Elevated temperature accelerated release testing of PLGA microspheres

Zolnik, Banu S.; Leary, Pauline E.; Burgess, Diane J.

doi:10.1016/j.jconrel.2006.02.015

Cited by 206 publications

(158 citation statements)

References 30 publications

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“…DLG 7525 6E) microspheres is normally governed by a combination of polymer erosion and drug diffusion (Zolnik et al, 2006). Accordingly, complex drug release characteristics (e.g.…”

Section: Discussionmentioning

confidence: 99%

“…Accelerated in vitro release testing based on elevated temperature has been successfully used as a fast quality control tool for PLGA based parenteral dosage forms (such as microspheres and implants) (D'Souza et al, 2014;Shen and Burgess, 2012a;Zolnik et al, 2006). Elevated temperature can accelerate PLGA polymer erosion (Zolnik et al, 2006), as well as enhance polymer mobility and thereby drug diffusion (Duda and Zielinski, 1996).…”

Section: Discussionmentioning

confidence: 99%

“…Elevated temperature can accelerate PLGA polymer erosion (Zolnik et al, 2006), as well as enhance polymer mobility and thereby drug diffusion (Duda and Zielinski, 1996). Accordingly, significantly reduced risperidone release duration was obtained for all prepared microspheres at 45°C (Figs.…”

Section: Discussionmentioning

confidence: 99%

“…temperature, pH, surfactants, and the presence of enzymes) can hasten the rate of polymer hydration and/or polymer degradation and drug diffusion, thus accelerating drug release from PLGA microspheres (Alexis, 2005;Shen and Burgess, 2012b;Zolnik and Burgess, 2007;Zolnik et al, 2006). Ideally, drug release in real-time and accelerated tests should follow the same release mechanism with a 1:1 correlation between the release profiles (Zolnik et al, 2006). However, it is possible that the drug release mechanism(s) may change since accelerated release tests are typically performed under extreme conditions (e.g.…”

Section: Introductionmentioning

confidence: 99%

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A reproducible accelerated in vitro release testing method for PLGA microspheres

Shen

Lee

Choi

et al. 2016

International Journal of Pharmaceutics

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The objective of the present study was to develop a discriminatory and reproducible accelerated in vitro release method for long-acting PLGA microspheres with inner structure/porosity differences. Risperidone was chosen as a model drug. Qualitatively and quantitatively equivalent PLGA microspheres with different inner structure/porosity were obtained using different manufacturing processes. Physicochemical properties as well as degradation profiles of the prepared microspheres were investigated. Furthermore, in vitro release testing of the prepared risperidone microspheres was performed using the most common in vitro release methods (i.e. sample-andseparate and flow through) for this type of product. The obtained compositionally equivalent risperidone microspheres had similar drug loading but different inner structure/porosity. When microsphere particle size appeared similar, porous risperidone microspheres showed faster microsphere degradation and drug release compared with less porous microspheres. Both in vitro release methods investigated were able to differentiate risperidone microsphere formulations with differences in porosity under real-time (37°C) and accelerated (45°C) testing conditions. Notably, only the accelerated USP apparatus 4 method showed good reproducibility for highly porous risperidone microspheres. These results indicated that the accelerated USP apparatus 4 method is an appropriate fast quality control tool for long-acting PLGA microspheres (even with porous structures). Graphical Abstract*

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“…DLG 7525 6E) microspheres is normally governed by a combination of polymer erosion and drug diffusion (Zolnik et al, 2006). Accordingly, complex drug release characteristics (e.g.…”

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

A reproducible accelerated in vitro release testing method for PLGA microspheres

Shen

Lee

Choi

et al. 2016

International Journal of Pharmaceutics

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“…A larger protein is supposed to be released slower than a smaller protein, because it takes more time for a larger molecule to diffuse out through the narrow interconnected channels of the hydrogel matrix [20]. BSA is an ellipsoid protein with "66,400 Da molecular weight, while insulin is a small protein ("6,000 Da), and hence, BSA should be released slower than insulin; however, it was observed that the release of BSA was much faster than insulin [21,22].…”

Section: In Vitro Releasementioning

confidence: 99%

Effect of Molar Mass and Water Solubility of Incorporated Molecules on the Degradation Profile of the Triblock Copolymer Delivery System

et al. 2015

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The purpose of this study was to investigate the effects of size and type of incorporated model molecules on the polymer degradation and release profile from thermosensitive triblock copolymer based controlled delivery systems. In vitro release of the incorporated molecules demonstrated slow release for risperidone (molecular weight (M w ) = 410.48 Da; partition coefficient (K o/w ) = 3.49), while bovine serum albumin (BSA) (M w = "66,400 Da; K o/w = 0.007) and insulin (M w = 5808 Da; K o/w = 0.02) showed initial burst release followed by controlled release. The proton NMR, Gel Permeation Chromatography, and Cryo-SEM studies suggest that the size and partition coefficient of incorporated molecules influence the pore size, polymer degradation, and their release. In spite of using a similar polymer delivery system the polymer degradation rate and drug release notably differ for these model molecules. Therefore, size and oil-water partition coefficient are important factors for designing the controlled release formulation of therapeutics from triblock copolymer based delivery systems.Polymers 2015, 7 1511

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D’Souza

2019

In Vitro Drug Release Testing of Special Dosage Forms

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Elevated temperature accelerated release testing of PLGA microspheres

Cited by 206 publications

References 30 publications

A reproducible accelerated in vitro release testing method for PLGA microspheres

A reproducible accelerated in vitro release testing method for PLGA microspheres

Effect of Molar Mass and Water Solubility of Incorporated Molecules on the Degradation Profile of the Triblock Copolymer Delivery System

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