COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2025
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IF 5.4
Chujing Wang,Zengliu Song,Xinyue Ning,Yong Wang,Jie Xiao
Chitosan-coated nanostructured lipid carriers (CS-NLCs) were engineered to overcome the gastrointestinal instability and limited absorption of glycerol distearate (GDS)/medium-chain triglyceride (MCT)-based NLCs. Using a dropwise coating method, we systematically evaluated the impact of chitosan coating on digestive stability and intestinal permeability through in vitro digestion models, Ussing chamber assays, and confocal laser scanning microscopy (CLSM). The results indicate that Chitosan coating improved NLCs’ storage stability (except G2M8 formulation). CS-NLCs exhibited more complete digestion (the maximum fatty acid released within 20 minutes versus 30 minutes for uncoated NLCs), with Turbiscan analysis demonstrating an increase in initial digestion rate compared to uncoated NLCs, though chitosan-induced flocculation reduced small intestinal permeability (52% lower apparent permeability coefficient in Ussing chambers). CLSM imaging identified a critical solid lipid threshold (>50%) for chitosan-mediated adhesion enhancement, with 80% solid lipid CS-NLCs showing 1.6-fold higher mucus adhesion due to incomplete chitosan degradation and increased particle size (from 747 nm to 16μm). Pharmacokinetic studies in rats confirmed that CS-NLCs with >50% solid lipid achieved 1.8-fold higher curcumin bioavailability versus uncoated counterparts. This study highlights the critical role of chitosan coating in optimizing the bioavailability of lipid-based nutraceuticals in the gastrointestinal tract.
研究领域:
药剂学
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生物医学工程
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营养学
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产品关联
DOI
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2016
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IF 2.76
Wenhua Lv,Shuangni Zhao,Hui Yu,Na Li,Vasil M. Garamus,Yiyin Chen,Peihao Yin,Rongguang Zhang,Yabin Gong,Aihua Zou
This study was aimed at preparing a stable nanostructure lipid carriers for Brucea javanica oil (BJO/NLCs) using the high-pressure homogenization (HPH) method. The obtained BJO/NLCs exhibited a particle size of approximately 180 nm and were quite stable during 30 days of storage. The entrapment efficiency (EE) and drug loading (DL) of BJO/NLCs were good, with values of up to 99.2% and 10.4%, respectively. The polydispersity index (PDI) and zeta potential values of BJO/NLCs were 0.17 and −31.2 mV, respectively. BJO/NLCs exhibited spherical or elongated particles when viewed by transmission electron microscopy (TEM). Small-angle X-ray scattering (SAXS) further confirmed that the internal structures of blank NLCs and BJO/NLCs were arranged into lamellar phases. Anti-tumor activity was studied using the MTT assay; the BJO/NLCs showed improved cytotoxicity to A549 cells. Taken together, these results indicate that this newly designed BJO/NLCs delivery system has the potential to exhibit improved BJO bioavailability.
研究领域:
药剂学
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肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2025
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IF 5.2
Shulin Shen,Yanyan Zheng,Yueyue Xie,Xinzi You,Xuechao Chen,Binghui Xie,Jiaqi Weng,Qingqing Huo,Yunxiang Zhang,Meselhy R. Meselhy Zayed,Qinying Yan
Microneedle technology has emerged as a promising transdermal platform for transdermal delivery of Alzheimer’s disease therapeutics. However, conventional passive diffusion approaches face fundamental limitations in overcoming both skin and blood–brain barriers. To address these limitations, we developed a rocket-inspired gas-propelled microneedle system integrating nanostructured lipid carriers for enhanced dual-barrier penetration. The study combined fluid vortex generation with blood–brain barrier endothelial remodeling to achieve efficient drug delivery. Specifically, the system featured a hierarchical cavity design with borneol-modified huperzine A-loaded nanostructured lipid carriers (NLCs) (particle size: 89.6 ± 0.7 nm; zeta potential: –22.5 ± 0.5 mV; Hup A encapsulation efficiency: 83.40 ± 1.51 %; drug loading capacity: 2.63 ± 0.06 %) in primary cavities and a spatially isolated pneumatic initiator (ascorbic acid/sodium bicarbonate) in secondary cavities. Through multiphysics simulation coupled fluid dynamics with chemical reaction kinetics and mass transport phenomena, which revealed that acid-base reactions generate CO 2 microbubbles capable of producing rapid thrust forces. This microbubble-mediated propulsion mechanism achieved a 50 % increase in penetration depth (up to ∼ 1428 µm) relative to conventional microneedle platforms. Remarkably, this innovative hierarchical cavity design achieved a high drug loading capacity of 182 μg/array while preserving spatial isolation between the reactants and therapeutic payload. In vivo studies validated efficient brain delivery, as evidenced by a marked increase (p < 0.001) in cortical acetylcholine concentrations and amelioration of scopolamine-induced spatial memory impairments in rat models. This work established a preclinical proof-of-concept for the enhanced brain delivery of therapeutics in neurodegenerative disease through the synergistic integration of gas-propulsion physics and advanced nanocarrier engineering, offering new possibilities for overcoming biological delivery barriers.
研究领域:
药物递送系统
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神经药剂学
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生物医学工程
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纳米医学
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转化医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Tissue Engineering Part A
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2014
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IF 0
Shane Gao,Peng Zhao,Chao Lin,Yuxi Sun,Yilei Wang,Zhichong Zhou,Danjing Yang,Xianli Wang,Hongzhen Xu,Fei Zhou,Limei Cao,Wei Zhou,Ke Ning,Xu Chen,Jun Xu
Multipotent human adipose-derived stromal/stem cells (hADSCs) hold a great promise for cell-based therapy for many devastating human diseases, such as spinal cord injury and stroke. If exogenous hADSCs can be cultured in a three-dimensional (3D) scaffold with effective proliferation and differentiation capacity, it will better mimic the in vivo environment, which will have profound impact on the therapeutic application of hADSCs. In this study, a group of elastic-dominant, porous bioscaffolds from photocurable chitosan and gelatin were fabricated and proven to be biocompatible with both hADSCs and hADSC-derived neuron-like cells (hADSC-NLCs) in vitro. The identity of harvested hADSCs was confirmed by their positive immunostaining of mesenchymal stem cell surface markers, CD29, CD44, and CD105, and also positive expression of stem markers, Sox-2, Oct-4, c-Myc, Nanog, and Klf4. Their multipotency was further confirmed by trilineage differentiation of hADSCs toward adipocyte, osteoblast, and chondrocyte. It was found that hADSCs could be conditioned to differentiate into neurons in vitro as determined by immunostaining the markers of Tuj1, MAP2, NeuN, and Synapsin. The hADSCs and hADSC-NLCs were proven to be biocompatible with 3D scaffold, which actually facilitated the proliferation and differentiation of hADSCs in vitro, by MTT assay and their neuronal gene expression profiling. Moreover, hADSC-NLCs, which were mixed with 3D scaffold and transplanted into traumatic brain injury mouse model, survived in vivo and led to the better repair of the damaged brain area. The immunohistochemical studies revealed that 3D scaffold indeed improved the viability of transplanted cells, their ability to incorporate into the in vivo neural circuit, and their capacity for tissue repair. This study indicates that hADSCs would have great therapeutic application potential as seeding cells for in vivo transplantation to treat various neurological diseases when co-applied with porous chitosan/gelatin bioscaffolds.
研究领域:
再生医学
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干细胞研究
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组织工程
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神经科学
✓ 已验证
产品关联
DOI
PubMed
Materials Today Bio
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2026
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IF 11
Fudan Dong,Zhen Liang,Xiaping Yao,Zhen Zhang,Yuan Tao,Hui Chen,Ping Lu,Huiyun Xia,Junjie Zhang,Guojuan Pu,Tianyang Zhou
Fungal keratitis (FK) is a sight-threatening infection with poor outcomes due to rapid tear clearance and insufficient corneal penetration. To overcome the limitations, we developed an ion-activated mucoadhesive in-situ gelling system (TH-NLC-ISG) integrating terbinafine-loaded nanostructured lipid carrier (TH-NLC) into a gellan gum/carboxymethyl chitosan matrix. The optimized formulation exhibited a particle size of 25.27 ± 0.75 nm. Upon contact with simulated tear fluid, the formulation underwent rapid sol-gel transition, achieving a 70-fold viscosity increase (34 °C, shear rate 1 s −1 ), critical for prolonged ocular residence. Fluorescence imaging demonstrated ocular retention of fluorescein sodium-labeled TH-NLC-ISG exceeding 60 min, significantly longer than the non-gelling control. In vivo pharmacokinetic studies revealed markedly improved ocular bioavailability, with higher area under the concentration in ocular tissues-time curve of TH in the TH-NLC-ISG group compared to TH-NLC. Corneal penetration studies confirmed that TH-NLC-ISG exhibited longer corneal retention time and higher corneal drug retention compared to TH-NLC. The formulation demonstrated excellent ocular biocompatibility in vitro and in vivo . TH-NLC-ISG exhibited potent in vitro antifungal activity against Fusarium solani. and Aspergillus flavus. , with a lower MIC 50 value than TH suspension. In rabbits and mice FK models, TH-NLC-ISG group achieved complete corneal healing, reduced clinical scores and corneal perforation rates, displaying efficacy superior to conventional natamycin eye drops. By synergistically augmenting retention and corneal permeation, TH-NLC-ISG provides a transformative strategy for enhanced fungal keratitis therapy.
✓ 已验证
产品关联
DOI
高影响因子
Frontiers in Bioengineering and Biotechnology
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2022
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IF 6.064
Wang Hongbo,Li Jing,Jin Jianbo,Hu Jingbo,Yang Chunlin
Oxidative stress plays a key role in the progress of acute lung injury (ALI), which is an acute, progressive respiratory failure characterized by alveolar capillary injury caused by various external and internal factors other than cardiogenic factors. Pulmonary vascular endothelial cells are the main target cells during ALI, and therefore the mitochondrial targeting antioxidant derivative triphenylphosphine-melatonin (TPP-MLT) was encapsulated in VCAM-1 antibodies-conjugated nanostructured lipid carriers (VCAM@TPP-MLT NLCs) for lung targeting delivery. VCAM@TPP-MLT NLCs could be preferentially internalized by inflammatory endothelial cells in lung tissues, and then the released TPP-MLT from NLCs effectively eliminated the excessive reactive oxide species (ROS) and ameliorated cell apoptosis. Overall, the results suggested that VCAM@TPP-MLT NLCs exhibited remarkable in vitro and in vivo therapeutic effect on ALI, and could be a promising and efficient strategy for the treatment of ALI.
研究领域:
药理学
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呼吸医学
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纳米技术
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分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
LANGMUIR
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2014
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IF 4.384
Shuangni Zhao,Xiaomin Yang,Vasil M. Garamus,Ulrich A. Handge,Luthringer Bérengère,Lin Zhao,Gabriele Salamon,Regine Willumeit,Aihua Zou,Saijun Fan
The objective of the present work was to investigate the effects of the mixture of nonionic/ionic surfactants on nanostructured lipid carriers (NLCs). Nonionic surfactant (polyethylene–poly(propylene glycol), Pluronic F68) and ionic surfactant (octenylsuccinic acid modified gum arabic, GA-OSA) were chosen as emulsifier for NLCs. The NLCs systems, which were composed of lipid matrix, modified 4-dedimethylaminosancycline (CMT-8), and various emulsifier agents, were characterized with dynamic light scattering (DLS), high performance liquid chromatography (HPLC), transmission electron microscopy (TEM), small-angle X-ray scattering (SAXS), differential scanning calorimetry (DSC), in vitro release, and phagocytosis assay. This mixture of nonionic/ionic surfactants showed significant effects on physical properties including particle size, polydispersity index (PDI), entrapment efficiency, and particle morphology. Compared with single stabilizer, this mixed nonionic/ionic surfactant system provided NLCs with better drug carrier properties including prolonged release profile and low phagocytosis by phagocyte. We expect that these explorations can provide a new strategy for the development of lipid nanoparticles as drug delivery.
研究领域:
药剂学
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药物递送系统
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纳米技术
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材料科学
✓ 已验证
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
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2018
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IF 8.097
Tingxizi Liang,Zhigang Yao,Jie Ding,Qianhao Min,Liping Jiang,Jun-Jie Zhu
Tumor-specific therapeutic platforms with improved targeting efficacy and minimized side effect are crucial in cancer therapy. Capitalizing on the recognition capability and biocompatibility of aptamers, we herein designed a multistage targeted drug-delivery system using multiple biodegradable molecules-enveloped nanovehicle that can be employed to efficiently treat human epithelial growth factor receptor (HER2)-overexpressing breast cancer. In this nanovehicle, two aptamers respectively specific to HER2 and ATP were organized in a hierarchical manner. The outmost HER2 aptamer (HB5) governs the recognition to HER2 protein overexpressed in SK-BR-3 cell lines, while the ATP aptamer incorporated with anticancer drug (−)-epigallocatechin gallate (EGCG) and protamine sulfate in the inner core functions as a switch of drug release in response to abundant intracellular ATP. The targeting and drug locker aptamers were cascaded for active targeting effect and stimuli responsiveness, guaranteeing the site-specific drug transportation and endogenous species-triggered drug release inside the tumor cells. Moreover, nanostructured lipid carriers (NLCs) were constructed to wrap and stabilize the loosely bounded ternary complex, minimizing premature drug leakage potentially encountered by the biomolecule assembled nanocarriers. This multiple biomolecules-enveloped nanovehicle demonstrated improved inhibitory actions on tumor growth and minimum side effect to normal organs and tissues both in vitro and in vivo. The presented nanovehicle built from recognition and therapeutic components in a nontoxic framework offered a promising drug-delivery platform with transport precision and biological safety.
研究领域:
癌症研究
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药物递送系统
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纳米技术
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分子生物学
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生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）