A reproducible accelerated in vitro release testing method for PLGA microspheres

Shen, Jie; Lee, Kyulim; Choi, Stephanie; Qu, Wen; Wang, Yan; Burgess, Diane J.

doi:10.1016/j.ijpharm.2015.12.031

Cited by 56 publications

(26 citation statements)

References 31 publications

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“…Poly-dl-lactic-coglycolic acid (PLGA), biodegradable polymer, has been approved for use in drug delivery such as Risperdal ® Consta ® , Lupron Depot ® , and Sandostatin ® LAR (long acting release) by the Food and Drug Administration, and it has been reported as a controlled release system (Kang et al, 2004;Shen et al, 2016). Moreover, to enhance solubility and permeability, surfactant addition is necessary when formulating PLGA NPs.…”

Section: Introductionmentioning

confidence: 99%

Enhancing the in vitro anticancer activity of albendazole incorporated into chitosan-coated PLGA nanoparticles

Kang

Choi

Lee

et al. 2017

Carbohydrate Polymers

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Section: Introductionmentioning

confidence: 99%

Enhancing the in vitro anticancer activity of albendazole incorporated into chitosan-coated PLGA nanoparticles

Kang

Choi

Lee

et al. 2017

Carbohydrate Polymers

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“…The degree of SSA gain depends on the type and concentration of used stabilizer as well as sort of organic solvent . These parameters are the renowned defining factors impacting the mechanical and hydrophobic properties of nanoparticles, thus also potentially affect the nonspherical nanoparticle shape stability.…”

Section: Discussionmentioning

confidence: 99%

Nonspherical Nanoparticle Shape Stability Is Affected by Complex Manufacturing Aspects: Its Implications for Drug Delivery and Targeting

Haryadi

Hafner

Amin

et al. 2019

Adv Healthcare Materials

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The shape of nanoparticles is known recently as an important design parameter influencing considerably the fate of nanoparticles with and in biological systems. Several manufacturing techniques to generate nonspherical nanoparticles as well as studies on in vitro and in vivo effects thereof have been described. However, nonspherical nanoparticle shape stability in physiological‐related conditions and the impact of formulation parameters on nonspherical nanoparticle resistance still need to be investigated. To address these issues, different nanoparticle fabrication methods using biodegradable polymers are explored to produce nonspherical nanoparticles via the prevailing film‐stretching method. In addition, systematic comparisons to other nanoparticle systems prepared by different manufacturing techniques and less biodegradable materials (but still commonly utilized for drug delivery and targeting) are conducted. The study evinces that the strong interplay from multiple nanoparticle properties (i.e., internal structure, Young's modulus, surface roughness, liquefaction temperature [glass transition (Tg) or melting (Tm)], porosity, and surface hydrophobicity) is present. It is not possible to predict the nonsphericity longevity by merely one or two factor(s). The most influential features in preserving the nonsphericity of nanoparticles are existence of internal structure and low surface hydrophobicity (i.e., surface‐free energy (SFE) > ≈55 mN m−1, material–water interfacial tension <6 mN m−1), especially if the nanoparticles are soft (<1 GPa), rough (Rrms > 10 nm), porous (>1 m2 g−1), and in possession of low bulk liquefaction temperature (<100 °C). Interestingly, low surface hydrophobicity of nanoparticles can be obtained indirectly by the significant presence of residual stabilizers. Therefore, it is strongly suggested that nonsphericity of particle systems is highly dependent on surface chemistry but cannot be appraised separately from other factors. These results and reviews allot valuable guidelines for the design and manufacturing of nonspherical nanoparticles having adequate shape stability, thereby appropriate with their usage purposes. Furthermore, they can assist in understanding and explaining the possible mechanisms of nonspherical nanoparticles effectivity loss and distinctive material behavior at the nanoscale.

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“…[16][17][18][19] For LAI drug products, there are also benefits to developing an accelerated drug release testing method. 20 There are several in vitro test methods available for measuring the drug release. 21 Commonly used methods include rotating basket (U.S. Pharmacopeia [USP] type I apparatus), paddletype (USP type II apparatus), and reciprocating cylinder (USP type III apparatus) methods which were developed specifically for oral dosage forms.…”

Section: Introductionmentioning

confidence: 99%

Beyond Q1/Q2: The Impact of Manufacturing Conditions and Test Methods on Drug Release From PLGA-Based Microparticle Depot Formulations

Garner

Skidmore

Park

et al. 2018

Journal of Pharmaceutical Sciences

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Drug-loaded polymeric microparticles have been used as long-acting injectable (LAI) depot formulations. To obtain U.S. Food and Drug Administration approval, a generic LAI depot product needs to be qualitatively (Q1) and quantitatively (Q2) the same in terms of inactive ingredients as its reference-listed drug. However, Q1/Q2 sameness as the reference-listed drug does not guarantee the same in vitro drug release profile and in vivo performance, especially when the manufacturing methods are different. There is little consensus on how the in vitro testing needs to be done to examine the release profiles of LAI depot formulations. This study examined the manufacturing differences in making risperidone-loaded poly(lactide-co-glycolide) microparticles and their impact on the release kinetics. It also examined the impacts of in vitro testing methods on the drug release profiles. Two in-house manufactured risperidone poly(lactide-co-glycolide) microparticles and Risperdal Consta were used in the study. Of the in vitro release methods tested, the orbital agitation method provided the most reproducible release profiles. The results indicate that the in vitro release kinetics depend not only on manufacturing procedures but also on the in vitro testing conditions, such as the agitation speed, vessel-dimensions, solid beads, media exchange volume, and other parameters both under real-time and accelerated testing conditions. In the current case, the in vitro experimental condition seemed to affect the drug release kinetics more than the manufacturing differences. The developed orbital agitation release testing method is simple, robust, and reproducible, which allows the comparison of in vitro release profiles of formulations that are prepared with manufacturing differences.

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A reproducible accelerated in vitro release testing method for PLGA microspheres

Cited by 56 publications

References 31 publications

Enhancing the in vitro anticancer activity of albendazole incorporated into chitosan-coated PLGA nanoparticles

Enhancing the in vitro anticancer activity of albendazole incorporated into chitosan-coated PLGA nanoparticles

Nonspherical Nanoparticle Shape Stability Is Affected by Complex Manufacturing Aspects: Its Implications for Drug Delivery and Targeting

Beyond Q1/Q2: The Impact of Manufacturing Conditions and Test Methods on Drug Release From PLGA-Based Microparticle Depot Formulations

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