JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2022
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IF 5.062
Han Qiao,Zhuo Xu,Mengchi Sun,Shuwen Fu,Fangxue Zhao,Danping Wang,Zhonggui He,Yinglei Zhai,Jin Sun
Dry eye disease (DED) is a public health concern that cause ocular discomfort and visual disturbance, which seriously affect quality of life. Rebamipide (RBM) is one of the drugs used for DED treatment, the ophthalmic RBM suspension (Mucosta®) has been used to treat DED in Japan. However, due to the drug removing through the nasolacrimal duct, the residence time of suspension on the ocular surface is short. RBM in excess of the therapeutic dose irritate the ocular surface and cause more tear production. Moreover, the opaque and turbid appearance of the suspension can lead to blurred vision after administration. In this study, we designed RBM liposomal eye drops for the treatment of DED, which have great stability, good patient compliance and a slow-release rate. RBM liposomes were prepared by remote loading technique and optimized for different formulation parameters. The appropriate HSPC-to-Chol ratio, drug-to-lipid ratio, calcium acetate solution concentration, incubation time and temperature were selected according to the encapsulation efficacy of RBM liposomes. The encapsulation efficacy and in vitro release of RBM were evaluated. The retention, tolerability and therapeutic effect of RBM liposomes were evaluated in rats. The ocular distribution of RBM was evaluated in vivo in rabbits’ eyes. The retention time of RBM liposomes in the cornea is longer than that of suspensions. While reducing the drug dose and irritation to ocular surface, RBM liposomes maintain the same efficacy and increase the concentration in cornea and aqueous humor. RBM liposomes suggested a further application in ophthalmic therapy, especially for DED.
研究领域:
药学
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眼科
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产品关联
DOI
高影响因子
Pharmaceutics
·
2025
·Vol. 17
·期 3
·332
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IF 5.5
Jiani Li,Panqin Ma,Shujia Guo,Danyi Qin,Yuqian Wang,Yuwen Liu,Zixuan Yang,Caihong Huang,Yi Han,Zuguo Liu
Background/Objectives:Blepharitis is a condition often caused byDemodex folliculoruminfestations, resulting in significant ocular discomfort and surface damage. Current treatments offer only temporary relief and fail to eliminate mites effectively. This study evaluates nano-niclosamide (nano-NCL), a lipophilic nanosuspension designed to enhance solubility and permeability, for targetingDemodex folliculorum.Methods:Nano-NCL was characterized by particle size, zeta potential, transmission electron microscopy, pH measurement, bacterial culture, and HPLC. Viable Demodex mites were collected from patients’ eyelashes and assigned to six treatment groups: DDW, F127, 0.15% nano-NCL, 0.3% nano-NCL, 20% TTO, and Okra. Mite survival was analyzed using Kaplan–Meier curves. The ocular surface safety was assessed via slit-lamp examination, corneal fluorescein staining, and in vivo confocal microscopy.Results:The nano-NCL particles are uniformly rod-shaped, approximately 291 nm in size, and exhibit good stability, remaining suspended in various media for up to 20 days. The formulation has a stable pH of 6 and demonstrated no bacterial growth, indicating sterility and suitability for clinical use. In vitro, both 0.15% (w/v) and 0.30% (w/v) nano-NCL significantly reduced Demodex survival, with mortality rates ranging from 70.6% to 92.3% within 2 h. Safety evaluations showed minimal corneal staining and inflammation. Notably, 0.15% nano-NCL displayed efficacy comparable to that of 20% tea tree oil (TTO) and Okra, which are established anti-Demodex treatments.Conclusions:Nano-NCL, particularly at 0.15%, rapidly eliminates mites while maintaining excellent ocular tolerability, making it a promising treatment for Demodex-related ocular surface diseases.
研究领域:
医学
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药理学
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眼科
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产品关联
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
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2022
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IF 16.744
Jingwen Yu,Yiming Wu,Qixuan Dai,Han Wu,Jintao Pan,Yuli Guo,Ke Yan,Huimin Zhu,Yi Mao,Sijie Lin,Wei Li,Gang Liu,Chengchao Chu
Corneal neovascularization (CNV) is one of the common blinding factors worldwide and how to treat CNV effectively is a knotty problem in clinical practice. Although, photothermal therapy (PTT) has been widely investigated in CNV management, it is still limited by the effective delivery of photothermal agents. Hereby, we proposed and validated an in vivo assembly drug delivery strategy, which composed of vascular targeting molecule (RGD-Bis(DPA-Zn), DRUG-1) and ultra-small nanoparticles (AuPt-ICG, DRUG-2). DRUG-2, with PTT and photoacoustic imaging (PAI) properties, could be co-assembled with DRUG-1 to form larger DRUG-1@2 nanocluster, accompanied by performance gains. To treat CNV, DRUG-1 was topically administrated via eye drops; and trapped at the target by the in situ co-assembled with DRUG-1, during which the dual-PAI system was applied to trace drug enrichment; finally, a safe NIR irradiation strategy was implemented to realize efficient CNV elimination. Moreover, the DRUG-1/2 -combined treatment demonstrated better biosecurity and broke new ground for CNV theranostics.
研究领域:
眼科
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纳米医学
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生物材料
✓ 已验证
产品关联
DOI
高影响因子
LANGMUIR
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2025
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IF 3.9
Hongdong Wang,Zhen Luo,Kunpeng Wang,Yuhong Liu,Jianhua Zhang
Ocular lubrication is a critical component of the biological lubrication system. Factors such as tear film instability and corneal epithelial damage can lead to increased friction on the ocular surface during blinking, which negatively impacts quality of life and results in economic burden. Eye drops are commonly used therapeutic purposes. Due to the frequent movement (blinking, tear secretion, nasolacrimal drainage), their bioavailability is low, requiring frequent applications. In this study, methacylated gellan gum (GGMA) hydrogels were synthesized using methacrylic anhydride and low-acyl gellan gum as raw materials. The elastic modulus of GGMA hydrogel increased nearly threefold after introduction of alkali metal ions. Macroscopic superlubricity was achieved in friction experiments simulating the ocular environment. At a contact pressure close to 10 kPa, the COF was reduced to 0.004. Detailed friction experiments and sophisticated simulations revealed the underlying mechanism, showing that the superlubricity of GGMA hydrogel is attributed to the hydration properties of alkali metal ions adsorbed onto the hydrogel surface. The GGMA hydrogel exhibits excellent lubricating properties, offering promising potential for enhancing ocular lubrication and supporting eye health.
研究领域:
生物材料学
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眼科医学
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摩擦学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
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2019
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IF 8.456
Sen Lin,Chaoxiang Ge,Doudou Wang,Qi Xie,Biao Wu,Jingjie Wang,Kaihui Nan,Qinxiang Zheng,Wei Chen
The sealed anatomical features of the eye and its physiological activity that rapidly removes drugs are called anatomical and physiological barriers, which are the cause of more than 90% of drug loss. This aspect remains a critical issue in eye surface medication. Thus, promoting tissue permeability of drugs as well as prolonging their retention on the eye surface can improve their bioavailability and enhance their therapeutic effects. Thanks to the existence of a negatively charged mucin layer on the eye surface, several peptide-decorated polymeric micelles were prepared to enhance the interaction between the micelle and eye surface, thus prolonging the drug retention on the eye surface and promoting its tissue permeability. Tacrolimus (also known as FK506) is a hydrophobic macrolide immunosuppressant used to treat dry eye syndrome and other eye diseases. However, its hydrophobic nature makes its delivery as a topical eye surface medication difficult, with the risk of side effects due to overdoses. Therefore, the aim of this work is to evaluate the ability of FK506 micelles in promoting their permeability on the eye surface. Our results showed that the positively charged nanomicelles could significantly prolong FK506 retention on the eye surface and enhance its corneal permeability in ex vivo and in vivo conditions. FK506 nanomicelles exhibited superior curing effects against dry eye diseases than the FK506 suspension and a commercial FK506 formula. It exerted better inhibitory effects on eye surface inflammation and corneal epithelium apoptosis when examined by a slip lamp and a transferase-mediated dUTP nick end labeling assay, respectively. Further assays revealed the higher suppressive effects on the expression of several inflammation-related factors at an mRNA and protein level. Hence, our results suggested that these positively charged nanomicelles might be a good drug delivery system for ocular surface medication.
研究领域:
药剂学
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眼科医学
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生物材料
✓ 已验证
DOI
PubMed
高影响因子
BMC Ophthalmology
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2018
·Vol. 18
·期 1
·1-11
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IF 1.77
Li Shanshan,He Jiangnan,Chen Qiuying,Zhu Jianfeng,Zou Haidong,Xu Xun
Background Our study aimed to investigate the ocular surface health of Shanghai University students. Methods This is a cross-sectional study carried out among freshmen and sophomores on the main campus of Shanghai University. Questionnaires including the widely-used ocular surface disease index (OSDI) and the Zung Self-rating Anxiety Scale (SAS) were completed first, and then ocular examinations were conducted regarding height & weight, blood pressure and heart rate, optometry, intraocular pressure exam, vision and subjective refraction, Aladdin, Macular pigment density measurement, tear test, anterior segment examination, fundus photography, ophthalmologist check, TOPCON OCT check, and Collin’s fundus blood test. Results Totally 901 students were involved in our five-day study. The prevalence of myopia was 92% (the spherical equivalent refraction (SER) < − 0.50 D), and that of high myopia was 23% (SER < − 6.0D). The prevalence of dry eye disease (DED) was 10%. The corneal epithelial loss rate (corneal fluorescein staining > 1) was 10%, and corneal sensation decline rate (≤ 30 mm) was 12%. 4.5% of subjects ( n = 40) had moderate or severe anxiety, 78% were mild and a small portion (17.5%) didn’t have anxiety at all. No statistical significant association was found between anxiety with DED, fluorescein staining or with corneal sensation (all p > 0.05). However, subjects with DED had more symptoms of anxiety. Results also showed that students who kept eye strain for a long time were more inclined to have DED (12.5%: 6.9%, p = 0.0407, 95% CI); those who watched mobile phones and/or computers for over eight hours daily were more vulnerable to DED and fluorescein staining than others (14.1%: 8.6%, p = 0.0129; 13.0%: 8.3%, p = 0.0233, 95% CI). Conclusions Keeping eye strain or near work for a long time is associated with DED, while students with DED tend to encounter anxiety symptoms. The prevalence of myopia in Chinese university students is still high. We consider it necessary to provide education to university students about the good eye-using habits, and to diagnose anxiety for student patients with DED.
研究领域:
眼科学
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公共卫生
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流行病学
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视觉科学
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心理卫生
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屈光医学
✓ 已验证
DOI
高影响因子
Science Advances
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2025
·Vol. 11
·期 30
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IF 12.5
Mei Yang,Xin Chen,Zhongxing Chen,Nan Zhao,Zhenhai Zeng,Xiaomin Huang,Zheng Li,Jiawei Li,Guoli Zhao,Manli Deng,Zhilin Zou,Hongxian Pan,Aodong Chen,Tingting Chen,Yue Wu,Xueyu Fu,Qimanguli Saiding,Na Kong,Wei Tao,Xingtao Zhou,Jinhai Huang
Oxidative stress, an imbalance between the body’s oxidative and antioxidant systems, contributes markedly to the development of numerous ocular surface diseases, particularly dry eye disease (DED). Effective elimination or reduction of reactive oxygen species (ROS) can halt disease progression and alleviate symptoms. This study presents an innovative thermoresponsive, metal-free carbon nanodot (CD) hydrogel, termed F-CD hydrogel, which exhibits potent neutralization capabilities against multiple free radicals, including OH·, O 2 − ·, and ·DPPH. This hydrogel demonstrates remarkable antioxidant, anti-inflammatory, and antiapoptotic capacity, effectively relieving DED symptoms by eliminating ROS at their source. Furthermore, its thermosensitive characteristics enhance the adherence of CDs to the ocular surface. In mouse models of DED, the F-CD hydrogel accelerates epithelial repair, thickens the corneal epithelium, promotes tear secretion, and boosts goblet cell count by up-regulating protective genes while suppressing those promoting apoptosis and oxidative stress. Coupled with its excellent biocompatibility and reduced administration frequency and treatment duration, the F-CD hydrogel emerges as a promising therapeutic approach for DED.
研究领域:
眼科学
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纳米医学
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生物材料
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药剂学
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分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Science Advances
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2025
·Vol. 11
·期 10
·
IF 12.5
Chuhan Wang,Xiaobing Liu,Wenyan Lv,Xiao Kuang,Feng Wu,Xianqun Fan,Yan Pang
Topical drug delivery on ocular surface always suffers from frequent administration and low bioavailability due to short drug residence. Despite advances of different adhesive ophthalmic drugs in extending release, cornea and eyelid nonselective adhesion inevitably causes ocular discomfort and even damage. Here, we describe in situ formation of an adhesive lubricative Janus nanocoating (ALJN) to enable long-lasting comfort drug delivery. By iron complexation, an asymmetric ALJN is formed on ocular surface via facile sequential instillation. The adhesive polyphenol inner layer binding with ocular surface enables drug loading and sustained release, while the lubricative zwitterionic polymer outer layer prevents eyelid adhesion to ensure comfort. Following instillation, ALJN retains on ocular surface over 24 hours and reduces blinking frequency to normal level. Moreover, ALJN demonstrates remarkable therapeutic potential in mouse and rabbit models of corneal contusion and alkali burn. This work proposes a comfortable long-lasting topical delivery platform for treating various ocular diseases.
研究领域:
眼科
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药剂学
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纳米技术
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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
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2023
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IF 8.2
Jia Liu,Yingni Xu,Yongrui Huang,Xiaomin Sun,Yuehai Peng,Wenjing Song,Jin Yuan,Li Ren
Corneal alkali burn is one of the most devastating ophthalmic emergencies correlated with remarkable morbidity resulting in severe visual impairment. Appropriate intervention in the acute phase determines the eventual outcome for later corneal restoration treatment. Since the epithelium plays an essential role in inhibiting inflammation and promoting tissue repair, sustained anti-matrix metalloproteinases (MMPs) and pro-epithelialization are the prior remedies during the first week. In this study, a drug-loaded collagen membrane (Dox-HCM/Col) that could be sutured to overlay the burned cornea was developed to accelerate the early reconstruction. Doxycycline (Dox), a specific inhibitor of MMPs, was encapsulated in collagen membrane (Col) through hydroxypropyl chitosan microspheres (HCM) to develop Dox-HCM/Col, affording a preferable pro-epithelialization microenvironment and an in-situ controlled release. Results showed that loading HCM into Col prolonged the release time to 7 days, and Dox-HCM/Col could significantly suppress the expression of MMP-9 and -13 in vitro and in vivo . Furthermore, the membrane accelerated the corneal complete re-epithelialization and promoted early reconstruction within the first week. Overall, Dox-HCM/Col was a promising biomaterial membrane for treating alkali-burned cornea in the early stage, and our attempt may provide a clinically feasible method for the ocular surface reconstruction.
研究领域:
眼科
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生物材料
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组织工程
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药学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
AAPS PHARMSCITECH
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2024
·Vol. 25
·期 5
·1-15
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IF 3.4
Hao Tianjiao,Tang Lu,Xu Qianzi,Wang Wei,Li Zengjing,Shen Yan,Xu Bohui,Luo Hao,Li Qian,Wang Jirong,Zhang Jinling
Purpose Dry eye syndrome (DES), arising from various etiologic factors, leads to tear film instability and ocular surface damage. Given its anti-inflammatory effects, cyclosporine A (CsA) has been widely used as a short-term treatment option for DES. However, poor bioavailability and solubility of CsA in aqueous phase make the development of a cyclosporine A-based eye drop for ocular topical application a huge challenge. Methods In this study, a novel strategy for preparing cyclosporine A-loaded silk fibroin nanoemulsion gel (CsA NBGs) was proposed to address these barriers. Additionally, the rheological properties, ocular irritation potential, tear elimination kinetics, and pharmacodynamics based on a rabbit dry eye model were investigated for the prepared CsA NBGs. Furthermore, the transcorneal mechanism across the ocular barrier was also investigated. Results The pharmacodynamics and pharmacokinetics of CsA NBGs exhibited superior performance compared to cyclosporine eye drops, leading to a significant enhancement in the bioavailability of CsA NBGs. Furthermore, our investigation into the transcorneal mechanism of CsA NBGs revealed their ability to be absorbed by corneal epithelial cells via the paracellular pathway. Conclusion The CsA NBG formulation exhibits promising potential for intraocular drug delivery, enabling safe, effective, and controlled administration of hydrophobic drugs into the eye. Moreover, it enhances drug retention within the ocular tissues and improves systemic bioavailability, thereby demonstrating significant clinical translational prospects.
研究领域:
药学
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眼科
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药物递送系统
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生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Drug Delivery and Translational Research
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2024
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IF 5.7
Wang Yanan,Shi Shaohua,Zhang Ling,Wang Songtao,Qin Hongqing,Wei Yanjun,Wu Xianggen,Zhang Mengmeng
Imatinib (IMB) is a type of tyrosine kinase inhibitor with great application potential for inhibiting corneal neovascularization (CNV), but its poor water solubility limits its application in eye disease treatment. In this study, novel IMB@glycymicelles entrapped in hydrogel (called IMB@glycymicelle-hydrogel) were prepared, characterized, and evaluated for their therapeutic effects on corneal alkali burn in mice. Imatinib could be successfully loaded in glycymicelles using glycyrrhizin as a nanocarrier with an optimized weight ratio of IMB:nanocarrier. The apparent solubility of IMB was significantly improved from 61.69 ± 5.55 μg/mL to bare IMB to 359,967.62 ± 20,059.42 μg/mL to IMB@glycymicelles. Then, the IMB@glycymicelles were entrapped in hydrogel fabricated with hydroxypropyl methylcellulose and sodium hyaluronate (HA) to prolong retention time on the ocular surface. Rabbit eye tolerance tests showed that IMB@glycymicelle-hydrogel possessed good ocular safety profiles. In a mouse model of corneal alkali burns, the topical administration of IMB@glycymicelle-hydrogel showed strong efficacy by prompting corneal wound healing, recovering corneal sensitivity, relieving corneal opacities, and inhibiting CNV, and these efficacy evaluation parameters were better than those of the positive drug HA. Overall, these results demonstrated that IMB@glycymicelle-hydrogel may be a promising candidate for the effective treatment of alkali ocular damage. Graphical abstract
研究领域:
药学
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眼科
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药物递送系统
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纳米技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF CONTROLLED RELEASE
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2024
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IF 10.5
Yan Dai,Jiali Zhang,Shimeng Zhang,Linhua Li,Chao Qu,Jiang Chen,Lei Lu
Bacterial keratitis is a major cause of blindness, hindered by the rising threat of antibiotic resistance. Although corneal bandage lenses (CBLs) are widely utilized in ophthalmic treatment, their effectiveness in treating bacterial keratitis remains limited due to risks of secondary infections, patient discomfort, and complications. In this study, we developed a novel biomimetic coating on CBLs by grafting Ag/Cu bimetallic nanoparticles (Ag/Cu-NPs) and thiol-functionalized heparin (Hep-SH) using a rapid polydopamine (PDA) deposition technique, effectively mimicking the ocular surface glycocalyx structure. The resulting Ag/Cu-NPs/Hep-SH coated CBLs (PNH-CBLs) exhibited significant antibacterial activity, with over 80 % reduction in Staphylococcus aureus ( S. aureus ) and 70 % in Escherichia coli ( E. coli ) due to the sustained release of Ag + and Cu 2+ , along with displaying favorable in vitro biocompatibility. Animal experiments conducted on New Zealand white rabbits with bacterial keratitis demonstrated successful treatment therapeutic outcomes, with PNH-CBLs leading to a significant decrease in clinical score. These biomimetic lenses also exhibited selective anti-protein adsorption properties, minimizing inflammation and promoting surface lubrication. Overall, this innovative approach addresses critical challenges in antibiotic resistance and offers a promising therapeutic strategy for managing ophthalmic infectious diseases.
研究领域:
眼科学
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纳米技术
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生物材料
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抗菌治疗
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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）