Formulation and Optimization of Itraconazole Loaded Novel Nanostructured Lipid Carrier-based Ocular Controlled Release Formulation.

Q2 Pharmacology, Toxicology and Pharmaceutics Drug Delivery Letters Pub Date : 2019-06-18 DOI:10.2174/2210303109666190618102616
Ajay kUMAR Pathania, S. Bhatt, Manish Kumar, V. Saini
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Abstract

The low penetration power and the retention time into the intraocular tissue are the main problems that make difficult for most of the drugs for the ocular drug delivery system. This is for those drugs that are having the low or poor solubility and the low permeability. Nanostructured Lipid Carriers (NLCs) loaded with Itraconazole (ITZ) were formulated with the aim to increase the solubility and enhance the retention time in the intraocular tissue. Methods: The NLCs were prepared by using Pluronic (PF127), stearic acid and oleic acid. Itraconazole loaded Nanostructured lipid carrier were prepared by high-pressure homogenization method and the formulations were prepared and optimized by 3 Level Factorial Design. F6 was selected on the basis of better entrapment efficiency (94.65), optimum particle size (310nm), and percentage cumulative release (68.67%). Scanning electron microscopy revealed spherical Nanostructured lipid carrier in the microemulsion. Nanostructured lipid carrier Irritation test showed the non-irritancy and antifungal activity showed a more inhibition zone as compared to the marketed formulation. Conclusively the optimized Formulation (F6) shows better results for the ocular drug delivery as compared to the marked formulation.
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负载伊曲康唑的新型纳米脂质载体眼控释制剂的制备与优化。
低穿透力和进入眼内组织的滞留时间是使大多数药物难以用于眼部药物递送系统的主要问题。这是针对那些具有低溶解度或差溶解度和低渗透性的药物。配制了负载伊曲康唑(ITZ)的纳米脂质载体(NLCs),旨在增加其在眼内组织中的溶解度并延长其停留时间。方法:采用Pluronic(PF127)、硬脂酸和油酸制备NLCs。采用高压均化法制备了负载伊曲康唑的纳米脂质载体,并采用三级因子设计对其配方进行了制备和优化。根据包封率(94.65)、最佳粒径(310nm)和累积释放率(68.67%)选择了F6。扫描电镜显示微乳液中存在球形纳米脂质载体。纳米结构脂质载体刺激试验显示,与市场上的制剂相比,非刺激性和抗真菌活性显示出更多的抑制区。总之,与标记的制剂相比,优化的制剂(F6)在眼部药物递送方面显示出更好的结果。
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来源期刊
Drug Delivery Letters
Drug Delivery Letters Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
CiteScore
1.70
自引率
0.00%
发文量
30
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