A review on lipid-based nanocarriers mimicking chylomicron and their potential in drug delivery and targeting infectious and cancerous diseases

Elnady, Rana E.; Amin, Maha M.; Zakaria, Mohamed Y.

doi:10.1186/s41120-023-00080-x

AAPS Open

Table 4 Therapeutic applications of EMLs in cancer

From: A review on lipid-based nanocarriers mimicking chylomicron and their potential in drug delivery and targeting infectious and cancerous diseases

S. No	Drug	Indication	Components	Method	PS	EE%	Animal or cell line model	Purpose of study	Outcomes	Ref
1	Piceatannol (PIC)	Colorectal cancer	Chol, tristearin, Lipoid ®S100 (hydrogenated soybean lecithin),	TFH	125.45 nm	93.14%	Colorectal cancer cells HCT 116	Development of EMLs and assessment of anti-tumor activity	• PIC-EMLs exhibited higher cell death against colon cancer cells than the raw PIC • PIC-EMLs decreased the IC50 by one-half than raw PIC	Alhakamy et al. 2020)
2	Baicalin	Lymphoma	CA, Lipoid S100 (l-α-PC), Chol	TFH	240.1 ± 1.07 nm	98.44 ± 0.06%	Male Sprague–Dawley rats	Lymphatic targeting ability of EMLs by chylomicron flow blockage assay	• Improved the bioavailability twofold compared with free drug	Rizk and Elsheikh 2021)
3	Methotrexate	Intestine lymphatic carcinoma	Soya lecithin, CA	TFH	160.3 ± 10.2 nm	72.8 ± 6.5%	Albino rats	Comparing pharmacokinetic parameters between plain and emulsomal methotrexate	• Relative bioavailability is enhanced by 5.7 times than free drug, with better absorption and longer residence duration in lymphatics	Paliwal et al. 2009a)
4	Sorafenib	Hepatocellular carcinoma	Lecithin, GMS	TFH	127 nm	95%	Hepatocellular carcinoma cells of HepG2	Cell cycle analysis comparing sorafenib-targeting EMLs, non-targeting EMLs, and free sorafenib	• Octreotide-PEGylated TMC-EMLs reduced the IC50 of free sorafenib from 6.265 µg/ml to 0.256 µg/ml on HepG2 cells	Varshosaz et al. 2019)
5	Raloxifene HCl (RLX)	Breast cancer	Chol, Tripalmitin, Tristearin,), CA, PC (Lipoid 90H)	TFH	97.2 ± 1.8 to 247.1 ± 9.8 nm	98.9 ± 4.9%	Human breast cancer (MCF-7) cells	Development of EMLs and assessment of anti-tumor activity	• Controlled release profile, enhanced anti-proliferative and apoptotic activity against cancer cells more than free RLX	Aldawsari et al. 2021)
6	Febuxostat (FBX)	Colon cancer	PC (P90H), Chol, Tripalmitin	TFH	79.97 ± 0.98 to 200.17 ± 3.98 nm	-	Human colorectal carcinoma (HCT 116) cells	Development of EMLs and assessment of anti-tumor activity	• Enhanced all parameters related to the toxic potential of the FBX towards colon cancer	Fahmy et al. 2020)
7	Fluvastatin	Prostate cancer	PC (P90H), Chol, Tripalmitin	TFH	85.12 nm	93.74%	PC3 prostate cancer cells	Development of EMLs and assessment of anti-tumor activity	• Compared to the free drug, significant anti-proliferative activity was explained by cell cycle arrest action	Alhakamy et al. 2021)
8	Simvastatin	Breast cancer	PC (P90H), Chol, Tripalmitin	TFH	112.42 ± 2.1 nm	94.34 ± 1.11%	MCF-7 breast cancer cells	Assessment of cytotoxic activities of simvastatin	• Slow drug release with significant cell death-inducing activity against MCF-7 cancer cells compared to pure SMV	Awan et al. 2020)
9	Curcumin	Hepatocellular carcinoma	Tripalmitin, Chol, DPPC	High-pressure extrusion	286 nm	-	HepG2 human liver carcinoma cell line	Assessment of cell viability, apoptosis, and cell cycle	• Prolongation of biological activity and demonstrated therapeutic efficacy compared to free curcumin against HepG2 in vitro	Ucisik et al. 2013a)
10	Curcumin	Human cancers	Tripalmitin, DPPC human IgG-Reagent Grade, anti-human IgG chain, Chol	High-pressure extrusion	291 ± 48 nm	-	-	Confirming selective targeting of tumor cells	• Exhibited a selective binding affinity for IgG which serves as a potential target in cancer therapy	Ucisik et al. 2015b)
11	Curcumin and Piperine	Colorectal Cancer	Tripalmitin, DPPC, Chol	TFH	184.21 and 248.76 nm, respectively	4.4 and 3.6%, respectively	HCT116 Colorectal Cancer	Anti-tumor activity assessment	• Combination of 7 µM Piperine EMLs and 25 µM Curcumin EMLs • Effectively inhibited cell proliferation • Achieved a fourfold increase in Caspase 3 level, with a sixfold increase in the level of apoptotic marker	Bolat et al. 2020)
12	Andrographolide	Non-Hodgkin’s lymphoma	PC (Lipoid® S100), Chol, CA	TFH	281.62 ± 1.73 nm	96.55% ± 0.25%	Sprague–Dawley male rats	Pharmacokinetics and Lymphatic Targeting Assessments	• Targeted delivery to the lymphatic system at a lower dose with fewer side effects • More than a sixfold increase in the rate and extent of absorption than the free drug	Elsheikh et al. 2021)
13	Morin hydrate	Leukemia	PC (P80H), GMS	TFH	271.7 ± 4.86 nm	79.95 ± 0.63%	Adult male Wistar rats	Pharmacokinetics and anti-tumor activity assessments	• A significant increase in all pharmacokinetic parameters compared to the free drug suspension • A significant decrease in cancer cell viability in MH-EMLs compared to the unmedicated one	Kamel et al. 2022)
13	Morin hydrate	Leukemia	PC (P80H), GMS	TFH	271.7 ± 4.86 nm	79.95 ± 0.63%	Acute monocytic leukemia (AML) cell line (Kasumi-1)	Pharmacokinetics and anti-tumor activity assessments		Kamel et al. 2022)

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