Journal of Oncology

Review Article

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

Table 4

Overview of nonlipid formulations, which have been designed to administer phytochemicals by oral route.


Active ingredient	Lipid-based formulation		Effect of formulation	Ref.
	Type	Subcategory

Curcumin	PBDS	PLGA^a-NPs	Overcome multidrug resistance and increased oral bioavailability in vivo.	[320]
Silymarin			In vitro sustained release and enhanced cytotoxicity.	[321]
Curcumin		Hydroxypropyl cellulose NPs	Temperature-dependent release in vitro.	[322]
Puerarin		Dendrimers	Increased in vitro oral bioavailability and reduced side effects.	[323, 324]
Curcumin
Resveratrol
Genistein
Podophyllotoxin
Curcumin		Hyaluronic acid conjugate	Improved water solubility, stability, and antitumoral activity in vitro.	[325]
		Alginate conjugate	Higher water solubility, stability, and cytotoxicity in vitro.	[326]

Rutin	CD inclusion complexes	α-CD, β-CD, HP-β-CD, and DM-β-CD^b	Improved water solubility and stability, increasing the oral bioavailability and bioefficacy.	[327]
3-EGCG				[328]

Silymarin (Silybum marianum)	Inorganic nanocarriers	Porous silica nanoparticles (PSN)	Sustained release and enhanced oral bioavailability in vivo.	[321]
Silybin meglumine				[329]

Resveratrol	Hybrid nanocarriers	TCC^c- liposomes	Improved absorption and oral bioavailability and reduced side effects in vivo In vitro controlled release and in vivo enhanced targeting and reduced side effects Overcome multidrug resistance. Enhanced in vitro and in vivo antitumor activity.	[330]
		DQA-PEG₁₉₃₀-DSPE^a liposomes		[153]
Vincristine		Dextran-sulfate-SLNs		[331]
		PLGA-PEG-R7^a NPs		[332]
Tripterine		CPP^a-NLCs		[118]

Silymarin	Other novel nanocarriers	Liquid crystalline nanocarrier	Sustained release. Improved water solubility, oral bioavailability, and biological activity (active targeting-liver) in vivo.	[333]
Quercetin		Folate-modified lipid nanocapsules		[334]
Tetrandrine		Lipid nanocapsules		[335]

PLGA: poly(lactic-co-glycolic acid); PEG: polyethylene glycol; R7 is a cell-penetrating peptide; DQA: dequalinium; DSPE: polyethylene glycol-distearoylphosphatidylethanolamine; R7 is a cell-penetrating peptide (CPP).
^bα/β-CD: alpha/beta-cyclodextrin; HP-β-CD: hydroxypropyl-β-cyclodextrin; DM-β-CD: dimethyl-β-cyclodextrin.
^cTCC: N-trimethyl chitosan chloride-coated.