Review Article

Improving In Vivo Efficacy of Bioactive Molecules: An Overview of Potentially Antitumor Phytochemicals and Currently Available Lipid-Based Delivery Systems

Table 5

Overview of lipid-based delivery systems to administer phytochemicals by oral route.

Active ingredientLipid-based formulationEffect of formulationRef.

VinorelbineLiposomesReduced side effects and increased circulation half-life.[94]
Improved therapeutic effect in vivo.
GypenosideActivated in vitro immune response in macrophages.[335]
CurcuminImproved pharmacokinetics and oral bioavailability in vivo.[329, 336]
3-EGCGEnhanced in vitro antitumor activity.[337]
BrucineImproved absorption and oral bioavailability, enhanced targeting, and reduced side effects in vivo.[338, 339]

QuercetinPhytosomeEnhanced membrane permeability, sustained and controlled release.
Enhanced absorption, oral bioavailability, and bioefficacy.
Kaempferol[101]
Isorhamnetin
Silybin[98, 99]
3-EGCG[102]
Quercetin[100]

β-ElemeneMicroemulsionsIncreased water solubility and permeability and improved oral bioavailability.[131]
Hydroxysafflor yellow A[130]
Puerarin[127, 340]

BaicalinSEDSEnhanced stability, oral bioavailability, and targeting effects in vitro and in vivo.[134]

CurcuminSMEDSEnhanced stability, oral bioavailability, and targeting effects in vitro and in vivo. [341]
Indirubin[88]
Hydroxysafflor yellow A[143, 144]
Gentiopicrin[341]
Lutein[342]
Apigenin[343]
Nobiletin[137]
Oridonin[139]
Silymarin[140]
Puerarin[344]
Hesperidin[345]
Berberine hydrochloride (BBH)[346]

MorinSNEDSEnhanced stability, oral bioavailability, and targeting effects in vitro and in vivo. [145]
Curcumin[347]
Lutein[146]
Oleanolic acid[348]
Vinpocetine[349]

PuerarinSLNsImproved absorption and oral bioavailability and reduced side effects (irritation of GI mucous membrane) in vivo.[120, 121]
Triptolide[350]
Cantharidin[351]
Resveratrol[352]

SilymarinNLCsIncreased absorption and oral bioavailability in vivo.
Enhanced in vitro and in vivo antitumor activity.
[123]
Tripterine[124]
Curcumin