Quantitative three-dimensional analysis of poly (lactic-co-glycolic acid) microsphere using hard X-ray nano-tomography revealed correlation between structural parameters and drug burst release

Xiao-zhou, Huang; Li, Na; Wang, Dajiang; Luo, Yunjun; Zhang, Wu; Guo, Zhefei; Jin, Quan; Liu, Zhuying; Huang, Yafei; Zhang, Yongming; Wu, Chuanbin

doi:10.1016/j.jpba.2015.04.017

Cited by 13 publications

(4 citation statements)

References 29 publications

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“…In this study, PCL microspheres containing the 8HQ corrosion inhibitor were successfully prepared using an O/W emulsion solvent evaporation technique . According to previous studies, the method was expected to produce a homogeneous distribution of the hydrophobic 8HQ inhibitor within the hydrophobic PCL microspheres. , Dichloromethane was chosen as the organic phase of the O/W emulsion because of its low boiling point (40 °C), which is beneficial for the solidification of the microspheres. The size of the microspheres decreased with increased stirring speed and with increasing stirring time.…”

Section: Results and Discussionmentioning

confidence: 99%

Triple-Action Self-Healing Protective Coatings Based on Shape Memory Polymers Containing Dual-Function Microspheres

Huang

Deng

et al. 2018

ACS Appl. Mater. Interfaces

176

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In this study, a new self-healing shape memory polymer (SMP) coating was prepared to protect the aluminum alloy 2024-T3 from corrosion by the incorporation of dual-function microspheres containing polycaprolactone and the corrosion inhibitor 8-hydroxyquinoline (8HQ). The self-healing properties of the coatings were investigated via scanning electron microscopy, electrochemical impedance spectroscopy, and scanning electrochemical microscopy following the application of different healing conditions. The results demonstrated that the coating possessed a triple-action self-healing ability enabled by the cooperation of the 8HQ inhibitor, the SMP coating matrix, and the melted microspheres. The coating released 8HQ in a pH-dependent fashion and immediately suppressed corrosion within the coating scratch. After heat treatment, the scratched coating exhibited excellent recovery of its anticorrosion performance, which was attributed to the simultaneous initiation of scratch closure by the shape memory effect of the coating matrix, sealing of the scratch by the melted microspheres, and the synergistic effect of corrosion inhibition by 8HQ.

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Section: Results and Discussionmentioning

confidence: 99%

Triple-Action Self-Healing Protective Coatings Based on Shape Memory Polymers Containing Dual-Function Microspheres

Huang

Deng

et al. 2018

ACS Appl. Mater. Interfaces

176

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“…Given the characteristics of the preparation method (S/O/W) and that the final process included filtration and washing, it is logical to assume that only a minimal amount of drug would be present on the surface and outermost layer of the MSs. Huang et al (Huang 2015) used hard X-ray nano-tomography to study the microstructure and porosity of PLGA MSs prepared with the W/O/W method. They observed a high porosity (19.27 ± 3.42%) in MSs measuring 2.35 ± 0.26 μm, which correlated well with "surface protein interconnectivity" and suggested that the initial explosive release at 5-10 h (burst effect) may be the result of rapid drug diffusion through what these authors refer to as interconnected pores.…”

Section: Discussionmentioning

confidence: 99%

Optimising the controlled release of dexamethasone from a new generation of PLGA-based microspheres intended for intravitreal administration

Villanueva

Bravo‐Osuna

Herrero-Vanrell

et al. 2016

European Journal of Pharmaceutical Sciences

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Successful therapy for chronic diseases affecting the posterior segment of the eye requires sustained drug concentrations at the site of action for extended periods of time. To achieve this, it is necessary to use high systemic doses or frequent intraocular injections, both associated with serious adverse effects. In order to avoid these complications and improve patient's quality of life, an experimental study has been conducted on the preparation of a new generation of biodegradable poly(D,L-lactide-co-glycolide) (50:50) (PLGA) polymer microspheres (MSs) loaded with Dxm, vitamin E and/or human serum albumin (HSA). Particles were prepared according to a S/O/W encapsulation method and the 20-40μm fraction was selected. This narrow size distribution is suitable for minimally invasive intravitreal injection by small calibre needles. Characterisation of the MSs showed high Dxm loading and encapsulation efficiency (> 90%) without a strong interaction with the polymer matrix, as revealed by DSC analysis. MSs drug release studies indicated a small burst effect (lower than 5%) during the first five hours and subsequently, drug release was sustained for at least 30days, led by diffusion and erosion mechanisms. Dxm release rate was modulated when solid state HSA was incorporated into MSs formulation. SDS-PAGE analysis showed that the protein maintained its integrity during the encapsulation process, as well as for the release study. MSs presented good tolerance and lack of cytotoxicity in macrophages and HeLa cultured cells. After 12months of storage under standard refrigerated conditions (4±1°C), MSs retained appropriate physical and chemical properties and analogous drug release kinetics. Therefore, we conclude that these microspheres are promising pharmaceutical systems for intraocular administration, allowing controlled release of the drug.

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“…Simultaneously, there have been studies on the structure of microspheres. Wang 44 and Huang 45 et al investigated the relationship between void structure and drug encapsulation efficiency of poly (lactic-acid-glycolic acid) (PLGA) microspheres encapsulating bovine serum albumin and the correlation between microsphere structure and drug release using hard X-ray nanotomography in 2014 and 2015, respectively. The results of the investigation pointed out that the smaller the internal pores of the microspheres, the higher the protein loading.…”

Section: Study Of Pellets and Microsphere Preparationmentioning

confidence: 99%

Advances in Structure Pharmaceutics from Discovery to Evaluation and Design

Xue

et al. 2023

Mol. Pharmaceutics

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Drug delivery systems (DDSs) play an important role in delivering active pharmaceutical ingredients (APIs) to targeted sites with a predesigned release pattern. The chemical and biological properties of APIs and excipients have been extensively studied for their contribution to DDS quality and effectiveness; however, the structural characteristics of DDSs have not been adequately explored. Structure pharmaceutics involves the study of the structure of DDSs, especially the three-dimensional (3D) structures, and its interaction with the physiological and pathological structure of organisms, possibly influencing their release kinetics and targeting abilities. A systematic overview of the structures of a variety of dosage forms, such as tablets, granules, pellets, microspheres, powders, and nanoparticles, is presented. Moreover, the influence of structures on the release and targeting capability of DDSs has also been discussed, especially the in vitro and in vivo release correlation and the structure-based organ- and tumor-targeting capabilities of particles with different structures. Additionally, an in-depth discussion is provided regarding the application of structural strategies in the DDSs design and evaluation. Furthermore, some of the most frequently used characterization techniques in structure pharmaceutics are briefly described along with their potential future applications.

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Quantitative three-dimensional analysis of poly (lactic-co-glycolic acid) microsphere using hard X-ray nano-tomography revealed correlation between structural parameters and drug burst release

Cited by 13 publications

References 29 publications

Triple-Action Self-Healing Protective Coatings Based on Shape Memory Polymers Containing Dual-Function Microspheres

Triple-Action Self-Healing Protective Coatings Based on Shape Memory Polymers Containing Dual-Function Microspheres

Optimising the controlled release of dexamethasone from a new generation of PLGA-based microspheres intended for intravitreal administration

Advances in Structure Pharmaceutics from Discovery to Evaluation and Design

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