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Fabrication and in vitro Evaluation of 4-HIA Encapsulated PLGA Nanoparticles on PC12 Cells
International Journal of Nanomedicine ( IF 8 ) Pub Date : 2021-08-17 , DOI: 10.2147/ijn.s317986 Tekupalli Ravikiran 1 , Santosh Anand 2 , Mohammad Azam Ansari 3 , Mohammad N Alomary 4 , Sami AlYahya 4 , Sowbhagya Ramachandregowda 1 , Saad Alghamdi 5 , Anupama Sindhghatta Kariyappa 1 , Bhagyalakshmi Dundaiah 1 , Mamatha Madhugiri Gopinath 1 , Sumreen Sultana 1 , Shital Manohar Punekar 1 , Thimappa Ramachandrappa Lakshmeesha 1
International Journal of Nanomedicine ( IF 8 ) Pub Date : 2021-08-17 , DOI: 10.2147/ijn.s317986 Tekupalli Ravikiran 1 , Santosh Anand 2 , Mohammad Azam Ansari 3 , Mohammad N Alomary 4 , Sami AlYahya 4 , Sowbhagya Ramachandregowda 1 , Saad Alghamdi 5 , Anupama Sindhghatta Kariyappa 1 , Bhagyalakshmi Dundaiah 1 , Mamatha Madhugiri Gopinath 1 , Sumreen Sultana 1 , Shital Manohar Punekar 1 , Thimappa Ramachandrappa Lakshmeesha 1
Affiliation
Purpose: 4-Hydroxyisophthalic acid (4-HIA) is a bioactive compound present in the roots of Decalepis hamiltonii, which has attracted considerable attention in attenuating oxidative stress-related neurodegenerative diseases. However, its efficacy is limited because of its low solubility and bioavailability. Therefore, the present study aimed to encapsulate 4-HIA using biocompatible copolymer polylactide-co-glycolide (PLGA) and evaluate its antioxidant and neuroprotective potential.
Methods: The nanoparticles (NPs) were fabricated by solid/oil/water (s/o/w) emulsion technique and characterized using XRD, SEM, HR-TEM, and FTIR spectroscopy. Antioxidant assays such as 1,1 diphenyl-2-picrylhydrazyl (DPPH), superoxide, and hydroxyl radical scavenging ability were performed to assess the antioxidant potential of the fabricated NPs.
Results: The bioactive component, 4-HIA, was efficiently encapsulated by the PLGA polymer and was found to be spherical and smooth with a size < 10nm. 4-HIA showed better scavenging capability in DPPH and superoxide assays as compared to 4-HIA encapsulated PLGA and butylated hydroxytoluene (BHT). In contrast, 4-HIA encapsulated PLGA NPs exhibited a significant hydroxyl radical scavenging activity than 4-HIA and BHT alone. Further, the encapsulated NPs efficiently curtailed hydrogen peroxide (H2O2)-induced cytotoxicity in PC12 cells.
Conclusion: Our findings indicate that 4-HIA encapsulated PLGA NPs might be a therapeutic intervention towards the effective management of oxidative stress as it has exhibited efficient neuroprotective potential against H2O2-induced oxidative stress in PC12 cells.
Keywords: 4-Hydroxyisophthalic acid, polylactic-co-glycolic acid, nanoencapsulation, PC12 cells, cytotoxicity
中文翻译：
4-HIA 封装 PLGA 纳米颗粒在 PC12 细胞上的制备和体外评价
目的： 4-羟基间苯二甲酸（4-HIA）是一种存在于哈密尔顿德卡勒皮斯根中的生物活性化合物，在减轻氧化应激相关的神经退行性疾病方面引起了广泛关注。然而，由于其低溶解度和生物利用度，其功效受到限制。因此，本研究旨在使用生物相容性共聚物聚乳酸-乙交酯 (PLGA) 封装 4-HIA，并评估其抗氧化和神经保护潜力。
方法：纳米粒子 (NPs) 采用固体/油/水 (s/o/w) 乳液技术制备，并使用 XRD、SEM、HR-TEM 和 FTIR 光谱进行表征。进行抗氧化剂测定，例如 1,1 二苯基-2-苦基肼 (DPPH)、超氧化物和羟基自由基清除能力，以评估制造的 NPs 的抗氧化潜力。
结果：生物活性成分 4-HIA 被 PLGA 聚合物有效封装，呈球形且光滑，尺寸 < 10nm。与 4-HIA 封装的 PLGA 和丁基化羟基甲苯 (BHT) 相比，4-HIA 在 DPPH 和超氧化物测定中显示出更好的清除能力。相比之下，4-HIA 封装的 PLGA NPs 比单独的 4-HIA 和 BHT 表现出显着的羟基自由基清除活性。此外，封装的 NPs 有效地减少了 PC12 细胞中过氧化氢 (H 2 O 2 ) 诱导的细胞毒性。
结论：我们的研究结果表明，4-HIA 封装的 PLGA NPs 可能是一种有效管理氧化应激的治疗干预措施，因为它对 H 2表现出有效的神经保护潜力O 2诱导的 PC12 细胞中的氧化应激。
关键词： 4-羟基间苯二甲酸，聚乳酸-乙醇酸共聚物，纳米包封，PC12细胞，细胞毒性
更新日期：2021-08-17
Methods: The nanoparticles (NPs) were fabricated by solid/oil/water (s/o/w) emulsion technique and characterized using XRD, SEM, HR-TEM, and FTIR spectroscopy. Antioxidant assays such as 1,1 diphenyl-2-picrylhydrazyl (DPPH), superoxide, and hydroxyl radical scavenging ability were performed to assess the antioxidant potential of the fabricated NPs.
Results: The bioactive component, 4-HIA, was efficiently encapsulated by the PLGA polymer and was found to be spherical and smooth with a size < 10nm. 4-HIA showed better scavenging capability in DPPH and superoxide assays as compared to 4-HIA encapsulated PLGA and butylated hydroxytoluene (BHT). In contrast, 4-HIA encapsulated PLGA NPs exhibited a significant hydroxyl radical scavenging activity than 4-HIA and BHT alone. Further, the encapsulated NPs efficiently curtailed hydrogen peroxide (H2O2)-induced cytotoxicity in PC12 cells.
Conclusion: Our findings indicate that 4-HIA encapsulated PLGA NPs might be a therapeutic intervention towards the effective management of oxidative stress as it has exhibited efficient neuroprotective potential against H2O2-induced oxidative stress in PC12 cells.
Keywords: 4-Hydroxyisophthalic acid, polylactic-co-glycolic acid, nanoencapsulation, PC12 cells, cytotoxicity
中文翻译：
4-HIA 封装 PLGA 纳米颗粒在 PC12 细胞上的制备和体外评价
目的： 4-羟基间苯二甲酸（4-HIA）是一种存在于哈密尔顿德卡勒皮斯根中的生物活性化合物，在减轻氧化应激相关的神经退行性疾病方面引起了广泛关注。然而，由于其低溶解度和生物利用度，其功效受到限制。因此，本研究旨在使用生物相容性共聚物聚乳酸-乙交酯 (PLGA) 封装 4-HIA，并评估其抗氧化和神经保护潜力。
方法：纳米粒子 (NPs) 采用固体/油/水 (s/o/w) 乳液技术制备，并使用 XRD、SEM、HR-TEM 和 FTIR 光谱进行表征。进行抗氧化剂测定，例如 1,1 二苯基-2-苦基肼 (DPPH)、超氧化物和羟基自由基清除能力，以评估制造的 NPs 的抗氧化潜力。
结果：生物活性成分 4-HIA 被 PLGA 聚合物有效封装，呈球形且光滑，尺寸 < 10nm。与 4-HIA 封装的 PLGA 和丁基化羟基甲苯 (BHT) 相比，4-HIA 在 DPPH 和超氧化物测定中显示出更好的清除能力。相比之下，4-HIA 封装的 PLGA NPs 比单独的 4-HIA 和 BHT 表现出显着的羟基自由基清除活性。此外，封装的 NPs 有效地减少了 PC12 细胞中过氧化氢 (H 2 O 2 ) 诱导的细胞毒性。
结论：我们的研究结果表明，4-HIA 封装的 PLGA NPs 可能是一种有效管理氧化应激的治疗干预措施，因为它对 H 2表现出有效的神经保护潜力O 2诱导的 PC12 细胞中的氧化应激。
关键词： 4-羟基间苯二甲酸，聚乳酸-乙醇酸共聚物，纳米包封，PC12细胞，细胞毒性
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