The effect of PLGA molecular weight differences on risperidone release from microspheres

Kohno, Moe; Andhariya, Janki V.; Wan, Bo; Bao, Quanying; Rothstein, Sam N.; Hezel, Michael; Wang, Yan; Burgess, Diane J.

doi:10.1016/j.ijpharm.2020.119339

Cited by 66 publications

(36 citation statements)

References 30 publications

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“…Therefore, the net sheer stress upon PLGA polymers is reduced during preparation of NPs, resulting in larger particle size of NPs. 23 , 30 , 31 With a constant LA/GA ratio, a higher MW of PLGA impedes formation of sufficient water-filled pores on NPs surface compared to a PLGA with lower MW, which limits drug diffusion through the NPs matrix and therefore protracts drug release. 32 , 33 However, the release kinetics of all PLGA NPs with different MWs followed the Higuchi model, indicating that the MWs did not significantly affect release kinetics.…”

Section: Resultsmentioning

confidence: 99%

<p>PLGA Nanoparticle Platform for Trans-Ocular Barrier to Enhance Drug Delivery: A Comparative Study Based on the Application of Oligosaccharides in the Outer Membrane of Carriers</p>

Jiang¹,

Jia²,

Qiu³

et al. 2020

IJN

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The trans-ocular barrier is a key factor limiting the therapeutic efficacy of triamcinolone acetonide. We developed a poly(lactic-co-glycolic acid) nanoparticles (PLGA NPs) surface modified respectively with 2-hydroxypropyl-β-cyclodextrin (2-HP-β-CD), chitosan oligosaccharide and trehalose. Determination of the drug/nanoparticles interactions, characterization of the nanoparticles, in vivo ocular compatibility tests, comparisons of their corneal permeability and their pharmacokinetics in aqueous humor were carried out. Methods: All PLGA NPs were prepared by the single emulsion and evaporation method and the drug-nanoparticle interaction was studied. The physiochemical features and in vitro corneal permeability of NPs were characterized while the aqueous humor pharmacokinetics was performed to evaluate in vivo corneal permeability of NPs. Ocular compatibility of NPs was investigated through Draize and histopathological test. Results: The PLGA NPs with lactide/glycolide ratio of 50:50 and small particle size (molecular weight 10 kDa) achieved optimal drug release and corneal permeability. Surface modification with different oligosaccharides resulted in uniform particle sizes and similar drug-nanoparticle interactions, although 2-HP-β-CD/PLGA NPs showed the highest entrapment efficiency. In vitro evaluation and aqueous humor pharmacokinetics further revealed that 2-HP-β-CD/PLGA NPs had greater trans-ocular permeation and retention compared to chitosan oligosaccharide/PLGA and trehalose/PLGA NPs. No ocular irritation in vivo was detected after applying modified/unmodified PLGA NPs to rabbit's eyes. Conclusion: 2-HP-β-CD/PLGA NPs are a promising nanoplatform for localized ocular drug delivery through topical administration.

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Section: Resultsmentioning

confidence: 99%

<p>PLGA Nanoparticle Platform for Trans-Ocular Barrier to Enhance Drug Delivery: A Comparative Study Based on the Application of Oligosaccharides in the Outer Membrane of Carriers</p>

Jiang¹,

Jia²,

Qiu³

et al. 2020

IJN

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“…The results of the residual solvents analysis showed that EA was employed in the preparation of Vivitrol ® . Furthermore, EA and water are partially miscible; thus, EA and water move dynamically during microsphere solidification [19,31]. This dynamic movement leads to water inclusion in PLGA micro-spheres, resulting in an irregular shape and indentation during the drying process [17].…”

Section: Discussionmentioning

confidence: 99%

“…Vivitrol ® and the GNM showed bi-phasic release profiles with a small burst release phase followed by continuous zero-order release over 35 days. These in vitro release profiles could depend on the physicochemical properties of PLGA (such as L/G ratio, molecular weight, crystallinity, and monomer sequence) and the drug, as well as the critical quality attributes of microspheres (such as drug loading, particle size, morphology, porosity, Tg, and contact angle) [19]. These data are consistent with the published literature, which shows that Vivitrol ® does not have a lag phase in vitro, potentially owing to enhanced polymer degradation as a result of quickly decreasing local acidic pH after one week, hydrolysis, and these accelerated PLGA degradations [26,27].…”

Section: Discussionmentioning

confidence: 99%

“…As shown in Table 1, the Tg of Vivitrol ® and the GNM was 47.32 ± 0.19 and 48.63 ± 3.73 °C, respectively (mean ± standard deviation (SD), n = 3), which provides guidance for the study of the method and mechanism of real-time and accelerated release in vitro [19].…”

Section: Tg and Water Contact Anglementioning

confidence: 90%

“…As shown in Table 1, the Tg of Vivitrol ® and the GNM was 47.32 ± 0.19 and 48.63 ± 3.73 • C, respectively (mean ± standard deviation (SD), n = 3), which provides guidance for the study of the method and mechanism of real-time and accelerated release in vitro [19]. The water contact angle of Vivitrol ® and the GNM was 64.41 ± 0.91 and 55.93 ± 0.38 • C, respectively, which may reflect the difference in a series of microsphere characteristics, such as porosity, particle size, and so on.…”

Section: Tg and Water Contact Anglementioning

confidence: 91%

See 2 more Smart Citations

Key Factor Study for Generic Long-Acting PLGA Microspheres Based on a Reverse Engineering of Vivitrol®

Hua¹,

Wang²,

Wang³

et al. 2021

Molecules

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The FDA (U.S. Food and Drug Administration) has approved only a negligible number of poly(lactide-co-glycolide) (PLGA)-based microsphere formulations, indicating the difficulty in developing a PLGA microsphere. A thorough understanding of microsphere formulations is essential to meet the challenge of developing innovative or generic microspheres. In this study, the key factors, especially the key process factors of the marketed PLGA microspheres, were revealed for the first time via a reverse engineering study on Vivitrol® and verified by the development of a generic naltrexone-loaded microsphere (GNM). Qualitative and quantitative similarity with Vivitrol®, in terms of inactive ingredients, was accomplished by the determination of PLGA. Physicochemical characterization of Vivitrol® helped to identify the critical process parameters in each manufacturing step. After being prepared according to the process parameters revealed by reverse engineering, the GNM demonstrated similarity to Vivitrol® in terms of quality attributes and in vitro release (f2 = 65.3). The research on the development of bioequivalent microspheres based on the similar technology of Vivitrol® will benefit the development of other generic or innovative microspheres.

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Profiling Pro‐Inflammatory Proteases as Biomolecular Signatures of Material‐Induced Subcutaneous Host Response in Immuno‐Competent Mice

Tran,

Truong,

Nguyen

et al. 2024

Advanced Science

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Proteases are important modulators of inflammation, but they remain understudied in material‐induced immune response, which is critical to clinical success of biomedical implants. Herein, molecular expression and proteolytic activity of three distinct proteases, namely neutrophil elastase, matrix metalloproteinases, cysteine cathepsins (cathepsin‐K and cathepsin‐B) are comprehensively profiled, in the subcutaneous host response of immuno‐competent mice against different biomaterial implants. Quantitative non‐invasive monitoring with activatable fluorescent probes reveals that different microparticulate materials induce distinct levels of protease activity with degradable poly(lactic‐co‐glycolic) acid inducing the strongest signal compared to nondegradable materials such as polystyrene and silica oxide. Furthermore, protein expression of selected proteases, attributable to both their inactive and active forms, notably deviates from their activities associated only with their active forms. Protease activity exhibits positive correlations with protein expression of pro‐inflammatory cytokines tumor necrosis factor α and interleukin 6 but negative correlation with pro‐fibrotic cytokine transforming growth factor β1. This study also demonstrates the predictive utility of protease activity as a non‐invasive, pro‐inflammatory parameter for evaluation of the anti‐inflammatory effects of model bioactive compounds on material‐induced host response. Overall, the findings provide new insights into protease presence in material‐induced immune responses, facilitating future biomaterial assessment to evoke appropriate host responses for implant applications.

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The effect of PLGA molecular weight differences on risperidone release from microspheres

Cited by 66 publications

References 30 publications

<p>PLGA Nanoparticle Platform for Trans-Ocular Barrier to Enhance Drug Delivery: A Comparative Study Based on the Application of Oligosaccharides in the Outer Membrane of Carriers</p>

<p>PLGA Nanoparticle Platform for Trans-Ocular Barrier to Enhance Drug Delivery: A Comparative Study Based on the Application of Oligosaccharides in the Outer Membrane of Carriers</p>

Key Factor Study for Generic Long-Acting PLGA Microspheres Based on a Reverse Engineering of Vivitrol®

Profiling Pro‐Inflammatory Proteases as Biomolecular Signatures of Material‐Induced Subcutaneous Host Response in Immuno‐Competent Mice

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