Preparation and In Vitro Characterization of Triamcinolone Acetonide-Loaded Lipid Liquid Crystal Nanocarriers for Ocular Delivery.

IF 3.1 Q2 PHARMACOLOGY & PHARMACY
Advanced pharmaceutical bulletin Pub Date : 2024-12-05 eCollection Date: 2025-04-01 DOI:10.34172/apb.43671
Fatemeh Asgharian Rezae, Malihe Karimi, Hossein Kamali, Bizhan Malaekeh-Nikouei
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引用次数: 0

Abstract

Purpose: This study aimed to develop sustained-release triamcinolone acetonide (TA) formulations using lipid liquid crystals (LLCs) for ocular drug delivery and to characterize the designed formulations.

Methods: Eighteen dispersed LLC formulations were prepared through a top-down approach, incorporating varying concentrations of TA and different proportions of glyceryl monooleate, deionized water, and pluronic F127. An additional formulation comprising TA: hydroxypropyl beta-cyclodextrin (HPβCD) complex was also developed to investigate the influence of HPβCD on the properties of the formulations. The formulations were evaluated for their rheological properties in room temperature using a rheometer, syringeability by passing them through a 27G needle, size measurements via dynamic light scattering (DLS), and morphology through polarized light microscopy (PLM). Furthermore, the prepared formulations were injected into a dialysis tube and placed in a phosphate buffer at pH 7.4 and 37 °C for in vitro release evaluation. Samples were taken at predetermined intervals and stored in a refrigerator until HPLC analysis. The percentage of Encapsulation efficacy and drug loading were evaluated using an indirect method. A reversed-phase HPLC method was employed to quantify the drug concentrations in the samples.

Results: All selected formulations demonstrated acceptable parameters, including particle size (less than 200 nm), polydispersity index (PDI) ranging from 0.202 to 0.355, and zeta potential values between -14.3 and -32.8 mV. Additionally, the formulations showed good syringeability and achieved 100% drug release within 48 hours (except for the formulation containing HPβCD). PLM analysis revealed the presence of hexosomes and cubosomes, indicating that an increase in hexosomes contributed to a more uniform drug release from the formulations.

Conclusion: Overall, the study findings suggest that liquid crystalline carriers can be a promising formulation for sustained ocular drug delivery of TA.

醋酸曲安奈德脂质液晶眼给药纳米载体的制备及体外表征。
目的:本研究旨在利用脂质液晶(llc)开发用于眼部给药的曲安奈德(triamcinolone acetonide, TA)缓释制剂,并对所设计的制剂进行表征。方法:采用自上而下的方法制备了18种分散的LLC配方,包括不同浓度的TA和不同比例的单油酸甘油、去离子水和pluronic F127。为了研究羟丙基β -环糊精(HPβCD)配合物对配方性能的影响,还开发了一种含有TA:羟丙基β -环糊精(HPβCD)配合物的配方。使用流变仪评估配方在室温下的流变特性,通过27G针通过注射性,通过动态光散射(DLS)测量尺寸,通过偏振光显微镜(PLM)测量形貌。此外,将制备的制剂注射到透析管中,置于pH 7.4和37°C的磷酸盐缓冲液中进行体外释放评估。样品在预定的时间间隔内取出,并保存在冰箱中,直到高效液相色谱分析。采用间接法评价包封率和载药量。采用反相高效液相色谱法定量样品中的药物浓度。结果:所有选择的配方均具有可接受的参数,包括粒径(小于200 nm),多分散性指数(PDI)在0.202 ~ 0.355之间,zeta电位值在-14.3 ~ -32.8 mV之间。此外,该制剂具有良好的注射性,并在48小时内达到100%的药物释放(含有HPβCD的制剂除外)。PLM分析显示六体体和立方体体的存在,表明六体体的增加有助于更均匀地从配方中释放药物。结论:总的来说,研究结果表明液晶载体可能是一种有前景的持续眼部给药制剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Advanced pharmaceutical bulletin
Advanced pharmaceutical bulletin PHARMACOLOGY & PHARMACY-
CiteScore
6.80
自引率
2.80%
发文量
51
审稿时长
12 weeks
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