Table 2.
Bioavailability issues of polyphenols and various pharmaceutical formulations/delivery systems to overcome it.
| Polyphenol | Bioavailability Issue | Delivery System | Subject | Result | Reference |
|---|---|---|---|---|---|
| Curcumin | Low bioavailability and degradation in solution form | Microencapsulation of curcumin in liposomes by the combination of ethanol injection and high-pressure processing | - | Effectively decreases the size of particle and PDI, which helps to cross the biological membrane. Sterilizes the bacterial, which prevent degradation in solution | [127] |
| Low bioavailability and rapid metabolism | Nanoparticle fabricated by EGCG and PVP | - | Bioavailability increased 12-fold through intestine EGCG Inhibit the metabolism of Cur, Shows high Caco-2 monolayer permeation and cellular uptake |
[128] | |
| Low bioavailability and rapid metabolism | Emulsion was formed using different types of oils: corn oil, olive oil, and medium chain triglycerides (MCT) | - | Type of oil increased its transenterocyte absorption and reduced cellular metabolism | [129] | |
| Less physicochemical properties and oral bioavailability | Microencapsulating turmeric oleoresin with bioenhancers by spray drying using piperine and quercetin | - | Spray-dried powder with piperine (PIP) and quercetin (Quer) has higher permeability | [130] | |
| Low solubility and bioavailability | Zein-based nanoparticles | Wistar rats | Incresaed (9-fold) oral bioavailability with respect to the standard curcumin natural extract. | [131] | |
| Low bioavailability | Curcugen: dispersible, 98.5% turmeric-based curcuminoids formula | Randomized double-blind, 2-way cross over, single oral dose in humans | Auc-39 times and Cmax 16.1 times higher than of curcumin | [132] | |
| Low bioavailability | Curcumin-encapsulated chitosan (Cur-CS) nanoparticles | Crandell–Rees feline kidney of cat | Enhanced bioavailability, Cmax- 621.5 ng/mL three times more than normal curcumin | [133] | |
| Low bioavailability | Curcumin-loaded self-microemulsifying lipid carriers | Male Wistar rats | Higher bioavailability (29-fold) as compared to curcumin suspension | [134] | |
| Quercetin | Low bioavailability and less efficacy | Quercetin nano emulsion | Streptozocin-induced antidiabetic study in rats | Cmax of quercetin NE is 5962.74 ± 238.54 ng/mL and of quercetin pure drug is 1634.28 ± 70.18 ng/mL. AUC0-t and AUC0−∞ were 4.46 and 5.32 times higher than pure drug, respectively | [135] |
| Green tea (Epigallocatechin-3-gallate and L-theanine) | EGCG bioavailability is <5% | Preparation of EGCG + LTA/β-cyclodextrin (βCD) inclusion complexes by freeze-drying EGCG + LTA |
Rats | EGCG bioavailability is improved through lipid lowerig and weight loss effects of EGCG (p < 0.05) | [136] |
| Low permeation and poor stability leads to low oral bioavailability | Nanospanlastic | Male Wistar rats | Cmax- niosomal formula (p < 0.05) and free EGCG dispersion (p < 0.001). AUC- niosomal formula (p < 0.01) and EGCG dispersion (p < 0.001) | [137] | |
| Low bioavailability and chemical instability | EGCG loaded solid lipid nanoparticles SLN | Male Wistar albino rats | Cmax of EGCG is 60.7 ± 1.07 * and EGCG loaded SLN 240 ± 16 * AUC of EGCG is 567 ± 14.5 * while EGCG loaded SL is 2329 ± 434.5 ** |
[138] | |
| Poor oral bioavailability | Nanoparticles (NP) | Sprague Dawley rats | Cmax- EGCG NP 653.5 ± 181.3 * and EGCG powder 564.5 ± 121.7 * AUC 0–∞- EGCG NP5,241.6 ± 387.9 ** and EGCG powder 1321.6 ± 201.4 ** |
[139] | |
| Poor bioaccesibility | Nanoemulsion | Sprague-Dawley (SD) rats | Cmax- nanoemulsion 166.7 ± 22.6 * and sol 258.8 ± 135.1 * AUC0-t- nanoemulsion 17.1 ± 0.1 ** and sol 13.3 ± 0.2 ** |
[140] | |
| Green tea (Catechin) | Poor oral bioavailability | Catechin-loaded chitosan-tethered liposomes (Chitosomes) | Male Wistar rats | Cmax- Chitosomes 239.0 ± 35.27 * and sol 120.0 ± 3.97 * AUC0–24- Chitosomes 12,183 ± 1760.00 ** and sol 5739 ± 205.50 ** |
[141] |
| Flaxseed | Poor efficacy | Flaxseed oil-based neuronanoemulsions (NNEs) | Balb/c mice | Plasma Cmax- NNE 24.09 ug/mL8 and pure drug suspension (PDS) 12.98 ug/ml * AUC0-12- NNE 96.38 ± 1.39 ** and PDS 18.10 ± 0.15 ** Brain Cmax- NNE 12.98 ± 0.05 * and PDS 1.67 ± 0.02 AUC0-12- NNE 107.58 ± 3.75 ** and PDS 13.18 ± 0.25 ** |
[142] |
| Gallic, quercetin, amla, pomegranate | Poor bioavailability | Polyherbal nanoparticles and polyherbal extract following oral administration, pharmacokinetic parameters for polyherbal nanop | Male Wistar rats | GA and quercetin in polymeric nanoparticles improve their oral bioavailability | [143] |
* Cmax—maximum plasma concentration (ng/mL), ** AUC—area under the curve (ng·h/mL). EGCG—epigallocatechin-3-gallate, PVP- poly (N-vinylpyrrolidone).