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coumarin-6
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS · 2017 · IF 4.159

Transport mechanism of chitosan-N-acetylcysteine, chitosan oligosaccharides or carboxymethyl chitosan decorated coumarin-6 loaded nanostructured lipid carriers across the rabbit ocular

Jinyu Li,Guoxin Tan,Bingchao Cheng,Dandan Liu,Weisan Pan

To facilitate the hydrophobic drugs modeled by coumarin-6 (Cou-6) acrossing the cornea to the anterior chamber of the rabbit eye, chitosan (CS) derivatives including chitosan-N-acetyl- l -cysteine (CS-NAC), chitosan oligosaccharides (COS) and carboxymethyl chitosan (CMCS) modified nanostructured lipid carriers (NLCs) were designed and characterized. We found that, with similar size distribution and positive   charges, different CS derivatives based on NLCs led to distinctive delivery performance. In vivo precorneal retention study on rabbits revealed that these CS derivatives coating exhibited a stronger resistant effect than Cou-6 eye drops and Cou-6-NLC (P   <   0.05), moreover, the AUC (0−∞) , C max and MRT (0−∞) of them followed the sequence of CMCS-Cou-6-NLC   <   COS-Cou-6-NLC   <   CS-NAC-Cou-6-NLC. Confocal laser fluorescence microscopy (CLSM) for in vitro corneal penetration study showed that COS-, and CS-NAC-coated NLCs penetrated through the whole corneal epithelium barrier (about 40   μm), while CMCS failed to significantly enhance the intraocular drug penetration as expected, displayed a negligible fluorescence at 30   μm deep. In addition, penetration through the intact cornea was achieved and the penetration levels through the ocular tissues were increased thoroughly for the COS and CS-NAC coating ones compared with CMCS-NLC (P   <   0.05), and successfully reduced the conjunctival-to-corneal permeability ratio (ratio (C - S/C) ) thus resulted in a higher bioavailability, which was confirmed by ex vivo fluorescence imaging on ocular tissues. In summary, CS-NAC-NLC and COS-NLC are promising ocular drug delivery systems to achieve prolonged precorneal retention, higher corneal permeability and enhanced ocular bioavailability. And comparatively speaking, CS-NAC-NLC possesses the highest potential for ocular drug delivery.

CAS / MDL: 38215-36-0
研究领域: 药剂学 · 眼科研究
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CARBOHYDRATE POLYMERS · 2018 · IF 5.158

Fabrication of folic acid decorated reductive-responsive starch-based microcapsules for targeted drug delivery via sonochemical method

Yuexin Sun,Chao Shi,Jiebing Yang,Shuangling Zhong,Zhanfeng Li,Lifeng Xu,Shengnan Zhao,Yan Gao,Xuejun Cui

In this present study, original, biodegradable, biocompatible, non-immunogenic and non-poisonous folic acid (FA) decorated reductive-responsive starch-based microcapsules (FA-RSMCs) were designed and fabricated via the sonochemical method for targeted delivery and controlled release of hydrophobic drugs. A green hydrophobic fluorescent dye, Coumarin 6 (C6), was encapsulated into the FA-RSMCs as a substitute of hydrophobic drugs. The as-synthesized C6-loaded FA-RSMCs were characterized by DLS, SEM and TEM. The results indicated that the obtained C6-loaded FA-RSMCs had an appropriate size range and could enter into the bloodstream with their splendid stability. Moreover, C6-loaded FA-RSMCs showed a high selectivity to Hela cells, and a brilliant targeted drugs delivery and reductive-responsive release ability for hydrophobic drugs, particularly for hydrophobic anti-cancer drugs.

CAS / MDL: 52-90-4 25952-53-8
研究领域: 药学 · 生物材料科学 · 纳米医学
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY · 2023 · IF 4.4

Fluorescent composite based on peptide nanotubes activating coumarin 6 for sensitive detection of new coccine in food samples

Fang Li,Rong Tang,Yujie Kang,Xiaoyan Cui,Ya Wang,Xiupei Yang

New coccine (NC), as a kind of common colorant, has been frequently used in our daily life. Herein, the fluorescent composite (PNTs@C6) prepared by the hydrophobic non-covalent interaction between peptide nanotubes and coumarin 6 (C6) was designed for the determination of NC. Due to the activation of C6 by peptide nanotubes, the composite exhibits strong green fluorescence emission, which can be selectively quenched by NC through the inner filter effect. Therefore, a new fluorescent method based on the PNTs@C6 composite for NC detection was constructed. Under optimal conditions, the fluorescence quenching of the sensor exhibits a good linear relationship with the concentration of NC in the range of 0.01–10 μM and the limit of detection is 3.6 nM. Furthermore, the strategy shows simplicity, rapid response and high selectivity and has been successfully applied to the detection of NC in food samples.

研究领域: 分析化学 · 食品科学 · 纳米技术 · 光谱学
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SENSORS AND ACTUATORS B-CHEMICAL · 2021 · IF 7.46

A novel insight into fluorescent sensor for patulin detection using thiol-terminated liposomes with encapsulated coumarin-6 as signal probe

Dongxia Nie,Dakai Guo,Qingwen Huang,Wenbo Guo,Jianhua Wang,Zhihui Zhao,Zheng Han

Nanocomposites of thiol-terminated liposomes encapsulating with coumarin-6 ( [email protected] ) were successfully prepared via a simple thin-film dispersion method to construct a novel fluorescent sensor for selectively detecting trace amounts of patulin. Thiol group ( SH) was designed not only as a specific recognition element to capture patulin, but also as a convenient linker for the further separation of patulin-derivatized and un-derivatized [email protected] by combination with magnetic NH 2 [email protected] 3 O 4 nanoparticles. Liposomes primarily provided an effective platform with a large surface area for facilitated accommodation of large amounts of recognition element ( SH group) and fluorophore (coumarin-6). In such an assay protocol, a reliable link was established between the changes in fluorescent intensity (ΔF) from the nanocomposites of [email protected] /NH 2 [email protected] 3 O 4 and the concentrations of patulin in the range of 0.05–20 ng mL −1 , with the correlation coefficient of 0.996. This approach also effectively eliminated the background interference from other mycotoxins and metal ions. Under the optimal conditions, the designed sensor displayed excellent performance for patulin analysis, with an extremely low detection limit (0.033 ng mL −1 ), high recovery (96.2–107.6 %) and excellent selectivity. Furthermore, the feasibility of its applications has also been demonstrated in the analysis of real juice samples, providing a novel tactics for rational design of a fluorescence assay, for point-of-care diagnostics of patulin, with great potential to be extended to other hazardous compounds by substitution of the recognition elements.

研究领域: 分析化学 · 纳米技术 · 食品安全 · 生物技术
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MOLECULAR PHARMACEUTICS · 2017 · IF 4.44

Ex Vivo and in Vivo Evaluation of the Effect of Coating a Coumarin-6-Labeled Nanostructured Lipid Carrier with Chitosan-N-acetylcysteine on Rabbit Ocular Distribution

Dandan Liu,Jinyu Li,Bingchao Cheng,Qingyin Wu,Hao Pan

This study is focused on further understanding the characteristics of chitosan-N-acetylcysteine surface-modified nanostructured lipid carriers (CS-NAC-NLCs) in their interaction with ocular mucosa. Coumarin-6 (C6)-labeled NLCs, including uncoated NLCs, chitosan hydrochloride (CH)-, and CS-NAC-coated NLCs, were developed using a melt-emulsification technique and subsequently decorated with different types or portions of chitosan derivatives. Mucoadhesion was evaluated ex vivo using a flow-through process with fluorescence detection. The results demonstrated that the presence of CS-NAC on the C6-NLC surface provided the most obvious enhancement in adhesion due to the formation of both noncovalent (ionic) and covalent (disulfide bridges) interactions with mucus chains. Meanwhile, the concentration of CS-NAC in the formulation positively influenced the viscosity of the nanoparticles and hence prolonged their retention in the ocular tissue. Transcorneal penetration studies revealed that CS-NAC-NLC particles were able to penetrate through the entire corneal epithelium primarily via a transcellular route. The transport depth and velocity strongly relied on the modification material and the particle size. Ex vivo fluorescence imaging and in vivo ocular distribution investigations showed that C6 was broadly distributed in rabbit eye tissues and absorbed by aqueous humor after CS-NAC-NLC instillation. In relation to C6 eye drops, CS-NAC-NLCs achieved considerably higher Cmax (4.01-fold), MRT0-∞ (1.87-fold), and AUC0-∞ (16.29-fold) in the aqueous humor. Moreover, the increase in drug absorption was greater in the cornea than in the conjunctiva. Thereby, it is possible to draw a conclusion that CS-NAC-NLCs presented great potential for drug application to the front portion of the eye.

CAS / MDL: 38215-36-0
研究领域: 药剂学 · 眼科研究 · 生物医学工程
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