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Development and Evaluation of Curcumin Encapsulated Self-assembled Nanoparticles as Potential Remedial Treatment for PCOS in a Female Rat Model
International Journal of Nanomedicine ( IF 6.6 ) Pub Date : 2021-09-10 , DOI: 10.2147/ijn.s302161 Mazhar Ali Raja 1, 2 , Martin Maldonado 2 , Jianying Chen 2 , Ying Zhong 2 , Jiang Gu 1, 2
International Journal of Nanomedicine ( IF 6.6 ) Pub Date : 2021-09-10 , DOI: 10.2147/ijn.s302161 Mazhar Ali Raja 1, 2 , Martin Maldonado 2 , Jianying Chen 2 , Ying Zhong 2 , Jiang Gu 1, 2
Affiliation
Purpose: Polycystic ovary syndrome (PCOS) is one of the most common endocrinopathies affecting women of reproductive age and leads to metabolic disorders and infertility. The present study was conducted to investigate the therapeutic effects of curcumin (Cur) encapsulated arginine (Arg) and N-acetyl histidine (NAcHis) modified chitosan (Arg-CS-NAcHis/Cur) nanoparticles (NPs).
Methods: In this study, amphiphilic chitosan (CS) conjugate was developed by modification with hydrophilic arginine (Arg) and hydrophobic N-acetyl histidine (NAcHis) group (Arg-CS-NAcHis). The synthesized conjugate was well characterized by FTIR and NMR studies. Self-assembled nanoparticles based on the synthesized conjugate were developed by simple sonication method and characterized for the physicochemical properties of zeta potential, particle size and drug encapsulation. Next, in vitro drug release, cytotoxicity, and cellular uptake studies of the NPs were evaluated. Finally, the developed nanoparticles were examined for their therapeutic potential against estradiol valerate (EV) induced PCOS rats by evaluating hormone level changes and ovarian morphology.
Results: The results showed that zeta potential of the nanoparticles was 39.8± 2.52 mV and the average size was 200 nm. The in vitro drug release profile showed sustained release pattern. Cytotoxicity and cellular uptake studies also showed preferential effectiveness than free curcumin. Both the biochemical and histopathological studies showed positive effects in reverting the symptoms of PCOS rats to normalcy.
Conclusion: Curcumin encapsulated arginine and N-acetyl histidine modified chitosan (Arg-CS-NAcHis/Cur) nanoparticles have been successfully developed. The present study suggested that treatment of the nanoparticles might reverse many of the PCOS symptoms. Therefore, these nanoparticles might be used as promising new candidate for delivery of curcumin to treat PCOS.
Keywords: polycystic ovary syndrome, curcumin, self-assembled nanoparticles, cytotoxicity, cellular uptake
中文翻译：
姜黄素封装自组装纳米颗粒的开发和评估作为雌性大鼠模型中 PCOS 的潜在治疗方法
目的：多囊卵巢综合征（PCOS）是影响育龄妇女的最常见内分泌疾病之一，可导致代谢紊乱和不孕。本研究旨在研究姜黄素 (Cur) 封装的精氨酸 (Arg) 和 N-乙酰组氨酸 (NAcHis) 修饰的壳聚糖 (Arg-CS-NAcHis/Cur) 纳米颗粒 (NPs) 的治疗效果。
方法：本研究通过亲水性精氨酸（Arg）和疏水性N-乙酰组氨酸（NAcHis）基团（Arg-CS-NAcHis）修饰开发了两亲性壳聚糖（CS）缀合物。合成的缀合物通过 FTIR 和 NMR 研究得到了很好的表征。通过简单的超声处理方法开发了基于合成缀合物的自组装纳米颗粒，并表征了 zeta 电位、粒径和药物封装的理化性质。接下来，评估了纳米粒子的体外药物释放、细胞毒性和细胞摄取研究。最后，通过评估激素水平变化和卵巢形态，检查了所开发的纳米颗粒对戊酸雌二醇（EV）诱导的 PCOS 大鼠的治疗潜力。
结果：结果显示纳米粒子的zeta电位为39.8±2.52 mV，平均尺寸为200 nm。体外药物释放曲线显示持续释放模式。细胞毒性和细胞摄取研究也显示出比游离姜黄素更有效的效果。生化和组织病理学研究均显示出对 PCOS 大鼠症状恢复正常的积极作用。
结论：已成功开发出姜黄素封装的精氨酸和N-乙酰组氨酸修饰的壳聚糖（Arg-CS-NAcHis/Cur）纳米颗粒。目前的研究表明，纳米颗粒的治疗可能会逆转许多多囊卵巢综合征的症状。因此，这些纳米颗粒可能被用作姜黄素治疗多囊卵巢综合症的有希望的新候选者。
关键词:多囊卵巢综合征, 姜黄素, 自组装纳米粒子, 细胞毒性, 细胞摄取
更新日期：2021-09-10
Methods: In this study, amphiphilic chitosan (CS) conjugate was developed by modification with hydrophilic arginine (Arg) and hydrophobic N-acetyl histidine (NAcHis) group (Arg-CS-NAcHis). The synthesized conjugate was well characterized by FTIR and NMR studies. Self-assembled nanoparticles based on the synthesized conjugate were developed by simple sonication method and characterized for the physicochemical properties of zeta potential, particle size and drug encapsulation. Next, in vitro drug release, cytotoxicity, and cellular uptake studies of the NPs were evaluated. Finally, the developed nanoparticles were examined for their therapeutic potential against estradiol valerate (EV) induced PCOS rats by evaluating hormone level changes and ovarian morphology.
Results: The results showed that zeta potential of the nanoparticles was 39.8± 2.52 mV and the average size was 200 nm. The in vitro drug release profile showed sustained release pattern. Cytotoxicity and cellular uptake studies also showed preferential effectiveness than free curcumin. Both the biochemical and histopathological studies showed positive effects in reverting the symptoms of PCOS rats to normalcy.
Conclusion: Curcumin encapsulated arginine and N-acetyl histidine modified chitosan (Arg-CS-NAcHis/Cur) nanoparticles have been successfully developed. The present study suggested that treatment of the nanoparticles might reverse many of the PCOS symptoms. Therefore, these nanoparticles might be used as promising new candidate for delivery of curcumin to treat PCOS.
Keywords: polycystic ovary syndrome, curcumin, self-assembled nanoparticles, cytotoxicity, cellular uptake
中文翻译：
姜黄素封装自组装纳米颗粒的开发和评估作为雌性大鼠模型中 PCOS 的潜在治疗方法
目的：多囊卵巢综合征（PCOS）是影响育龄妇女的最常见内分泌疾病之一，可导致代谢紊乱和不孕。本研究旨在研究姜黄素 (Cur) 封装的精氨酸 (Arg) 和 N-乙酰组氨酸 (NAcHis) 修饰的壳聚糖 (Arg-CS-NAcHis/Cur) 纳米颗粒 (NPs) 的治疗效果。
方法：本研究通过亲水性精氨酸（Arg）和疏水性N-乙酰组氨酸（NAcHis）基团（Arg-CS-NAcHis）修饰开发了两亲性壳聚糖（CS）缀合物。合成的缀合物通过 FTIR 和 NMR 研究得到了很好的表征。通过简单的超声处理方法开发了基于合成缀合物的自组装纳米颗粒，并表征了 zeta 电位、粒径和药物封装的理化性质。接下来，评估了纳米粒子的体外药物释放、细胞毒性和细胞摄取研究。最后，通过评估激素水平变化和卵巢形态，检查了所开发的纳米颗粒对戊酸雌二醇（EV）诱导的 PCOS 大鼠的治疗潜力。
结果：结果显示纳米粒子的zeta电位为39.8±2.52 mV，平均尺寸为200 nm。体外药物释放曲线显示持续释放模式。细胞毒性和细胞摄取研究也显示出比游离姜黄素更有效的效果。生化和组织病理学研究均显示出对 PCOS 大鼠症状恢复正常的积极作用。
结论：已成功开发出姜黄素封装的精氨酸和N-乙酰组氨酸修饰的壳聚糖（Arg-CS-NAcHis/Cur）纳米颗粒。目前的研究表明，纳米颗粒的治疗可能会逆转许多多囊卵巢综合征的症状。因此，这些纳米颗粒可能被用作姜黄素治疗多囊卵巢综合症的有希望的新候选者。
关键词:多囊卵巢综合征, 姜黄素, 自组装纳米粒子, 细胞毒性, 细胞摄取
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