant, surface and structure characteristics of the microspheres were determined for each size fraction. An increase in average particle size with a reduction of stirring rate appeared in limited interval in both series. The average particle size of microspheres without chitosan, prepared at the same stirring rate, was smaller. Pipemidic acid content increased with increasing fraction particle size, but not with increasing stirring rate as it was observed for microspheres without chitosan. We presume that high pipemidic acid content in larger microspheres is a consequence of cumulation of undissolved pipemidic acid particles in larger droplets during microspheres preparation procedure. Pipemidic acid release was faster from microspheres with chitosan and no correlation between Higuchi dissolution rate constant and stirring rate or fraction particle size was found, though it existed in the system without chitosan. Structure and surface characteristics of microspheres observed by scanning electron microscope (SEM) were not changed significantly by incorporation of chitosan. But in contrast with microspheres without chitosan, the surface of chitosan microspheres was more porous after three hours of dissolution. It is supposed that the influence of particle size fraction and stirring rate on release characteristics is expressed to a great extent through porosity and indirectly through total effective surface area, but the incorporation of highly soluble component i.e. chitosan salt hides these effects on drug release. In conclusion, changes in biopharmaceutical properties due to varying stirring rate and fraction particle size exhibited the same direction as those reported for the microspheres without chitosan, although they are less expressed because of increased experimental variability, likely caused by chitosan.

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The study of drug release from microspheres adhered on pig vesical mucosa

Cited by 35 publications

References 7 publications

Innovative Methods and Applications in Mucoadhesion Research

Innovative Methods and Applications in Mucoadhesion Research

Design and evaluation of an intravesical delivery system for superficial bladder cancer: preparation of gemcitabine HCl-loaded chitosan–thioglycolic acid nanoparticles and comparison of chitosan/poloxamer gels as carriers

The Influence of Chitosan on in Vitro Properties of Eudragit RS Microspheres.

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The study of drug release from microspheres adhered on pig vesical mucosa

Cited by 35 publications

References 7 publications

Innovative Methods and Applications in Mucoadhesion Research

Innovative Methods and Applications in Mucoadhesion Research

Design and evaluation of an intravesical delivery system for superficial bladder cancer: preparation of gemcitabine HCl-loaded chitosan&ndash;thioglycolic acid nanoparticles and comparison of chitosan/poloxamer gels as carriers

The Influence of Chitosan on in Vitro Properties of Eudragit RS Microspheres.

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Design and evaluation of an intravesical delivery system for superficial bladder cancer: preparation of gemcitabine HCl-loaded chitosan–thioglycolic acid nanoparticles and comparison of chitosan/poloxamer gels as carriers