Pharmacokinetics of Curcumin Delivered by Nanoparticles and the Relationship with Antitumor Efficacy: A Systematic Review

Abstract

Curcumin is a polyphenolic compound, derived from Curcuma longa, and it has several pharmacological effects such as antioxidant, anti-inflammatory, and antitumor. Although it is a pleiotropic molecule, curcumin’s free form, which is lipophilic, has low bioavailability and is rapidly metabolized, limiting its clinical use. With the advances in techniques for loading curcumin into nanostructures, it is possible to improve its bioavailability and extend its applications. In this review, we gather evidence about the comparison of the pharmacokinetics (biodistribution and bioavailability) between free curcumin (Cur) and nanostructured curcumin (Cur-NPs) and their respective relationships with antitumor efficacy. The search was performed in the following databases: Cochrane, LILACS, Embase, MEDLINE/Pubmed, Clinical Trials, BSV regional portal, ScienceDirect, Scopus, and Web of Science. The selected studies were based on studies that used High-Performance Liquid Chromatography (HPLC) as the pharmacokinetics evaluation method. Of the 345 studies initially pooled, 11 met the inclusion criteria and all included studies classified as high quality. In this search, a variety of nanoparticles used to deliver curcumin (polymeric, copolymeric, nanocrystals, nanovesicles, and nanosuspension) were found. Most Cur-NPs presented negative Zeta potential ranging from −25 mV to 12.7 mV, polydispersion index (PDI) ranging from 0.06 to 0.283, and hydrodynamic diameter ranging from 30.47 to 550.1 nm. Selected studies adopted mainly oral and intravenous administrations. In the pharmacokinetics analysis, samples of plasma, liver, tumor, lung, brain, kidney, and spleen were evaluated. The administration of curcumin, in nanoparticle systems, resulted in a higher level of curcumin in tumors compared to free curcumin, leading to an improved antitumor effect. Thus, the use of nanoparticles can be a promising alternative for curcumin delivery since this improves its bioavailability.

Enhancing the Bioavailability and Bioactivity of Curcumin for Disease Prevention and Treatment

“…Nanoformulations may prevent diseases with an inflammatory, oxidative stress-, or aging-related component including cardiovascular, liver, lung, neurodegenerative, cancer, metabolic, and gastrointestinal diseases ( Table 1 ) [ 33 , 34 , 37 , 38 , 39 , 46 , 48 , 55 , 56 ].…”

Targeting Neutrophil Extracellular Traps in Gouty Arthritis: Insights into Pathogenesis and Therapeutic Potential

“…It should be also noted the fact that the application of curcumin is limited due to its rapid degradation, poor aqueous solubility, and low bioavailability. 273,274 Modifying curcumin to strengthen the therapeutic effect becomes a strategy. For instance, curcumin-loaded tetrahedral framework nucleic acids were synthesized to deliver curcumin, which exhibited better drug stability, biocompatibility, ease of uptake, higher tissue utilization and a better anti-inflammatory effect when compared to free curcumin in vitro and in vivo.…”

The Role of Curcumin in Oral Health and Diseases: A Systematic Review

“…Due to its poor oral bioavailability, non-hydrophilic nature, and rapid degradation, curcumin’s therapeutic potential is limited. With oral administration, approximately 40–85% of curcumin passes through the gastrointestinal tract unabsorbed [ 30 , 31 ]. It is largely metabolized in the intestine and liver and rapidly eliminated.…”

“…Different formulations of use have been studied (tablets, liposomal encapsulation, emulsions, capsules, nanoparticles, gels, ointments, and powder) to improve their bioavailability [ 30 ]. It has been administered alone or combined with other substances (lycopene and piperine, honey, green tea, tulsi, triamcinolone-hyaluronidase gel, and photodynamic therapy) [ 33 ].…”

“…Curcumin-containing toothpastes have been produced, recognizing their effectiveness in preventing dental plaque and gingivitis due to their antimicrobial action [ 30 ].…”