AAPS PHARMSCITECH
·
2022
·Vol. 23
·期 4
·1-10
·
IF 4.026
Liu Xia,Zhang Mengying,Tian Yuxin,Liu Ruijia,Wang Yunfei,Guo Feifei,Gong Yanling,Yan Meixing
Luteolin (Lu) is a kind of flavonoid that has been proved to treat non-alcoholic fatty liver disease by alleviating intestinal microbiota disorder. In this study, luteolin was coated with methoxy poly(ethylene glycol)–poly(dl-lactide-co-glycolic acid) (mPEG-PLGA) using an emulsion solvent evaporation method, and the optimum preparation process was determined by a single-factor experiment combined with response surface methodology (RSM). Methacrylic acid-methyl methacrylate (1:2) copolymer (Eudragit S100) was then used to coat the surface of Lu/mPEG-PLGA nanoparticles. The physical parameters of Eudragit S100-coated Lu/mPEG-PLGA nanoparticles (Lu-NPs), such as appearance, particle size, potential, particle size distribution and drug release, and stability in vitro, were evaluated. In addition, its cytotoxicity in vitro , pharmacokinetics, tissue distribution, and toxicity in vivo were also studied. The results showed that the prepared Lu-NPs had uniform particle size distribution, high encapsulation efficiency, and good stability. Normal colonic epithelial cells showed good tolerance to Lu-NPs. After oral administration, the blood concentration of luteolin peaked at 8 h, and the main tissue distribution was within the colon, confirming its colon-targeted profile. Safety assessments also indicated that no significant changes were observed in main organs after administration of Lu-NPs. The use of Eudragit S100-coated Lu/mPEG-PLGA nanoparticles is a new strategy for colon-targeted delivery of luteolin that encourages luteolin to fulfill its role in the colon. Graphical abstract
研究领域:
药学
·
纳米技术
·
药物递送系统
·
药理学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2024
·
IF 5.3
Qin Chen,Fen-Sheng Qiu,Wei Xie,Wen-Ying Yu,Zhao-An Su,Guang-Ming Qin,You-Kun Kang,Song-Lin Jiang,Chen-Huan Yu
Diabetic retinopathy (DR) is one of the chronic microvascular complications of type 2 diabetes mellitus (T2DM), which will cause retinal detachment and blindness without ideal therapies. Gypenoside A (GPA) are the main bioactive compound from Gynostemma pentaphyllum , and have various pharmacological effects. However, it suffered from poor bioavailability and potential cardiotoxicity in the clinical application. To overcome those limitations, in this study, nearly spherical nanoparticles (GPA-NP) with a mean particle size of 140.6 ± 22.4 nm were prepared by encapsulating GPA into mPEG-PLGA. This encapsulation efficiency was 84.4 ± 6.9 %, and the drug load was 4.02 %±0.35 %. The results showed that GPA-NP displayed more prolonged GPA release and higher bioavailability in vitro than GPA. GPA-NP obviously reduced the levels of oxidative stress markers and inflammatory cytokines in both retinal tissues of DR mice and high glucose-exposed HRMEC better than GPA alone. Mechanismly, GPA blocked the Nrf2-Keap1 interaction by binding with Kelch domain of Keap1 via alkyl and hydrogen bonds. Therefore, GPA-NP exerted more potent protectivity effects against high glucose-induced retinal microvascular endothelial ferroptosis in vitro and in vivo by activating Nrf2/HO-1/GPX4 pathway. It could be a promising therapeutic agent for preventing DR.
研究领域:
药理学
·
纳米技术
·
糖尿病
·
眼科学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
·
2019
·
IF 4.708
Shuang Li,Jiaxin Liu,Ge Li,Xueyan Zhang,Fei Xu,Zhijiang Fu,Lesheng Teng,Youxin Li,Fengying Sun
Parkinson’s disease (PD) is associated with symptoms such as tremor and bradykinesia which, together with a rigorous dosing regimen, can place an untenable burden on patients. These issues underscore the need for triggerable, modulated drug delivery systems . Currently, pramipexole (PRX) is the most widely used non-ergot dopamine agonist for the treatment of PD. In this study, near-infrared light-responsive PRX and hollow gold nanospheres (HGNS)-loaded biodegradable poly (D, L-lactide-co-glycolide) (PLGA) microspheres (PRX/HGNS MS) were fabricated using solid-in-oil-in-water (S/O/W) and water-in-oil-in-water (W/O/W) emulsion-solvent evaporation techniques to achieve modulated drug release. The PRX/HGNS MS were uniform, with an average diameter of approximately 24 µm, favorable PRX and HGNS encapsulation efficiencies (51.71 ± 0.54% and 65.15 ± 2.30%, respectively) and rapid, controllable drug release both in vitro and in vivo . Cytotoxicity tests revealed no significant differences between HGNS and PRX/HGNS MS when compared with a negative control. Pharmacodynamics and immunohistochemistry studies revealed a more rapid recovery of striatum in the group treated with PRX/HGNS MS produced using the S/O/W method. The results clearly demonstrate that light-responsive PRX/HGNS MS produced using the S/O/W method have the potential to address PD patients’ mobility problems in a smart, controllable and remotely triggerable manner.
研究领域:
神经学
·
药学
·
纳米技术
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
DRUG DELIVERY
·
2018
·
IF 3.095
Shengnuo Fan,Yuqiu Zheng,Xuan Liu,Wenli Fang,Xiaoyu Chen,Wang Liao,Xiuna Jing,Ming Lei,Enxiang Tao,Qiulan Ma,Xingmei Zhang,Rui Guo,Jun Liu
Alzheimer’s disease is a neurodegenerative disorder mainly characterized by β-amyloid deposit and tau hyperphosphorylation with no curative treatments. Curcumin (Cur) has been proved to have potential use in Alzheimer’s disease with its anti-amyloid, anti-inflammatory, and anti-oxidant properties, etc. However, its hydrophobicity and low bioavailability hinder its application. In this paper, we designed a novel brain-target nanoparticle, poly(lactide-co-glycolide)-block-poly(ethylene glycol) (PLGA-PEG) conjugated with B6 peptide and was loaded with Cur (PLGA-PEG-B6/Cur) and administered it into HT22 cells and APP/PS1 Al transgenic mice. The in vitro assays including dynamic light scattering (DLS), flow cytometry (FCM), red blood cell (RBC) lysis, and thromboelastography (TEG) analysis indicated that this nanoparticle could narrow the diameter of Cur, increase its cellular uptake and possess good blood compatibility. The results from Morris water maze proved that PLGA-PEG-B6/Cur could tremendously improve the spatial learning and memory capability of APP/PS1 mice, compared with native Cur. The ex vivo assays including Bielschowsky silver staining, immunostaining, and western blotting demonstrated that PLGA-PEG-B6/Cur could reduce hippocampal β-amyloid formation and deposit and tau hyperphosphorylation. Thus, we suggested that PLGA-PEG-B6/Cur nanoparticles would be of potential and promising use for the treatment of Alzheimer’s disease.
研究领域:
神经科学
·
药学
·
纳米技术
·
神经退行性疾病
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CELL AND TISSUE RESEARCH
·
2015
·Vol. 364
·期 1
·17-28
·
IF 3.565
Wen Yujun,Yu Shukui,Wu Yanhong,Ju Rongkai,Wang Hao,Liu Yujun,Wang Ying,Xu Qunyuan
In order to create an optimal microenvironment for neural regeneration in the lesion area after spinal cord injury (SCI), we fabricated a novel scaffold composed of a hyaluronic acid (HA) hydrogel with a longitudinal multi-tubular conformation. The scaffold was modified by binding with an anti-Nogo receptor antibody (antiNgR) and mixed further with poly(lactic-co-glycolic acid) (PLGA) microspheres containing brain-derived neurotrophic factor and vascular endothelial growth factor (HA+PLGA). In the rat, after implantation of this composite into an injured area created by a dorsal hemisection at T9-10 of the spinal cord, favorable effects were seen with regard to the promotion of spinal repair, including excellent integration of the implants with host tissue, inhibition of inflammation, and gliosis. In particular, large numbers of new blood vessels and regenerated nerve fibers were found within and around the implants. Simultaneously, the implanted rats exhibited improved locomotor recovery. Thus, this novel composite material might provide a suitable microenvironment for neural regeneration following SCI.
研究领域:
神经科学
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生物医学工程
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组织工程
·
再生医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2024
·
IF 10.5
Hezhi Wang,Ye Yuan,Lu Qin,Mengmeng Yue,Jingwen Xue,Zhixiang Cui,Xuanguang Zhan,Jiayi Gai,Xin Zhang,Jian Guan,Shirui Mao
Faced with the threat of lung cancer-related deaths worldwide, small interfering RNA (siRNA) can silence tumor related messenger RNA (mRNA) to tackle the issue of drug resistance with enhanced anti-tumor effects. However, how to increase lung tumor targeting and penetration with enhanced gene silencing are the issues to be addressed. Thus, the objective of this study is to explore the feasibility of designing non-viral siRNA vectors for enhanced lung tumor therapy via inhalation. Here, shell-core based polymer-lipid hybrid nanoparticles (HNPs) were prepared via microfluidics by coating PLGA on siRNA-loaded cationic liposomes (Lipoplexes). Transmission electron microscopy and energy dispersive spectroscopy study demonstrated that HNP consists of a PLGA shell and a lipid core. Atomic force microscopy study indicated that the rigidity of HNPs could be well tuned by changing thickness of the PLGA shell. The designed HNPs were muco-inert with increased stability in mucus and BALF, good safety, enhanced mucus penetration and cellular uptake. Crucially, HNP1 with the thinnest PLGA shell exhibited superior transfection efficiency (84.83%) in A549 cells, which was comparable to that of lipoplexes and Lipofectamine 2000, and its tumor permeability was 1.88 times that of lipoplexes in A549-3T3 tumor spheroids. After internalization of the HNPs, not only endosomal escape but also lysosomal exocytosis was observed. The transfection efficiency of HNP1 (39.33%) was 2.26 times that of lipoplexes in A549-3T3 tumor spheroids. Moreover, HNPs exhibited excellent stability during nebulization via soft mist inhaler. In conclusion, our study reveals the great potential of HNP1 in siRNA delivery for lung cancer therapy via inhalation.
研究领域:
药学
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纳米技术
·
癌症研究
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生物医学工程
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2021
·
IF 6.953
Wei Song,Yu Xiao
As generally accepted, inhibiting the bacterial invasion at initial stage and promoting the behavior of related osteogenesis cells afterwards is crucial to achieve favorable osteointegration after dental implantation. In this study, a novel combined structured hydrogel composed of chitosan and pore-closed poly(lactic- co -glycolic acid) microparticles was prepared and characterized. In vitro and in-vivo studies have identified that this biocompatible material can rapidly release vancomycin at initial 2 days and then sustainedly release recombinant human bone morphogenetic protein-2 for about 12 days, thus respectively accomplish antibacterial and osteogenesis functions. This sequential drug release system can be used as a promising coating material to improve the surface conditions of dental implant to enhance the osteointegration after surgery.
研究领域:
生物医学工程
·
药学
·
牙科种植学
·
组织工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Drug Design Development and Therapy
·
2022
·
IF 4.319
Yu Li,Zhan-Zhao Zhang
Background Excessive reactive oxygen species production caused by type 2 diabetes conditions can disrupt normal bone metabolism and greatly impair bone regeneration.Materials and methods In the present study, curcumin (Cur)-loaded microspheres were incorporated into a fish collagen nano-hydroxyapatite scaffold to promote bone repair under diabetic conditions by inhibiting the reactive oxygen species production.Results The drug release kinetic study showed that the Cur release from the composite scaffolds lasted up to 30 days. The sustained curcumin release from the scaffold significantly inhibited the overproduction of reactive oxygen species in mesenchymal stem cells caused by diabetic serum. Moreover, the Cur-loaded scaffold also remarkedly alleviated the negative effects of diabetic serum on the proliferation, migration, and osteogenic differentiation of mesenchymal stem cells. When implanted into bone defects in type 2 diabetic rats, the Cur-loaded scaffold also showed a greater bone formation capability compared to the pure scaffold.Conclusion The results of this study suggested that the novel controlled Cur release system may provide a promising route to improve bone regeneration in type 2 diabetic patients.
研究领域:
药理学
·
生物材料科学
·
组织工程
·
糖尿病研究
·
骨科
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2015
·
IF 3.65
Chenhui Wang,Changhui Yu,Jiaxin Liu,Lesheng Teng,Fengying Sun,Youxin Li
The goal of this research is to prepare poly(cyclohexane-1,4 diyl acetone dimethylene ketal) (PCADK)/poly( d , l -lactide-co-glycolide) (PLGA) blend microspheres loaded with recombinant human growth hormone (rhGH). The effect of PCADK degradation products on the structural integrity, secondary and tertiary structure and pharmacodynamics of rhGH was evaluated by native-polyacrylamide gel electrophoresis (Native-PAGE), size-exclusion high performance liquid chromatography (SEC-HPLC), circular dichroism (CD), fluorescence spectroscopy and in hypophysectomized rat models. Compared with PLGA degradation products, rhGH was found to be more stable in the presence of PCADK degradation products. PCADK/PLGA blend microspheres were then prepared and the morphology, encapsulation efficiency, release behavior and rhGH stability were investigated. PCADK/PLGA microspheres had regular shapes and smooth surfaces when the proportion of PCADK was less than 50%. The late-releasable amount of rhGH in PCADK/PLGA microspheres was greater than that in PLGA microspheres. In addition, the PCADK/PLGA microspheres showed larger AUC and improved therapeutic effects on rats than PLGA microspheres. Furthermore, the pH inside the microspheres was detected by CLSM to explain the improved rhGH stability in the PCADK/PLGA microspheres. In conclusion, PCADK/PLGA blend microspheres showed potential to improve rhGH stability and the efficacy of sustained-release of rhGH compared with PLGA microspheres.
研究领域:
药剂学
·
生物材料
·
药物递送系统
·
蛋白质稳定性
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF BIOMATERIALS APPLICATIONS
·
2022
·
IF 2.712
Shengtang Li,Xuewen Shi,Bo Xu,Jian Wang,Peng Li,Xin Wang,Jinpeng Lou,Ziyao Li,Chengwei Yang,Songkai Li,Ping Zhen
Currently, the treatment of osteomyelitis poses a great challenge to clinical orthopedics. The use of biodegradable materials combined with antibiotics provides a completely new option for the treatment of osteomyelitis. In this study, vancomycin hydrochloride (VANCO) loaded poly (lactic-co-glycolic acid) (PLGA) microspheres were prepared by a double emulsion solvent evaporation method, and the in vitro drug release behaviors of the drug loaded microspheres were explored after coating with different concentrations of silk fibroin (SF). Drug loading, encapsulation efficiency, Scanning electron microscopy, particle size analysis, Fourier transform infrared spectroscopy, hydrophilicity, in vitro drug release, and in vitro antibacterial activity were evaluated. The results showed that the drug loading of vancomycin loaded PLGA microspheres was (24.11 ±1.72)%, and the encapsulation efficiency was (48.21 ±3.44)%. The in vitro drug release indicated that the drug loaded microspheres showed an obvious initial burst release, and the drug loaded microspheres coated with SF could alleviate the initial burst release in varying degrees. It also can reduce the amount of cumulative drug release, and the effect of microspheres coated with 0.1% concentration of SF is the best. The time of in vitro drug release in different groups of drug loaded microspheres can be up to 28 days. The microspheres coated with (0.1%SF) or without (0%SF) SF showed a cumulative release of (82.50±3.51)% and (67.70±3.81)%,respectively. Therefore, the surface coating with SF of vancomycin loaded microspheres can alleviate the initial burst release, reduce the cumulative drug release, potentially prolong the drug action time, and improve the anti-infection effect.
研究领域:
药剂学
·
生物医学工程
·
材料科学
·
骨科
✓ 已验证
DOI
PubMed
高影响因子
RSC Advances
·
2018
·Vol. 8
·期 23
·12503-12516
·
IF 2.936
Ping Li,Bing Qi,Kun Li,Junwei Xu,Meili Liu,Xuenan Gu,Xufeng Niu,Yubo Fan
Besides the particle size and surface performance, the shape also plays a key role in drug delivery systems. Red blood cells are the most abundant blood cells in the human body, and are excellent oxygen carriers, due to their unique biconcave discoid shape. In this study, red blood cell (RBC)-like Fe3O4/TbLa3(Bim)12/poly(lactic-co-glycolic acid) (PLGA) composite particles, with magnetic response and bioimaging functions, were prepared by electrospraying. Various electrospraying parameters, such as solvent, PLGA concentration, collecting distance and solution flow rate were investigated in detail to attempt to obtain RBC-like composite particles. The size distribution, morphology, structure, and hydrophobicity–hydrophilicity of particles were characterized. The results revealed the RBC-like Fe3O4/TbLa3(Bim)12/PLGA composite particles exhibited a strong green fluorescence and good magnetic behavior even when incubated with cells. Furthermore, the intensity of the magnetization and fluorescence can be adjusted by changing the contents of Fe3O4 and TbLa3(Bim)12. The effect on cell viability of the RBC-like Fe3O4/TbLa3(Bim)12/PLGA composite particles was evaluated in A549 cells and RBCs, and it was determined to have low cytotoxicity and excellent blood biocompatibility, suggesting that it is a promising candidate for application in drug delivery, targeting and tracking.
研究领域:
材料科学
·
纳米技术
·
生物医学工程
·
药学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF NANOPARTICLE RESEARCH
·
2025
·Vol. 27
·期 4
·1-14
·
IF 2.6
Zhu Yuan,Lu Peiqi,Liao Youwu,Adu-Frimpong Michael,Zou Zhihui,Jin Zhou,Wang Chengwei,Peng Min,Peng Houping,Xu Jingze,Xu Ying,Yu Jiangnan,Xu Ximing
This study aimed to prepare core–shell structural PLGA nanoparticles of astaxanthin (ASTA-PLGA@M) via micelle template for sustained release in vitro and long-term hepatoprotective effects in vivo. The morphology, mean particle size, zeta potential, polydispersity index (PDI), and drug loading efficiency of optimized formulation were investigated. Meanwhile, the physicochemical characterizations including X-ray diffraction (XRD) and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) of ASTA-PLGA@M were evaluated to prove the successful encapsulation of astaxanthin. The in vitro release of astaxanthin from ASTA-PLGA@M in four different media was sustained slowly for 120 h. An in vivo release study also demonstrated that ASTA-PLGA@M nanoparticles enhanced oral bioavailability significantly. In addition, the hepatoprotective effects of astaxanthin on oxidative stress (OS) accompanied by apoptosis in acute hepatic damage caused by carbon tetrachloride (CCl 4 ) in mice were investigated. ASTA-PLGA@M nanoparticles provide a clear elevating effect on the activity of SOD and inhibit the increase of MDA during acute liver damage caused by CCl4. Moreover, histopathological analysis was conducted to study the long-term hepatoprotective effects of ASTA-PLGA@M for further application of astaxanthin in functional food or clinical use.
研究领域:
纳米医学
·
药剂学
·
药物递送
·
肝脏病学
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）