Difference and alteration in pharmacokinetic and metabolic characteristics of low-solubility natural medicines

Abstract

Drug metabolism plays vital roles in the absorption and pharmacological activity of poorly soluble natural medicines. It is important to choose suitable delivery systems to increase the bioavailability and bioactivity of natural medicines with low solubility by regulating their metabolism and pharmacokinetics. This review investigates recent developments about the metabolic and pharmacokinetic behavior of poorly soluble natural medicines and their delivery systems. Delivery systems, dosage, administration route and drug-drug interactions alter the metabolic pathway, and bioavailability of low-solubility natural medicines to different degrees. Influencing factors such as formulation, dosage, and administration route are discussed. The metabolic reactions, metabolic enzymes, metabolites and pharmacokinetic behaviors of low-solubility natural medicines, and their delivery systems are systematically reviewed. There are various metabolic situations in the case of low-solubility natural medicines. CYP3A4 and CYP2C are the most common metabolic enzymes, and hydroxylation is the most common metabolic reaction of low solubility natural medicines. The stereo isomeric configuration can have a large influence on metabolism. This review will be useful for physicians and pharmacists to guide more accurate treatment with low-solubility natural medicines by increasing drug efficacies and protecting patients from toxic side effects.

Research progress on evodiamine, a bioactive alkaloid of Evodiae fructus: Focus on its anti‑cancer activity and bioavailability (Review)

“…The metabolism of low-solubility natural medicines partly depend on drug-drug interactions and the delivery systems (33). Appropriate drug delivery systems can contribute to increased absorption, improved bioavailability, prolonged residence time and minimized side effects of low-solubility natural medicines (33).…”

“…Cytotoxic drug-carrying nano-carriers are a viable strategy for enhancing cancer cell cytotoxicity and minimizing side effects. Nano-emulsion, which includes lipid nano-emulsion, inclusion complexes, nanoparticles and noisomes, is a vital component of nano-carriers (33). A novel type of water-in-oil nano-emulsion containing EVO-phospholipid nanocomplexes (NEEPN) was considered to be a good carrier for the oral delivery of EVO due to its favorable in vivo kinetic characteristics in rat (93).…”

“…Drug metabolism serves crucial roles in the bioavailability and subsequent pharmacological activities of poorly soluble, naturally occurring therapeutic agents, which significant impacts their toxicity profile and side effects (33). Previous studies have reported that the toxicity of EVO may be associated with its mechanism of metabolism in vivo and pharmacokinetics (34,35).…”

Natural Oral Anticancer Medication in Small Ethanol Nanosomes Coated with a Natural Alkaline Polysaccharide

“…The medicinal natural product curcumin (CM) has shown high potential against various chronic diseases, including many solid tumors, such as various types of lung cancer cells and stem cells. − However, the clinical applications of CM have been severely limited because of its low bioavailability caused by poor solubility, instability, low absorption, and rapid elimination . Different CM analogues and nanosystems , have been developed and applied to address the above problems.…”

“…7−10 However, the clinical applications of CM have been severely limited because of its low bioavailability caused by poor solubility, instability, low absorption, and rapid elimination. 11 Different CM analogues 12 and nanosystems 13,14 have been developed and applied to address the above problems. Considering the feasibility of clinical transformation, liposomes are the first choice for anticancer drug formulation.…”