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Changes in chemical stability and bioactivities of curcumin by forming inclusion complexes of beta- and Gama-cyclodextrins
Journal of Polymer Research ( IF 2.8 ) Pub Date : 2020-01-29 , DOI: 10.1007/s10965-019-1994-z
Nina Alizadeh , Shokufeh Malakzadeh

In the present study investigated the effect of curcumin (CUR), beta (β) and gamma (γ) cyclodextrin (CD) complexes on its solubility, stability, antioxidating activity and bioavailability. CUR the active principle of turmeric is a natural antioxidant agent with potent anti-inflammatory activity along with chemotherapeutic and chemopreventive properties. Poor solubility and poor oral bioavailability are the main reasons which preclude CUR use in therapy. Curcumin/CD complex systems were prepared and characterized by FT-IR, UV-Vis and 1HNMR spectroscopies. The content, solubility, dissolution, and stability of the complexes were evaluated and compared with curcumin and their physical mixture. The phase solubility analysis indicated that the solubility of CUR was increased in the presence of CDs and revealed an A(L)-type diagram, suggesting the formation of a 1:1 inclusion complex. The estimated apparent stability constant (K1:1), according to the Higuchi and Connors method, is 1.87 × 105 M−1 and 5.99 × 105 M−1 for CUR/β-CD and CUR/γ-CD respectively. The results of this study confirm the formation of inclusion complexes in solution and suggest that the complexes formation between CUR and CDs could improve the bioavailability of the drug due to the enhancing absorption expected from increased drug solubility. Furthermore, the antioxidant activities of CUR and CDs inclusion complexes were determined by the 1,1-diphenyl-2-picryl-hydrazyl (DPPH) method. The experimental results confirmed the forming of CUR complexes with CDs also these indicated that the CUR/CDs inclusion complexes were the most reactive than its free form into antioxidant activity.



中文翻译:

通过形成β-和Gama-环糊精的包合物形成姜黄素的化学稳定性和生物活性的变化

在本研究中,研究了姜黄素(CUR),β(β)和γ(γ)环糊精(CD)复合物对其溶解度,稳定性,抗氧化活性和生物利用度的影响。CUR姜黄的活性成分是一种天然抗氧化剂,具有强大的抗炎活性以及化学治疗和化学预防作用。溶解度差和口服生物利用度差是阻止CUR用于治疗的主要原因。制备姜黄素/ CD复合体系并通过FT-IR,UV-Vis和1表征HNMR光谱学。评价复合物的含量,溶解度,溶解度和稳定性,并将其与姜黄素及其物理混合物进行比较。相溶解度分析表明,在CD的存在下CUR的溶解度增加,并显示A(L)型图,表明形成了1:1的包合物。根据Higuchi和Connors方法,估计的视在稳定常数(K1:1)为1.87×10 5  M -1和5.99×10 5  M -1分别用于CUR /β-CD和CUR /γ-CD。这项研究的结果证实了溶液中包合物的形成,并表明CUR和CD之间的复合物的形成可以提高药物的生物利用度,因为药物溶解度的提高有望增强吸收。此外,CUR和CD包合物的抗氧化活性是通过1,1-二苯基-2-吡啶基-肼基(DPPH)方法测定的。实验结果证实了具有CD的CUR复合物的形成,这也表明CUR / CDs包含物的复合物比其游离形式更具活性,具有抗氧化活性。

更新日期:2020-01-29
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