INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2013
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IF 3.458
Xiaomin Yang,Lin Zhao,Laszlo Almasy,Vasil M. Garamus,Aihua Zou,Regine Willumeit,Saijun Fan
Chemically modified tetracyclines (CMTs) have been reported to strongly inhibit proliferation and metastasis of various cancers, but their efficacy is restricted by poor water solubility. In the present study, a hydrophilic 4-dedimethylamino sancycline (CMT-3) loaded nanostructured lipid carrier (CMT-3/NLC) was produced by high pressure homogenization (HPH). The physical properties of CMT-3/NLC formulations were characterized by dynamic light scattering (DLS), high efficiency liquid chromatography (HPLC), atomic force microscopy (AFM), scanning electron microscopy (SEM), small-angle neutron scattering (SANS), small-angle X-ray scattering (SAXS) and wide-angle X-ray powder diffraction (XRD). The lipid and surfactant ingredients, as well as drug/lipid concentrations (m/m) were optimized to produce stable and sustained NLC formulations. In vitro cytotoxicity of CMT-3/NLC against HeLa cells was evaluated by MTT assay. The diameter of CMT-3/NLC was found to increase from 153.1 ± 3.0 nm to a maximum of 168.5 ± 2.0 nm after 30 days of storage, while the entrapment efficiency remained constant at >90%. CMT-3/NLC demonstrated a burst-sustained release profile in release media with different pH, a property attributed to the 3-dimensional structure of CMT-3/NLC. Cell uptake and localization studies indicated that NLC reached the cytoplasm and could thereby facilitate CMT-3 entry into HeLa cells.
研究领域:
药剂学
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肿瘤学
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材料科学
✓ 已验证
DOI
PubMed
高影响因子
MOLECULAR CRYSTALS AND LIQUID CRYSTALS
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2014
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IF 0.491
Hengfeng Fan,Huafeng Zhou,Chaolong Ma,Yiqing Huang,Yan Li,Qiang Xia
The nanostructured lipid carrier (NLC) encapsulating two potent skin whitening ingredients was developed by our group for cosmetic and dermatological treatment. The particle showed spherical shape morphology under atomic force microscope, and the value of the zeta potential of the NLC was − 65.4 ± 4.3 mV. Good physical stability was observed by dynamic light scattering during 45 days’ storage, respectively. The skin whitening effect was improved when applying the NLC. Therefore, the NLC might be a potential delivery vehicle in dermal products.
研究领域:
化妆品学
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皮肤病学
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药学
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材料科学
✓ 已验证
产品关联
DOI
高影响因子
DRUG DELIVERY
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2021
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IF 6.419
Ya-Wen Zhang,Ling-Lan Tu,Yi Zhang,Jie-Chao Pan,Gao-Li Zheng,Li-Na Yin
Liver fibrosis is a major global health concern. Management of chronic liver disease is severely restricted in clinics due to ineffective treatment approaches. However, a lack of targeted therapy may aggravate this condition. Asiatic acid (AA), a pentacyclic triterpenoid acid, can effectively protect the liver from hepatic disorders. However, the pharmaceutical application of AA is limited by low oral bioavailability and poor targeting efficiency. This study synthesized a novel liver-targeting material from PEG-SA, chemically linked to ursodeoxycholic acid (UA), and utilized it to modify AA nanostructured lipid carriers (UP-AA-NLC) with enhanced targeting and improved efficacy. The formulation of UP-AA-NLC was optimized via the Box–Behnken Experimental Design (BBD) and characterized by size, zeta potential, TEM, DSC, and XRD. Furthermore, in vitro antifibrotic activity and proliferation of AA and NLCs were assessed in LX-2 cells. The addition of UP-AA-NLC significantly stimulated the TGF-beta1-induced expression of α-SMA, FN1, and Col I α1. In vivo near-infrared fluorescence imaging and distribution trials in rats demonstrated that UP-AA-NLC could significantly improve oral absorption and liver-targeting efficiency. Oral UP-AA-NLC greatly alleviated carbon tetrachloride-induced liver injury and fibrosis in rats in a dosage-dependent manner, as reflected by serum biochemical parameters (AST, ALT, and ALB), histopathological features (H&E and Masson staining), and antioxidant activity parameters (SOD and MDA). Also, treatment with UP-AA-NLC lowered liver hydroxyproline levels, demonstrating a reduction of collagen accumulation in the fibrotic liver. Collectively, optimized UP-AA-NLC has potential application prospects in liver-targeted therapy and holds great promise as a drug delivery system for treating liver diseases.
研究领域:
药理学
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肝病学
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药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Biomaterials Science & Engineering
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2020
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IF 4.152
Yibin Yu,Shuo Xu,Shihui Yu,Jinyu Li,Guoxin Tan,Sanming Li,Weisan Pan
We developed a hybrid nanostructured lipid carrier/dual pH- and thermo-sensitive hydrogel (NLC-Gel) for ocular delivery of quercetin (QN). The hydrogel consisted of carboxymethyl chitosan and poloxamer 407 (P407) was cross-linked using a naturally occurring cross-linker genipin (GP), while the hydrogel cross-linked using glutaraldehyde was used as a control. NLC loaded with quercetin/hydrogel cross-linked by a genipin hybrid drug delivery system (QN-NLC-Gel-GP) exhibited better cytocompatibility and lower ocular irritation than its glutaraldehyde counterpart. The levels of cellular uptake in NLC and NLC-Gel groups were improved. The results of fluorescence imaging and ex vivo transcorneal study indicated that NLC could facilitate transcorneal penetration of lipophilic molecules and incorporation into the hydrogel could increase the precorneal residence time of NLC. The area under the curve of quercetin in the NLC-Gel group was 4.4-fold that in the Eye drops group because of a longer precorneal retention time. In summary, the developed drug delivery system has enormous potential for ophthalmic applications.
研究领域:
药学
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材料科学
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眼科学
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药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Drug Delivery and Translational Research
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2023
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IF 5.4
Xu Hongjia,Hu Hao,Zhao Mengyuan,Shi Caihong,Zhang Xiangrong
This study investigated a nanostructured lipid carrier (NLC)-gel system containing luteolin (LUT), a potential drug delivery system for the treatment of psoriasis. LUT-NLC was prepared by solvent emulsification ultrasonication method. The particle size was 199.9 ± 2.6 nm, with the encapsulation efficiency of 99.81% and drug loading of 4.06%. X-ray diffractometry (XRD), Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) were used to characterize the LUT-NLC. The NLC was dispersed in Carbomer 940 to form the NLC based gel. The rheological characteristics of LUT-NLC-gel showed an excellent shear-thinning behavior (non-Newtonian properties) and coincided with the Herschel-Bulkley model. LUT-NLC-gel (78.89 μg/cm 2 ) exhibited better permeation properties and released over 36 hours than LUT gel (32.17 μg/cm 2 ). The dye-labeled LUT-NLC presented intense fluorescence in the epidermis and dermis by the visualization of fluorescence and confocal microscopy, and it could accumulate in the hair follicles. The effect of LUT-NLC-gel on imiquimod-induced psoriasis mice was evaluated by psoriasis area severity index scoring, spleen index assay, histopathology, and inflammatory cytokines. These results confirmed that LUT-NLC-gel with high dose (80 mg/kg/day) remarkably reduced the level of inflammatory and proliferation factors such as TNF-α, IL-6, IL-17, and IL-23 in both skin lesions and blood. LUT-NLC-gel improved the macroscopic features. Therefore, the LUT-NLC-gel had great potential as an effective delivery system for skin diseases. Graphical Abstract
研究领域:
药剂学
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皮肤科
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药物递送系统
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炎症研究
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）