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伏立康唑眼用固体脂质纳米粒原位凝胶的制备与评价

Formulation and evaluation of voriconazole ophthalmic solid lipid nanoparticles in situ gel.

作者信息

Pandurangan Dinesh Kumar, Bodagala Prathima, Palanirajan Vijayaraj Kumar, Govindaraj Saravanan

机构信息

Department of Pharmaceutics, Hindu College of Pharmacy, Acharya Nagarjuna University, Guntur, Andhra Pradesh, India.

Department of Pharmaceutics, School of Pharmacy, University College Sadaya International University, Kuala Lumpur, Malaysia.

出版信息

Int J Pharm Investig. 2016 Jan-Mar;6(1):56-62. doi: 10.4103/2230-973X.176488.

Abstract

In the present investigation, solid lipid nanoparticles (SLNs)-loaded in situ gel with voriconazole drug was formulated. Further, the formulation was characterized for pH, gelling capacity, entrapment efficiency, in vitro drug release, drug content, and viscosity. Voriconazole is an antifungal drug used to treat various infections caused by yeast or other types of fungi. Film hydration technique was used to prepared SLNs from lecithin and cholesterol. Based on the entrapment efficiency 67.2-97.3% and drug release, the optimized formulation NF1 of SLNs was incorporated into in situ gels. The in situ gels were prepared using viscosity-enhancing polymers such as Carbopol and (hydroxypropyl)methyl cellulose (HPMC). Formulated SLN in situ gel formulations were characterized, which showed pH 4.9-7.1, drug content 65.69-96.3%, and viscosity (100 rpm) 120-620 cps. From the characterizations given above, F6 was optimized and evaluated for microbial assay and ocular irritation studies. Microbial assay was conducted by the cup-plate method using Candida albicans as the test organism. An ocular irritation study was conducted on albino rabbits. The results revealed that there was no ocular damage to the cornea, conjunctiva, or iris. Stability studies were carried out on the F6 formulation for 3 months, which showed that the formulation had good stability. These results indicate that the studied SLNs-loaded in situ gel is a promising vehicle for ocular delivery.

摘要

在本研究中,制备了载有伏立康唑药物的固体脂质纳米粒(SLNs)原位凝胶。此外,对该制剂的pH值、胶凝能力、包封率、体外药物释放、药物含量和粘度进行了表征。伏立康唑是一种抗真菌药物,用于治疗由酵母或其他类型真菌引起的各种感染。采用薄膜水化技术由卵磷脂和胆固醇制备SLNs。基于67.2 - 97.3%的包封率和药物释放情况,将优化后的SLNs制剂NF1加入原位凝胶中。原位凝胶使用诸如卡波姆和羟丙基甲基纤维素(HPMC)等增粘聚合物制备。对所制备的SLN原位凝胶制剂进行了表征,结果显示pH值为4.9 - 7.1,药物含量为65.69 - 96.3%,粘度(100转/分钟)为120 - 620厘泊。根据上述表征结果,对F6进行了优化,并进行了微生物检测和眼部刺激性研究。微生物检测采用杯碟法,以白色念珠菌作为测试微生物。对白化兔进行了眼部刺激性研究。结果显示,对角膜、结膜或虹膜没有造成眼部损伤。对F6制剂进行了3个月的稳定性研究,结果表明该制剂具有良好的稳定性。这些结果表明,所研究的载有SLNs的原位凝胶是一种有前景的眼部给药载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ec9/4787063/c82ba53d5af1/IJPI-6-56-g003.jpg

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