{"title":"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。","authors":"Fatemeh Asgharian Rezae, Malihe Karimi, Hossein Kamali, Bizhan Malaekeh-Nikouei","doi":"10.34172/apb.43671","DOIUrl":null,"url":null,"abstract":"<p><strong>Purpose: </strong>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.</p><p><strong>Methods: </strong>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 <i>in vitro</i> 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.</p><p><strong>Results: </strong>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.</p><p><strong>Conclusion: </strong>Overall, the study findings suggest that liquid crystalline carriers can be a promising formulation for sustained ocular drug delivery of TA.</p>","PeriodicalId":7256,"journal":{"name":"Advanced pharmaceutical bulletin","volume":"15 1","pages":"70-81"},"PeriodicalIF":3.1000,"publicationDate":"2024-12-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12235358/pdf/","citationCount":"0","resultStr":"{\"title\":\"Preparation and <i>In Vitro</i> Characterization of Triamcinolone Acetonide-Loaded Lipid Liquid Crystal Nanocarriers for Ocular Delivery.\",\"authors\":\"Fatemeh Asgharian Rezae, Malihe Karimi, Hossein Kamali, Bizhan Malaekeh-Nikouei\",\"doi\":\"10.34172/apb.43671\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Purpose: </strong>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.</p><p><strong>Methods: </strong>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 <i>in vitro</i> 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.</p><p><strong>Results: </strong>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.</p><p><strong>Conclusion: </strong>Overall, the study findings suggest that liquid crystalline carriers can be a promising formulation for sustained ocular drug delivery of TA.</p>\",\"PeriodicalId\":7256,\"journal\":{\"name\":\"Advanced pharmaceutical bulletin\",\"volume\":\"15 1\",\"pages\":\"70-81\"},\"PeriodicalIF\":3.1000,\"publicationDate\":\"2024-12-05\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12235358/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Advanced pharmaceutical bulletin\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.34172/apb.43671\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2025/4/1 0:00:00\",\"PubModel\":\"eCollection\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Advanced pharmaceutical bulletin","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.34172/apb.43671","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/4/1 0:00:00","PubModel":"eCollection","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Preparation and In Vitro Characterization of Triamcinolone Acetonide-Loaded Lipid Liquid Crystal Nanocarriers for Ocular Delivery.
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.