Preparation, optimization, characterization and in vitro release of baicalein-solubilizing glycyrrhizic acid nano-micelles

You, Guangjiao; Feng, Tao; Zhang, Guoqin; Chen, Mei‐Ling; Liu, Fan; Sun, Lili; Wang, Meng; Ren, Xiaoliang

doi:10.1016/j.ijpharm.2021.120546

Cited by 40 publications

(18 citation statements)

References 26 publications

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“…BCL, one of the main ingredients of Scutellariae radix , has been clinically used to limit inflammation and is relevant to a wide array of cells related to the healing processes of bone fractures . Additionally, BCL has been shown to protect against MSC apoptosis through antioxidation, antiapoptosis, and anti-inflammatory mechanisms . Therefore, BCL has great potential in the prevention and treatment of bone remodeling conditions, including fractures and osteoporosis. , However, owing to its low aqueous solubility, its bioavailability is poor, which extensively restricts the bioactivity and clinical use of BCL …”

Section: Discussionmentioning

confidence: 99%

Dual-Targeted Nanoplatform Regulating the Bone Immune Microenvironment Enhances Fracture Healing

Zhou

Lin

Xiong

et al. 2021

ACS Appl. Mater. Interfaces

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The immune system and skeletal system are closely linked. Macrophages are one of the most important immune cells for bone remodeling, playing a prohealing role mainly through M2 phenotype polarization. Baicalein (5,6,7-trihydroxyflavone, BCL) has been well documented to have a noticeable promotion effect on M2 macrophage polarization. However, due to the limitations in targeted delivery to macrophages and the toxic effect on other organs, BCL has rarely been used in the treatment of bone fractures. In this study, we developed mesoporous silica and Fe3O4 composite-targeted nanoparticles loaded with BCL (BCL@MMSNPs-SS-CD-NW), which could be magnetically delivered to the fracture site. This induced macrophage recruitment in a targeted manner, polarizing them toward the M2 phenotype, which was demonstrated to induce mesenchymal stem cells (MSCs) toward osteoblastic differentiation. The mesoporous silicon nanoparticles (MSNs) were prepared with surface sulfhydrylation and amination modification, and the mesoporous channels were blocked with β-cyclodextrin. The outer layer of the mesoporous silicon was added with an amantane-modified NW-targeting peptide to obtain the targeted nanosystem. After entering macrophages, BCL could be released from nanoparticles since the disulfide linker could be cleaved by intracellular glutathione (GSH), resulting in the removal of cyclodextrin (CD) gatekeeper, which is a key element in the pro-bone-remodeling functions such as anti-inflammation and induction of M2 macrophage polarization to facilitate osteogenic differentiation. This nanosystem passively accumulated in the fracture site, promoting osteogenic differentiation activities, highlighting a potent therapeutic benefit with high biosafety.

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Section: Discussionmentioning

confidence: 99%

Dual-Targeted Nanoplatform Regulating the Bone Immune Microenvironment Enhances Fracture Healing

Zhou

Lin

Xiong

et al. 2021

ACS Appl. Mater. Interfaces

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show abstract

“…BCL, one of the main ingredients of Scutellariae radix, has been clinically used to limit in ammation and is relevant to a wide array of cells related to the healing processes of bone fractures [36]. Additionally, BCL has been shown to protect against MSC apoptosis through anti-oxidation, anti-apoptosis and antiin ammatory mechanisms [37]. Therefore, BCL has great potential in the prevention and treatment of bone remodeling conditions, including fractures and osteoporosis [38,39].…”

Section: Discussionmentioning

confidence: 99%

Magnetically-Targeted Nanoparticle-Guided M2 Macrophage Polarization For Fracture Healing Promotion

Zhou

Lin

Xiong

et al. 2021

Preprint

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Background: Macrophages are essential for fracture healing, acting mainly through remodeling of the extracellular matrix and promotion of angiogenesis. The role of macrophages in regulating osteogenic differentiation, particularly that of the M2 phenotype, is increasingly researched. Baicalein (BCL) had also been shown to have pro-fracture-healing effects.Results: In this study, we developed mesoporous silica and Fe3O4 composite-targeted nanoparticles loaded with BCL (BCL@MMSNPs-SS-CD-NW), that could be magnetically delivered to the fracture site. These induced macrophage recruitment in a targeted manner, polarizing them towards the M2 phenotype, and thereby inducing MSCs towards osteoblastic differentiation. The mesoporous silicon nanoparticles (MSNs) were prepared with surface sulfhydrylation and amination modification, and the mesoporous channels were blocked with β-cyclodextrin. The outer layer of the mesoporous silicon was added with an amantane-modified NW targeting peptide to obtain the targeted nano-system. After entering macrophages, BCL could be released from nanoparticles since the disulfide linker could be cleaved by intracellular glutathione (GSH) resulting in the removing of CD gatekeeper, which is a key element in the pro-bone-remodeling functions, such as anti-inflammation and induction of M2 macrophage polarization to facilitate osteogenic differentiation.Conclusions: This nano-system passively accumulated in the fracture site, promoting osteogenic differentiation activities, highlighting a potent therapeutic benefit with high biosafety.

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“…Moreover, the absorption peak at 1408 cm −1 can be attributed to the bending stretching of -CH 2 [41], at 1150 cm −1 were assigned to the symmetric stretching of C-O-C bond, and at 1028 cm −1 were assigned to the C-O stretching vibrations [42][43][44]. In addition, the C=O stretching vibrations of GA can also be observed at 2943 cm −1 [45]. With the introduction of ZnO/PAL nanorods (2.5 wt.% or 5.0 wt.%) into the CG film, the peak at 1408 cm −1 shifted to 1402 cm −1 , and the peak at 1028 cm −1 shifted to 1021 cm −1 , indicating the interaction of CS, GA and ZnO/PAL nanorods.…”

Section: Characterizations Of Cg and Cgzp Filmsmentioning

confidence: 94%

Synergistic Effect of Glycyrrhizic Acid and ZnO/Palygorskite on Improving Chitosan-Based Films and Their Potential Application in Wound Healing

Zhang

Hui

et al. 2021

Polymers

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The synergistic effect of chitosan (CS), glycyrrhizic acid (GA) and ZnO/palygorskite (ZnO/PAL) as potential wound dressing was evaluated in the form of films by the solution casting method. The nanocomposite films were well-characterized with ATR-FTIR, XRD and SEM to explore the interactions between CS, GA and ZnO/PAL. Physical, mechanical and antibacterial properties of the nanocomposite films were systematically investigated for their reliability in end-up utilization. Importantly, it was found that the presence of PAL in the films provided enhanced mechanical properties, whereas CS, GA and ZnO supplied a broad-spectrum antibacterial activity, especially for drug-resistant bacteria such as ESBL—E. coli and MRSA. Overall, this research demonstrated that the prepared films can be a promising candidate for wound-care materials.

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Preparation, optimization, characterization and in vitro release of baicalein-solubilizing glycyrrhizic acid nano-micelles

Cited by 40 publications

References 26 publications

Dual-Targeted Nanoplatform Regulating the Bone Immune Microenvironment Enhances Fracture Healing

Dual-Targeted Nanoplatform Regulating the Bone Immune Microenvironment Enhances Fracture Healing

Magnetically-Targeted Nanoparticle-Guided M2 Macrophage Polarization For Fracture Healing Promotion

Synergistic Effect of Glycyrrhizic Acid and ZnO/Palygorskite on Improving Chitosan-Based Films and Their Potential Application in Wound Healing

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