Ipar Vinod S, Dsouza Anisha, Devarajan Padma V
Institute of Chemical Technology, Mumbai, India.
Piramal Enterprises Limited, Lighthall, A-wing, Saki Vihar road, Chandivali, Andheri, Mumbai, 400072, India.
Eur J Drug Metab Pharmacokinet. 2019 Aug;44(4):459-480. doi: 10.1007/s13318-019-00545-z.
Curcumin is a promising therapeutic agent that exhibits manifold therapeutic activities. However, it is challenging to study curcumin as it exhibits poor aqueous solubility and low permeability and it is a substrate for P-glycoprotein (P-gp). It is readily metabolized in the body, but many active metabolites of curcumin have been identified that could also be exploited for therapy. Strategies for the oral bioenhancement of curcumin to leverage the potential of curcumin as a therapeutic molecule are discussed here in light of these challenges. A brief discussion of conventional bioenhancement strategies using cyclodextrin complexes, solid dispersions, and solid self-emulsifying drug delivery systems is given. However, the major focus of this review is the application of nano-based approaches to the bioenhancement of curcumin. A description of the main advantages of nanosystems is followed by a detailed review of various nanosystems of curcumin, including nanosuspensions and various carrier-based nanosystems. Each nanosystem considered here is first briefly introduced, and then studies of the nanosystem containing curcumin are discussed. Lipid-based systems including liposomes and solid lipid nanoparticles, microemulsions, self-microemulsifying drug-delivery systems, nanoemulsions, and polymeric nanoparticles-which are widely explored-are dealt with in detail. Other miscellaneous systems discussed include inorganic nanoparticles, micelles, solid nanodispersions, phytosomes, and dendrimers. The possibility of using intact nanoparticles to achieve the targeted oral delivery of curcumin and thus harness the benefits of this wonder nutraceutical is an exciting prospect.
姜黄素是一种有前景的治疗剂，具有多种治疗活性。然而，研究姜黄素具有挑战性，因为它的水溶性差、渗透性低，并且是P-糖蛋白（P-gp）的底物。它在体内很容易被代谢，但已鉴定出许多姜黄素的活性代谢物，它们也可用于治疗。鉴于这些挑战，本文讨论了增强姜黄素口服生物利用度以发挥其作为治疗分子潜力的策略。简要讨论了使用环糊精复合物、固体分散体和固体自乳化药物递送系统的传统生物增强策略。然而，本综述的主要重点是基于纳米的方法在姜黄素生物增强中的应用。在描述纳米系统的主要优点之后，详细综述了姜黄素的各种纳米系统，包括纳米混悬液和各种基于载体的纳米系统。这里考虑的每个纳米系统首先简要介绍，然后讨论含姜黄素纳米系统的研究。对包括脂质体和固体脂质纳米粒、微乳、自微乳化药物递送系统、纳米乳和聚合物纳米粒等广泛探索的基于脂质的系统进行了详细阐述。讨论的其他杂项系统包括无机纳米粒、胶束、固体纳米分散体、植物脂质体和树枝状聚合物。使用完整的纳米粒实现姜黄素的靶向口服递送并因此利用这种神奇营养保健品的益处是一个令人兴奋的前景。
