Evaluation of in vivo release characteristics of protein-loaded biodegradable microspheres in rats and severe combined immunodeficiency disease mice

Morita, Takahiro; Sakamura, Yumi; Horikiri, Yuji; Suzuki, Takehiko; Yoshino, Hideaki

doi:10.1016/s0168-3659(01)00280-2

Cited by 21 publications

(7 citation statements)

References 16 publications

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“…The first high plasma drug concentration of nalmefene in the earlier five days was due to the initial fast drug release from the microparticles [ 35 ]. The later high drug level may be associated with the second fast in vivo drug release of the microspheres, in which the microparticles break down and the degraded pieces were intake by macrophage [ 38 , 39 ].…”

Section: Resultsmentioning

confidence: 99%

In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene

Xie

Lin

Xing³

et al. 2015

PLoS ONE

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Poor patient compliance, untoward reactions and unstable blood drug levels after the bolus administration are impeding the pharmacotherapy for insobriety. A long-acting preparation may address these limitations. The aim of this paper was to further investigate the in vitro characteristics and in vivo performances of nalmefene microspheres. Nalmefene was blended with poly (lactide-co-glycolide) (PLGA) to prepare the target microspheres by an O/O emulsification solvent evaporation method. The prepared microspheres exhibited a controlled release profile of nalmefene in vitro over 4 weeks, which was well fitted with a first-order model. In vitro degradation study showed that the drug release in vitro was dominated by both drug diffusion and polymer degradation mechanisms. Pharmacokinetics study indicated that the prepared microspheres could provide a relatively constant of nalmefene plasma concentration for at least one month in rats. The in vivo pharmacokinetics profile was well correlated with the in vitro drug release. Pharmacodynamics studies revealed that the drug loaded microspheres could produce a long-acting antagonism efficacy on rats. These results demonstrated the promising application of injectable PLGA microspheres containing nalmefene for the long-term treatment of alcohol dependence.

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Section: Resultsmentioning

confidence: 99%

In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene

Xie

Lin

Xing³

et al. 2015

PLoS ONE

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“…This drug delivery system has emerged as a remedial measure to improve site-specific drug delivery to a considerable extent and has already been applied to improve the therapeutic response and to reduce adverse effects [13]. The drugs in implant microspheres are absorbed by the capillaries of the injection site and lymph organs, enter the systemic circulation, and then tend to be distributed to the target organ to play a pharmacodynamics [14], which can bypass the first pass effect and avoid pre-systemic elimination in the Gl tract or liver with oral administration.…”

Section: Introductionmentioning

confidence: 99%

Docetaxel-Loaded Chitosan Microspheres as a Lung Targeted Drug Delivery System: In Vitro and in Vivo Evaluation

Wang

Zhou

2014

IJMS

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The aim of this study was to prepare docetaxel-loaded chitosan microspheres and to evaluate their in vitro and in vivo characteristics. Glutaraldehyde crosslinked microspheres were prepared using a water-in-oil emulsification method, and characterized in terms of the morphological examination, particle size distribution, encapsulation ratio, drug-loading coefficient and in vitro release. Pharmacokinetics and biodistribution studies were used to evaluate that microspheres have more advantage than the conventional formulations. The emulsion crosslinking method was simple to prepare microspheres and easy to scale up. The formed microspheres were spherical in shape, with a smooth surface and the size was uniform (9.6 ± 0.8 μm); the encapsulation efficiency and drug loading of prepared microspheres were 88.1% ± 3.5% and 18.7% ± 1.2%, respectively. In vitro release indicated that the DTX microspheres had a well-sustained release efficacy and in vivo studies showed that the microspheres were found to release the drug to a maximum extent in the target tissue (lung). The prepared microspheres were found to possess suitable physico-chemical properties and the particle size range. The sustained release of DTX from microspheres revealed its applicability as drug delivery system to minimize the exposure of healthy tissues while increasing the accumulation of therapeutic drug in target sites.

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“…These include proteins such as lysozyme (75), bovine-derived superoxide dismutase (124), and peptides such as orntide (116,117), vapreotide (41), TRH (125,126), and small molecules such as methadone (74). SpragueYDawley (SYD) or Wistar species of the rat are the most commonly used models for in vivo experiments.…”

Section: Ivivc With Parenteral Microspheresmentioning

confidence: 99%

Methods to Assess in Vitro Drug Release from Injectable Polymeric Particulate Systems

2006

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This review provides a compilation of the methods used to study real-time (37 degrees C) drug release from parenteral microparticulate drug delivery systems administered via the subcutaneous or intramuscular route. Current methods fall into three broad categories, viz., sample and separate, flow-through cell, and dialysis techniques. The principle of the specific method employed along with the advantages and disadvantages are described. With the "sample and separate" technique, drug-loaded microparticles are introduced into a vessel, and release is monitored over time by analysis of supernatant or drug remaining in the microspheres. In the "flow-through cell" technique, media is continuously circulated through a column containing drug-loaded microparticles followed by analysis of the eluent. The "dialysis" method achieves a physical separation of the drug-loaded microparticles from the release media by use of a membrane, which allows for sampling without interference of the microspheres. With all these methods, the setup and sampling techniques seem to influence in vitro release; the results are discussed in detail, and criteria to aid in selection of a method are stated. Attempts to establish in vitro-in vivo correlation for these injectable dosage forms are also discussed. It would be prudent to have an in vitro test method for microparticles that satisfies compendial and regulatory requirements, is user friendly, robust, and reproducible, and can be used for quality-control purposes at real-time and elevated temperatures.

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Evaluation of in vivo release characteristics of protein-loaded biodegradable microspheres in rats and severe combined immunodeficiency disease mice

Cited by 21 publications

References 16 publications

In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene

In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene

Docetaxel-Loaded Chitosan Microspheres as a Lung Targeted Drug Delivery System: In Vitro and in Vivo Evaluation

Methods to Assess in Vitro Drug Release from Injectable Polymeric Particulate Systems

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