Suvarna Vasanti, Gujar Parul, Murahari Manikanta
Department of Pharmaceutical Chemistry and Quality Assurance, SVKM's Dr. Bhanuben Nanavati College of Pharmacy, V.L. Mehta Road, Vile Parle (West), Mumbai 400056, Maharashtra, India.
Department of Pharmaceutical Chemistry and Quality Assurance, SVKM's Dr. Bhanuben Nanavati College of Pharmacy, V.L. Mehta Road, Vile Parle (West), Mumbai 400056, Maharashtra, India.
Biomed Pharmacother. 2017 Apr;88:1122-1144. doi: 10.1016/j.biopha.2017.01.157. Epub 2017 Feb 12.
Natural compounds have been attracting huge attention because of their broad therapeutic properties with specificity in their action in human health care as functional foods, pharmaceuticals and nutraceuticals. However poor bioavailability and reduced bioactivity attributed to poor solubility and instability is the major drawback hindering the incorporation of these therapeutically potential molecules in novel drug delivery systems. Based on the findings of reported research investigations; complexation of poorly water soluble phytochemicals with cyclodextrins has emerged to be a promising approach to improve their aqueous solubility, stability, rate of dissolution and bioavailability. The present article summarizes the encapsulation of natural compounds ranging from various flavonoids, phenolic derivatives, coumestans to triterpenes, with cyclodextrin and their derivatives. Also the article highlights the method of complexation, complexation ability, drug solubility, stability, bioavailability and safety aspects of reported natural compounds. Additionally we present the glimpses of patents published in recent 10-15 years to highlight the significance of inclusion of phytochemicals in cyclodextrins. In patents narrated, improvement in stability and solubility of curcumin by complexation with alkyl ether derivative of gamma-cyclodextrin is claimed. Another patent mentioned, complexation of artemisinins with β-cyclodextrin, improved the stability and integrity of peroxide part of artemisinins for long period. On the other hand the complex of dihydromyricetin with γ-CD has shown improved solubility, stability and bioavailability. Thus it can be concluded that phytochemicals have multiple biological activities with broader safety index and improvement of their solubility will be truly beneficial to aid their effective delivery in healthcare.
天然化合物因其具有广泛的治疗特性,在人类医疗保健中作为功能性食品、药物和营养保健品发挥着特定作用,因而备受关注。然而,由于溶解度差和稳定性低导致生物利用度差和生物活性降低,这是阻碍这些具有治疗潜力的分子纳入新型药物递送系统的主要缺点。基于已报道的研究调查结果,将水溶性差的植物化学物质与环糊精络合已成为提高其水溶性、稳定性、溶解速率和生物利用度的一种有前景的方法。本文总结了从各种黄酮类化合物、酚类衍生物、香豆雌酚到三萜类化合物等天然化合物与环糊精及其衍生物的包封情况。此外,本文还重点介绍了已报道的天然化合物的络合方法、络合能力、药物溶解度、稳定性、生物利用度和安全性方面。此外,我们还展示了最近10 - 15年发表的专利概况,以突出植物化学物质纳入环糊精的重要性。在所叙述的专利中,有人声称通过与γ-环糊精的烷基醚衍生物络合可提高姜黄素的稳定性和溶解度。另一项专利提到,青蒿素与β-环糊精络合,可长期提高青蒿素过氧化物部分的稳定性和完整性。另一方面,二氢杨梅素与γ-环糊精的络合物显示出溶解度、稳定性和生物利用度的提高。因此可以得出结论,植物化学物质具有多种生物活性,安全指数较高,提高其溶解度将真正有助于在医疗保健中实现其有效递送。