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

Table 6

Overview of lipid and nonlipid formulations, which have been designed to administer phytochemicals by parental and topical routes.

Phytochemical	Lipid-based formulation		Effect of formulation	Admin. route	Ref.
	Type	Subcategory
Curcumin	LBDS	NLCs	Enhanced stability and brain targeting in vivo.	Intraperitoneal	[353]
Baicalein	LBDS	Tocol-NLCs			[354]
β-Elemene		NLCs	Less irritating and toxic and enhanced bioavailability and antitumor efficacy in vivo.		[355]
Bufadienolides			Reduced toxicity and improved pharmacokinetic profile in vivo.	Intravenous	[356]
Breviscapine		Ionic-complex-based NLCs	Sustained-release and protection against liver enzyme degradation in vivo.		[357]
Berberine		DQA-PEG2000-DSPE liposomes	Overcome multidrug resistance in vivo.		[358]
Quercetin	LBDS	MEs		Transdermal	[158]
Genistein			Increased permeation and skin retention.		[159]
Chlorogenic acid			Efficient systemic distribution in vivo.		[160]
Resveratrol
Curcumin		PEG liposomes	Increased stability and anti-inflammatory effects in vivo		[359]
Bufadienolides		Poloxamer-liposomes	Reduced toxicity and enhanced antitumor efficacy in vivo.		[360]
Ligustrazine phosp.		Ethosomes	Enhanced skin permeation in vitro and bioactivity in vivo.		[152]
Apigenin			Enhanced anti-inflammatory effects in vivo.		[361]
Curcumin		NLCs	Enhanced antitumor activity and brain targeting in vitro.	Intranasal	[362]
Tetrandrine		Charged SLNs	Reduced irritation of eye mucous membrane in vivo.	Ocular	[363]
3-ECGC	Inorganic carriers	Gold NPs	Enhanced efficacy and reduced toxicity in vivo.	Intratumoral injection	[155]
Curcumin	PBDS	Dextran sulfate-chitosan NPs	Controlled release and targeted effect against tumor cells in vitro.	Intravenous	[364]
Curcumin		Chitosan/PBCA NPs	In vivo anticancer effect on hepatic tumor cells.		[365]
Trans-resveratrol		Chitosan-NPs	Higher in vivo liver targeting effect and in vitro cytotoxicity on hepatic cancer cells.		[366–368]
Oridonin		Galactosylated chitosan NPs	Enhanced targeting and binding to the specific site of action (liver).
Artemisinin	PBDS	Polymeric micelles; Targeted polymeric micelles	Achieving site-specific cell targeting and enhancing intracellular drug accumulation.	Intraperitoneal	[369]
Resveratrol		Transferrin modified PEG-PLA conjugate	Cellular uptake, in vivo biodistribution, and antitumor activity. Targeted therapy of glioma.		[370]
Bufalin		Biotinylated chitosan NPs	Enhanced targeting and binding to the specific site of action breast carcinoma.		[371]
Quercetin	PBDS	Lecithin-chitosan NPs	In vitro and in vivo enhanced skin permeation.	Topical	[371]

PEG: polyethylene glycol; DQA: dequalinium; DSPE: polyethylene glycol-distearoylphosphatidylethanolamine.
PBCA: poly(butyl cyanoacrylate).
PLA: polylactic acid.