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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.

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/fd95/8470191/8ef3c3956646/polymers-13-03038-g001.jpg

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