• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

聚乙烯吡咯烷酮K90和泊洛沙姆407自组装纳米胶束的研发与评价：青蒿素眼部局部递送的增强作用

Development and Evaluation of Polyvinylpyrrolidone K90 and Poloxamer 407 Self-Assembled Nanomicelles: Enhanced Topical Ocular Delivery of Artemisinin.

作者信息

Ponnusamy Chandrasekar, Sugumaran Abimanyu, Krishnaswami Venkateshwaran, Palanichamy Rajaguru, Velayutham Ravichandiran, Natesan Subramanian

机构信息

Department of Pharmaceutical Technology, University College of Engineering, Bharathidasan Institute of Technology Campus, Anna University, Tiruchirappalli 620024, Tamil Nadu, India.

Department of Pharmaceutics, SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur 603203, Tamil Nadu, India.

出版信息

Polymers (Basel). 2021 Sep 8;13(18):3038. doi: 10.3390/polym13183038.

DOI:10.3390/polym13183038
PMID:34577939
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8470191/
Abstract

Age-related macular degeneration is a multifactorial disease affecting the posterior segment of the eye and is characterized by aberrant nascent blood vessels that leak blood and fluid. It ends with vision loss. In the present study, artemisinin which is poorly water-soluble and has potent anti-angiogenic and anti-inflammatory properties was formulated into nanomicelles and characterized for its ocular application and anti-angiogenic activity using a CAM assay. Artemisinin-loaded nanomicelles were prepared by varying the concentrations of PVP k90 and poloxamer 407 at different ratios and showed spherical shape particles in the size range of 41-51 nm. The transparency and cloud point of the developed artemisinin-loaded nanomicelles was found to be 99-94% and 68-70 °C, respectively. The in vitro release of artemisinin from the nanomicelles was found to be 96.0-99.0% within 8 h. The trans-corneal permeation studies exhibited a 1.717-2.169 µg permeation of the artemisinin from nanomicelles through the excised rabbit eye cornea for 2 h. Drug-free nanomicelles did not exhibit noticeable DNA damage and showed an acceptable level of hemolytic potential. Artemisinin-loaded nanomicelles exhibited remarkable anti-angiogenic activity compared to artemisinin suspension. Hence, the formulated artemisinin-loaded nanomicelles might have the potential for the treatment of AMD.

摘要

年龄相关性黄斑变性是一种影响眼球后段的多因素疾病，其特征是新生血管异常，会渗漏血液和液体，最终导致视力丧失。在本研究中，将水溶性差但具有强大抗血管生成和抗炎特性的青蒿素制成纳米胶束，并使用鸡胚绒毛尿囊膜（CAM）试验对其眼部应用和抗血管生成活性进行表征。通过以不同比例改变聚乙烯吡咯烷酮k90（PVP k90）和泊洛沙姆407的浓度来制备负载青蒿素的纳米胶束，其呈现出球形颗粒，粒径范围为41 - 51纳米。所制备的负载青蒿素的纳米胶束的透明度和浊点分别为99 - 94%和68 - 70℃。发现青蒿素从纳米胶束中的体外释放率在8小时内为96.0 - 99.0%。经角膜渗透研究表明，在2小时内，负载青蒿素的纳米胶束中有1.717 - 2.169微克的青蒿素透过离体兔眼角膜。不含药物的纳米胶束未表现出明显的DNA损伤，且溶血潜力处于可接受水平。与青蒿素悬浮液相比，负载青蒿素的纳米胶束表现出显著的抗血管生成活性。因此，所制备的负载青蒿素的纳米胶束可能具有治疗年龄相关性黄斑变性的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/32d9fd0346ba/polymers-13-03038-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/8ef3c3956646/polymers-13-03038-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/877a333ca6c7/polymers-13-03038-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/fb3f94c4c635/polymers-13-03038-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/7d01582f6bcf/polymers-13-03038-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/2414f49b6cc3/polymers-13-03038-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/5ca4216e20fb/polymers-13-03038-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/8674d8829b04/polymers-13-03038-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/ab08907270da/polymers-13-03038-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/3269c66d8dd8/polymers-13-03038-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/798d927f72ba/polymers-13-03038-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/32d9fd0346ba/polymers-13-03038-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/8ef3c3956646/polymers-13-03038-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/877a333ca6c7/polymers-13-03038-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/fb3f94c4c635/polymers-13-03038-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/7d01582f6bcf/polymers-13-03038-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/2414f49b6cc3/polymers-13-03038-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/5ca4216e20fb/polymers-13-03038-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/8674d8829b04/polymers-13-03038-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/ab08907270da/polymers-13-03038-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/3269c66d8dd8/polymers-13-03038-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/798d927f72ba/polymers-13-03038-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd95/8470191/32d9fd0346ba/polymers-13-03038-g011.jpg

相似文献

1
Development and Evaluation of Polyvinylpyrrolidone K90 and Poloxamer 407 Self-Assembled Nanomicelles: Enhanced Topical Ocular Delivery of Artemisinin.聚乙烯吡咯烷酮K90和泊洛沙姆407自组装纳米胶束的研发与评价：青蒿素眼部局部递送的增强作用
Polymers (Basel). 2021 Sep 8;13(18):3038. doi: 10.3390/polym13183038.
2
Design and development of artemisinin and dexamethasone loaded topical nanodispersion for the effective treatment of age-related macular degeneration.设计和开发青蒿素和地塞米松负载的局部纳米分散体，用于有效治疗年龄相关性黄斑变性。
IET Nanobiotechnol. 2019 Oct;13(8):868-874. doi: 10.1049/iet-nbt.2019.0130.
3
A grafted copolymer-based nanomicelles for topical ocular delivery of everolimus: Formulation, characterization, ex-vivo permeation, in-vitro ocular toxicity, and stability study.一种用于局部眼部递送依维莫司的基于接枝共聚物的纳米胶束：制剂、表征、离体渗透、体外眼毒性及稳定性研究。
Eur J Pharm Sci. 2021 Apr 1;159:105735. doi: 10.1016/j.ejps.2021.105735. Epub 2021 Jan 28.
4
Development of Bromfenac Sodium Loaded Pluronic Nanomicelles: Characterization and Corneal Permeation Study.溴芬酸钠载聚氧乙烯醚纳米胶束的研制：表征及角膜渗透研究。
Recent Adv Drug Deliv Formul. 2022;16(1):68-78. doi: 10.2174/2667387816666220128123737.
5
Development and evaluation of dexamethasone nanomicelles with potential for treating posterior uveitis after topical application.局部应用后具有治疗后葡萄膜炎潜力的地塞米松纳米胶束的研发与评估。
J Ocul Pharmacol Ther. 2015 May;31(4):215-27. doi: 10.1089/jop.2014.0152. Epub 2015 Apr 3.
6
Topical Formulation of Self-Assembled Antiviral Prodrug Nanomicelles for Targeted Retinal Delivery.用于靶向视网膜递送的自组装抗病毒前药纳米胶束的局部制剂。
Mol Pharm. 2017 Jun 5;14(6):2056-2069. doi: 10.1021/acs.molpharmaceut.7b00128. Epub 2017 May 17.
7
Aqueous nanomicellar formulation for topical delivery of biotinylated lipid prodrug of acyclovir: formulation development and ocular biocompatibility.用于阿昔洛韦生物素化脂质前药经皮递药的水基胶束制剂：制剂开发和眼部生物相容性。
J Ocul Pharmacol Ther. 2014 Feb;30(1):49-58. doi: 10.1089/jop.2013.0157. Epub 2013 Nov 5.
8
Mucoadhesive phenylboronic acid conjugated chitosan oligosaccharide-vitamin E copolymer for topical ocular delivery of voriconazole: Synthesis, in vitro/vivo evaluation, and mechanism.基于硼酸的黏附性壳聚糖寡糖-维生素 E 共聚体作为伏立康唑局部眼用给药系统的研究：合成、体外/体内评价及作用机制。
Acta Biomater. 2022 Jan 15;138:193-207. doi: 10.1016/j.actbio.2021.10.047. Epub 2021 Oct 30.
9
Combination of self-assembling system and N,O-carboxymethyl chitosan improves ocular residence of anti-glaucoma drug.自组装系统与 N,O-羧甲基壳聚糖的联合应用提高了抗青光眼药物的眼部滞留时间。
Eur J Pharm Biopharm. 2024 Apr;197:114208. doi: 10.1016/j.ejpb.2024.114208. Epub 2024 Feb 7.
10
Topical, Aqueous, Clear Cyclosporine Formulation Design for Anterior and Posterior Ocular Delivery.用于眼前段和眼后段给药的局部用、水性、透明环孢素制剂设计
Transl Vis Sci Technol. 2015 May 1;4(3):1. doi: 10.1167/tvst.4.3.1. eCollection 2015 May.

引用本文的文献

1
Comparative Study of Dexamethasone-Loaded Thermoresponsive In Situ Gels and Polymeric Micelles for Ocular Drug Delivery.载地塞米松的热敏原位凝胶和聚合物胶束用于眼部给药的比较研究。
Int J Mol Sci. 2025 Aug 29;26(17):8414. doi: 10.3390/ijms26178414.
2
Development and Evaluation of Cyclosporine a Mixed Micelle Eye Drops for Enhanced Ocular Drug Delivery.用于增强眼部药物递送的环孢素A混合胶束滴眼液的研发与评价
AAPS PharmSciTech. 2025 May 16;26(5):136. doi: 10.1208/s12249-025-03129-0.
3
Artemisinin and Its Derivatives: Promising Therapeutic Agents for Age-Related Macular Degeneration.

本文引用的文献

1
Nanomicelles: Types, properties and applications in drug delivery.纳米胶束：类型、性质及其在药物传递中的应用。
IET Nanobiotechnol. 2021 Feb;15(1):19-27. doi: 10.1049/nbt2.12018. Epub 2021 Feb 2.
2
Antimalarial and anticancer properties of artesunate and other artemisinins: current development.青蒿琥酯及其他青蒿素的抗疟和抗癌特性：当前进展
Monatsh Chem. 2021;152(4):387-400. doi: 10.1007/s00706-021-02759-x. Epub 2021 Mar 30.
3
Distribution of polymeric nanoparticles in the eye: implications in ocular disease therapy.聚合物纳米粒子在眼部的分布：在眼部疾病治疗中的意义。
青蒿素及其衍生物：治疗年龄相关性黄斑变性的有前景的治疗药物。
Pharmaceuticals (Basel). 2025 Apr 6;18(4):535. doi: 10.3390/ph18040535.
4
Frontier applications of retinal nanomedicine: progress, challenges and perspectives.视网膜纳米医学的前沿应用：进展、挑战与展望
J Nanobiotechnology. 2025 Feb 25;23(1):143. doi: 10.1186/s12951-025-03095-6.
5
Therapeutic applications of artemisinin in ophthalmic diseases.青蒿素在眼科疾病中的治疗应用。
Heliyon. 2025 Jan 17;11(2):e42066. doi: 10.1016/j.heliyon.2025.e42066. eCollection 2025 Jan 30.
6
Fabrication and Characterization of Dissolving Microneedles Containing L. Extract Complex for Enhancement of Transfollicular Delivery.用于增强经毛囊递送的含L.提取物复合物的可溶微针的制备与表征
Polymers (Basel). 2024 Aug 22;16(16):2377. doi: 10.3390/polym16162377.
7
Development and Evaluation of Different Electrospun Cysteamine-Loaded Nanofibrous Webs: A Promising Option for Treating a Rare Lysosomal Storage Disorder.不同载有半胱胺的电纺纳米纤维网的开发与评估：治疗一种罕见溶酶体贮积症的有前景选择
Pharmaceutics. 2024 Aug 9;16(8):1052. doi: 10.3390/pharmaceutics16081052.
8
HPMC/PVP K90 Dissolving Microneedles Fabricated from 3D-Printed Master Molds: Impact on Microneedle Morphology, Mechanical Strength, and Topical Dissolving Property.由3D打印母模制成的HPMC/PVP K90溶解微针：对微针形态、机械强度和局部溶解性能的影响。
Polymers (Basel). 2024 Feb 6;16(4):452. doi: 10.3390/polym16040452.
9
Overview of Recent Advances in Nano-Based Ocular Drug Delivery.基于纳米的眼部药物输送的最新进展概述。
Int J Mol Sci. 2023 Oct 19;24(20):15352. doi: 10.3390/ijms242015352.
10
Design and Optimization of In Situ Gelling Mucoadhesive Eye Drops Containing Dexamethasone.含地塞米松的原位凝胶型黏膜黏附性滴眼液的设计与优化
Gels. 2022 Sep 2;8(9):561. doi: 10.3390/gels8090561.
J Nanobiotechnology. 2021 Jan 7;19(1):10. doi: 10.1186/s12951-020-00745-9.
4
The Diagnosis and Treatment of Age-Related Macular Degeneration.年龄相关性黄斑变性的诊断与治疗。
Dtsch Arztebl Int. 2020 Jul 20;117(29-30):513-520. doi: 10.3238/arztebl.2020.0513.
5
Rapid assessment of ocular drug delivery in a novel ex vivo corneal model.新型离体角膜模型中眼部药物传递的快速评估。
Sci Rep. 2020 Jul 16;10(1):11754. doi: 10.1038/s41598-020-68254-1.
6
Anti-malarial drug, artemisinin and its derivatives for the treatment of respiratory diseases.抗疟药物青蒿素及其衍生物治疗呼吸系统疾病。
Pharmacol Res. 2020 Aug;158:104901. doi: 10.1016/j.phrs.2020.104901. Epub 2020 May 13.
7
Influence factors on the critical micelle concentration determination using pyrene as a probe and a simple method of preparing samples.以芘为探针测定临界胶束浓度的影响因素及一种简单的样品制备方法。
R Soc Open Sci. 2020 Mar 4;7(3):192092. doi: 10.1098/rsos.192092. eCollection 2020 Mar.
8
Drug Delivery to the Posterior Segment of the Eye: Biopharmaceutic and Pharmacokinetic Considerations.眼部后段给药：生物药剂学和药代动力学考量
Pharmaceutics. 2020 Mar 16;12(3):269. doi: 10.3390/pharmaceutics12030269.
9
Potential applications of artemisinins in ocular diseases.青蒿素在眼部疾病中的潜在应用。
Int J Ophthalmol. 2019 Nov 18;12(11):1793-1800. doi: 10.18240/ijo.2019.11.20. eCollection 2019.
10
Design and development of artemisinin and dexamethasone loaded topical nanodispersion for the effective treatment of age-related macular degeneration.设计和开发青蒿素和地塞米松负载的局部纳米分散体，用于有效治疗年龄相关性黄斑变性。
IET Nanobiotechnol. 2019 Oct;13(8):868-874. doi: 10.1049/iet-nbt.2019.0130.