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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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Eye and Vision · 2021 ·Vol. 8 ·期 1 ·22 · IF 3.257

Lens thickness and associated ocular biometric factors among cataract patients in Shanghai

Meng Jiaqi,Wei Ling,He Wenwen,Qi Jiao,Lu Yi,Zhu Xiangjia

Background To evaluate the distribution of lens thickness (LT) and its associations with other ocular biometric factors among cataract patients in Shanghai. Methods Twenty-four thousand thirteen eyes from 24,013 cataract patients were retrospectively included. Ocular biometric factors including LT, central corneal thickness (CCT), anterior chamber depth (ACD), white-to-white (WTW) distance, anterior corneal curvature, and axial length (AL) were obtained using the IOLMaster700. The associations between LT and general or ocular factors were assessed. Results The mean age was 62.5 ± 13.6 years and 56.1% were female. The mean LT was 4.51 ± 0.46 mm. The LT was greater in older patients ( P  < 0.001). LT was positively correlated with CCT, while negatively correlated with ACD, WTW, and anterior corneal curvature ( P  < 0.001). Multivariate analysis revealed that increased LT was associated with older age, male gender, thicker CCT, shallower ACD, larger WTW, and flatter anterior corneal curvature ( P  < 0.001). LT changed with a variable behavior according to AL. In short eyes LT increased as AL increased, then decreased with longer AL in normal eyes and moderate myopic eyes, but increased again as AL increased in highly myopic eyes. Thickest LT was found in the 20.01–22 mm AL group. The correlation between LT and other biometric factors remained significant when stratified by ALs. Conclusions In a large Chinese cataractous population, we found that the thicker lens may be associated with older age, male gender, thicker CCT, shallower ACD, larger WTW, and flatter anterior corneal curvature. As AL increased, the change of LT was nonlinear, with the thickest lens seen in the 20–22 mm AL group.

研究领域: 眼科 · 生物医学工程 · 临床眼科学 · 屈光手术 · 白内障研究
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Eye and Vision · 2023 ·Vol. 10 ·期 1 ·1-14 · IF 4.2

Comprehensive comparisons of ocular biometry: A network-based big data analysis

Yu Jinjin,Wen Daizong,Zhao Jing,Wang Yiran,Feng Ke,Wan Ting,Savini Giacomo,McAlinden Colm,Lin Xuanqiao,Niu Lingling,Chen Sisi,Gao Qingyi,Ning Rui,Jin Yili,Zhou Xingtao,Huang Jinhai

Purpose To systematically compare and rank ocular measurements with optical and ultrasound biometers based on big data. Methods PubMed, Embase, the Cochrane Library and the US trial registry ( www.ClinicalTrial.gov ) were used to systematically search trials published up to October 22nd, 2020. We included comparative studies reporting the following parameters measured by at least two devices: axial length (AL), flattest meridian keratometry (Kf), steepest meridian keratometry (Ks), mean keratometry (Km), astigmatism (AST), astigmatism vectors J 0 and J 45 , anterior chamber depth (ACD), aqueous depth (AQD), central corneal thickness (CCT), corneal diameter (CD) and lens thickness (LT). A network-based big data analysis was conducted using STATA version 13.1. Results Across 129 studies involving 17,181 eyes, 12 optical biometers and two ultrasound biometers (with both contact and immersion techniques) were identified. A network meta-analysis for AL and ACD measurements found that statistically significant differences existed when contact ultrasound biometry was compared with the optical biometers. There were no statistically significant differences among the four swept-source optical coherence tomography (SS-OCT) based devices (IOLMaster 700, OA-2000, Argos and ANTERION). As for Ks, Km and CD, statistically significant differences were found when the Pentacam AXL was compared with the IOLMaster and IOLMaster 500. There were statistically significant differences for CCT when the OA-2000 was compared to Pentacam AXL, IOLMaster 700, Lenstar, AL-Scan and Galilei G6. Conclusion For AL and ACD, contact ultrasound biometry obtains the lower values compared with optical biometers. The Pentacam AXL achieves the lowest values for keratometry and CD. The smallest value for CCT measurement is found with the OA-2000.

研究领域: 眼科 · 生物医学工程 · 临床研究 · 循证医学 · 视觉科学
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International Journal of Nanomedicine · 2017 · IF 4.3

A novel ion-exchange carrier based upon liposome-encapsulated montmorillonite for ophthalmic delivery of betaxolol hydrochloride

Yi Huang,Qi Tao,Dongzhi Hou,Sheng Hu,Shuangyan Tian,Yanzhong Chen,Ruyi Gui,Lingling Yang,Yao Wang

As a novel ion-exchange carrier with high surface area and excellent exchangeability, montmorillonite (Mt) was intercalated with betaxolol hydrochloride (BH) to form a nanocomposite and then encapsulated by liposomes (Mt-BH-LPs) for an ophthalmic drug-delivery system. The Mt-BH and Mt-BH-LPs were prepared by an acidification process and ethanol injection combined with ammonium sulfate gradient methods. The successful formation of Mt-BH and Mt-BH-LPs was verified by thermogravimetric analysis, X-ray diffraction, Fourier-transform infrared spectra, and transmission electron microscopy. Mt-BH-LPs possessed the favorable physical characteristics of encapsulation efficiency, drug loading, mean particle size, and ζ-potential. In vitro release studies indicated Mt-BH-LPs effectively maintained a relatively sustained slow release. Immortalized human corneal epithelial cell cytotoxicity, in vivo rabbit eye-irritation tests, and chorioallantoic membrane–trypan blue staining all revealed that Mt-BH-LPs had no obvious irritation on ocular tissues. A new in vitro tear-turnover model, including inserts containing human corneal epithelial cells, was designed to evaluate the precorneal retention time of Mt-BH-LPs. The results showed that Mt-BH-LPs maintained a certain BH concentration in tear fluid for a longer period than the BH solution. In vivo precorneal retention studies also indicated Mt-BH-LPs prolonged drug retention on the ocular surface more than the BH solution. Furthermore, pharmacodynamic studies showed that Mt-BH-LPs had a prolonged effect on decreasing intraocular optical pressure in rabbits. Our results demonstrated that Mt-BH-LPs have potential as an ophthalmic delivery system.

CAS / MDL: 59937-28-9
研究领域: 药剂学 · 纳米技术 · 眼科学 · 药物递送系统
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CARBOHYDRATE POLYMERS · 2021 · IF 9.381

γ-Cyclodextrin-based polypseudorotaxane hydrogels for ophthalmic delivery of flurbiprofen to treat anterior uveitis

Guihua Fang,Qiuxiang Wang,Xuewen Yang,Yu Qian,Guowei Zhang,Bo Tang

Anterior uveitis is a sight-threatening inflammation inside the eyes. Conventional eye drops for anti-inflammatory therapy need to be administered frequently owing to the rapid elimination and corneal barrier. To address these issues, polypseudorotaxane hydrogels were developed by mixing Soluplus micelles (99.4 nm) and cyclodextrins solution. The optimized hydrogels exhibited shear-thinning and sustained release properties. The hydrogels exhibited higher transcorneal permeability coefficient (P app , 1.84 folds) than that of drug solutions. Moreover, animal study indicated that the hydrogels significantly increased the precorneal retention (AUC, 21.2 folds) and intraocular bioavailability of flurbiprofen (AUC Aqueous humor , 17.8 folds) in comparison with drug solutions. Importantly, the hydrogels obviously boosted anti-inflammatory efficacy in rabbit model of endotoxin-induced uveitis at a reduced administration frequency. Additionally, the safety of hydrogels was confirmed by cytotoxicity and ocular irritation studies. In all, the present study demonstrates a friendly non-invasive strategy based on γ- CD-based polypseudorotaxane hydrogels for ocular drug delivery.

CAS / MDL: 81-88-9
研究领域: 药学 · 眼科 · 药物递送系统 · 炎症研究
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