Critical attributes of formulation and of elaboration process of PLGA-protein microparticles

Fraguas-Sánchez, Ana Isabel; Aparicio-Blanco, Juan; Cano‐Abad, María F.; Torres-Suárez, Ana Isabel

doi:10.1016/j.ijpharm.2015.01.008

Cited by 26 publications

(11 citation statements)

References 33 publications

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“…Formulation or processing parameters and respective mechanistic effect on the microparticles coupled with their expected performance impact. Drug release rate decreases [43][44][45][46][47] PLGA molecular weight (MW) increase Low MW polymer more soluble in an organic phase → • Slow solidification resulting in porous microparticles • Degradation rate decrease Drug release rate decreases [48][49][50] Drug loading increase Increase of drug:PLGA ratio Drug release rate increases [ 10,51,52] Polymer concentration increase • Increase in viscosity delays drug diffusion from droplets • Polymer precipitates faster on surface Encapsulation efficiency increases [ 53,54] Emulsifier concentration increase Decrease in particle size Drug release rate increases [ 55,56] Energy input increase (e.g., homogenization speed, sonication amplitude)…”

Section: Skin Formationmentioning

confidence: 99%

Initial Formation of the Skin Layer of PLGA Microparticles

Sharifi¹,

Otte²,

Park³

2021

Adv Healthcare Materials

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The Special Issue Dedicated to Professor Nicholas Peppas Poly(lactide-co-glycolide) (PLGA) has been extensively used in making long-acting injectable formulations. The critical factors affecting the PLGA formulation properties have been adjusted to control the drug release kinetics and obtain desirable properties of PLGA-based drug delivery systems. The PLGA microparticle formation begins as soon as the drug/PLGA-dissolved in the organic solvent phase (oil phase) is exposed to the water phase. The initial skin (or shell) formation on the oil droplets occurs very quickly, sometimes in the matter of milliseconds, and studying the process has been difficult. The skin formation on the PLGA emulsion droplet surface that can affect the subsequent hardening steps is examined. PLGA droplets with different compositions are prepared. Using collimated light and a high-speed camera made it possible to detect the diffusion of acetonitrile from the oil phase into the water phase during the oil droplet formation. Although the skin formation is not visible on the surface of the oil phase droplet with the current setup, the droplet shapes, solid strand formation, and the difference in the spreading time suggest that the initial contact time between the oil and water phases in the range of a few seconds is critical to the properties of the skin.

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Section: Skin Formationmentioning

confidence: 99%

Initial Formation of the Skin Layer of PLGA Microparticles

Sharifi¹,

Otte²,

Park³

2021

Adv Healthcare Materials

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“…There are several parameters that have to be adjusted to optimize the characteristics of particles prepared by the double emulsion method. These include the amount of hydrophilic drug to be added, polymer concentration, type of solvent, stabilizer concentration, volume of the second aqueous phase, stirring rate and other variables [1,17,29,[32][33][34]. Fig.…”

Section: Double Emulsionmentioning

confidence: 99%

PLA micro- and nano-particles

Lee

Yun

Park

2016

Advanced Drug Delivery Reviews

273

177

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Poly(D,L-lactic acid) (PLA) has been widely used for various biomedical applications for its biodegradable, biocompatible, and nontoxic properties. Various methods, such as emulsion, salting out, and precipitation, have been used to make better PLA micro and nano-particle formulations. They are widely used as controlled drug delivery systems of therapeutic molecules, including proteins, genes, vaccines, and anti-cancer drugs. Even though PLA-based particles have challenges to overcome, such as low drug loading capacity, low encapsulation efficiency, and terminal sterilization, continuous innovations in particulate formulations will lead to development of clinically useful formulations.

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“…Although the studied polyesters are extensively used in drug carrier applications since they are biocompatible materials (Martín-Sabroso et al, 2015;Nanaki et al, 2017;Shen et al, 2011), in the present work their cytotoxicity was compared with Acacia mearnsii proanthocyanidins loaded PLGA microparticles.…”

Section: Cytotoxicity Of Plga and Plga/pac Microparticlesmentioning

confidence: 99%

SYNTHESIS, CHARACTERIZATION AND in vitro CYTOTOXICITY OF Acacia mearnsii PROANTHOCYANIDIN LOADED PLGA MICROPARTICLES

Grasel

Behrens

Strassburger

et al. 2019

Braz. J. Chem. Eng.

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One of the highlighted areas in the development of new materials is the generation of micro-and nanoparticles as drug carriers which allow the progress in formulations with the ability to release active agents in a controlled way. The proanthocyanidins (PAC) extracted from the bark of the Black Wattle have stood out for their biological activities. However, most polyflavonoids have some features which limit their application in the pharmaceutical field, such as light fastness, low bioavailability of active agents, and unpleasant taste. In this context, this study aims to present the synthesis and characterization of PAC-loaded lactic-co-glycolic acid (PLGA) microparticles obtained by the multiple emulsion method. The incorporation of PAC into PLGA was successfully achieved with PAC encapsulation efficiency around 73%. Spherical microparticles were obtained with a size distribution in the range of 0.6 to 2.4 μm. The presence of PAC modified the thermal properties of the PLGA matrix. The results of in vitro assays with Vero and T24 lineage celss showed that PLGA/PAC microparticles did not promote any effect on cell proliferation by MTT assay after 24 h. The novel Acacia mearnsii proanthocyanidin-loaded PLGA microparticles have potential for application in biological systems.

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Critical attributes of formulation and of elaboration process of PLGA-protein microparticles

Cited by 26 publications

References 33 publications

Initial Formation of the Skin Layer of PLGA Microparticles

Initial Formation of the Skin Layer of PLGA Microparticles

PLA micro- and nano-particles

SYNTHESIS, CHARACTERIZATION AND in vitro CYTOTOXICITY OF Acacia mearnsii PROANTHOCYANIDIN LOADED PLGA MICROPARTICLES

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