Research progress on pharmacokinetics and dosage forms of crocin and crocetin / 中草药

ABSTRACT

Crocin is derived from stigmas of Crocus sativus and fruits of Gardenia jasminoides. It is a type of unique water-soluble carotenoids with long conjugate, possessing remarkable neuroprotection, cardiovascular protection, antitumor, and other pharmacological activities. Data showed that orally administrated crocin couldn’t permeate into the bloodstream as the prototype, but it can be absorbed into the blood circulation after being hydrolyzed to crocetin in gastrointestinal tract. Then, crocetin is converted to glucuronic acid conjugate. Moreover, the metabolite crocetin are mainly distributed in heart, liver, spleen, lung, and other blood-rich tissues. In view of the low bioavailability and poor stability of crocin and its metabolite crocetin, researchers have extensively employed novel drug delivery system to study crocin (crocetin) in order to improve its stability, bioavailability, and pharmacological activity. This article reviews in vivo metabolism of crocin (crocetin) in recent years and investigations on drug delivery system, therefore, facilitating further research and development of these natural products.