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载盐酸环丙沙星的眼部丝素蛋白脂质体:制剂、表征、细胞毒性及抗菌活性

Ciprofloxacin hydrochloride-loaded ocular silk fibroin liposomes: Formulation, characterisation, cytotoxicity, and antimicrobial activity.

作者信息

Bhat Umer Mushtaq, Khan Nisar Ahmad, Raza Syed Naiem, Ali Mohammad, Mehdi Seema, Mohiuddin Ishfaq, Shakeel Faiyaz, Bhat Zulfikar Ali, Bader Ghulam Nabi, Chashoo Ishtiaq Ahmad, Din Wani Shahid Ud

机构信息

Department of Pharmaceutical Sciences, School of Applied Sciences and Technology, University of Kashmir, Srinagar, 190006, India.

Department of Pharmacology, Sri Adichunchanagiri College of Pharmacy, Adichunchanagiri University, B.G Nagar, Nagamagala, Bellur, Karnataka, 571418, India.

出版信息

Heliyon. 2024 Oct 1;10(22):e38777. doi: 10.1016/j.heliyon.2024.e38777. eCollection 2024 Nov 30.

Abstract

Ocular drugs have low absorption because of the unique environment in the eye, making ocular drugs one of the most challenging pharmaceutical initiatives. Liposomes have shown to be a promising ocular drug delivery system over the years because of enhanced drug absorption, biocompatibility, and biodegradability. Utilising a mucoadhesive material alongside liposomes could be a promising strategy to increase the therapeutic efficacy of ocular drugs. The present study aimed to develop a silk fibroin (SF)-coated liposomal formulation as an ocular drug delivery system. Regenerated silk fibroin (a novel biopolymer) was coated on ciprofloxacin hydrochloride-loaded liposomes (CPH-SFLs). Studies were carried out on the morphology, drug encapsulation efficiency, and drug release. Human corneal epithelial cells (HCEC) were used to examine the cellular adherence and cytotoxicity of CPH-SFLs. CPH-SFLs had an average particle size of 183 ± 3 nm as opposed to 169 ± 4 of blank SFLs. CPH-loaded SFLs lacked the endothermic peak of CPH at 150 °C, indicating that the CPH molecules were trapped in the SF polymeric grid. In the case of the formulations, 25 %-45 % of the medicine was released at a relatively fast pace over the course of the first 4 h and then at a slower rate over the course of the next 12-24 h. CPH-SFLs demonstrated sustained drug release and high ocular penetration of CPH. The MTT test was conducted to gauge the viability of HCECs, cell viability was higher than 85 %, demonstrating that CPH-SFLs had no adverse effects on HCEC. The observed CPH-SFL adhesions to HCECs were swift and persistent, like the cellular uptake of CPH-SFLs by HCECs. When compared to CPH-solution, the produced formulation CPH-SFLs demonstrated significantly (P < 0.0001) greater susceptibility. The studies concluded that SF-coated liposomes could be the most viable ocular drug delivery in comparison to conventional eye drops.

摘要

由于眼部独特的环境,眼部药物的吸收较低,这使得眼部药物成为最具挑战性的制药项目之一。多年来,脂质体已被证明是一种很有前景的眼部药物递送系统,因为它能提高药物吸收、具有生物相容性和可生物降解性。将粘膜粘附材料与脂质体一起使用可能是提高眼部药物治疗效果的一种有前景的策略。本研究旨在开发一种丝素蛋白(SF)包被的脂质体制剂作为眼部药物递送系统。将再生丝素蛋白(一种新型生物聚合物)包被在载有盐酸环丙沙星的脂质体(CPH-SFLs)上。对其形态、药物包封率和药物释放进行了研究。使用人角膜上皮细胞(HCEC)来检测CPH-SFLs的细胞粘附性和细胞毒性。CPH-SFLs的平均粒径为183±3nm,而空白SFLs为169±4nm。载有CPH的SFLs在150℃时没有CPH的吸热峰,表明CPH分子被困在SF聚合物网格中。对于这些制剂,25%-45%的药物在前4小时内以相对较快的速度释放,然后在接下来的12-24小时内以较慢的速度释放。CPH-SFLs显示出药物的持续释放和CPH的高眼部渗透性。进行MTT试验以评估HCEC的活力,细胞活力高于85%,表明CPH-SFLs对HCEC没有不良影响。观察到CPH-SFLs对HCEC的粘附迅速且持久,就像HCEC对CPH-SFLs的细胞摄取一样。与CPH溶液相比,所制备的制剂CPH-SFLs表现出显著更高的敏感性(P<0.0001)。研究得出结论,与传统眼药水相比,SF包被的脂质体可能是最可行的眼部药物递送方式。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d43e/11605355/c3f11281d8b8/ga1.jpg

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