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. 2022 Dec 3;14(12):2706. doi: 10.3390/pharmaceutics14122706

Table 3.

In Vitro tested liposomal TKI formulations.

TKI Ingredients Particle Size Tested Human Cancer Cell Lines Benefits Refs.
erlotinib lecithin, cholesterol, chitosan, anti-EGFR aptamer 70–200 nm lung adenocarcinoma PC-9, H-1975 cells long-term stability
effective targeting
↑ drug accumulation
↑ anticancer effect
[135]
imatinib sodium-deoxycholate, hyaluronic acid, lecithin ca. 159 nm HT-29 colorectal adenocarcinoma cellsColo-320-DMF colon carcinoma ↑ cellular uptake
↑ anticancer effect
[136]
imatinib + paclitaxel 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(polyethylene glycol)-2000], cholesterol, folic acid, phosphatidylcholine ca. 122 nm MCF-7 breast cancer cellsPC-3 prostate cancer cells ↑ internalization and accumulation in cancer cells
↑ anticancer effect
[137]
imatinib + tamoxifen 1,2-dipalmitoyl-sn-glycero-3-phosphocholine, monopalmitoyl-2-hydroxy- sn-glycero-3-phosphocholine, sorbitan monooleate ca. 168 nm MCF-7, MDA-MB-231 breast cancer cells synergistic inhibition
↑ anticancer effect
[138]
sorafenib maleimide-polyethylen glycol-N-hydroxysuccinimide, soya lecithin, trimethyl chitosan, octreotide ca. 127 nm HepG2 hepatocellular carcinoma cells sustained release
↑ accumulation in cancer cells
↑ anticancer effect
[139]
sorafenib 1,2-dipalmitoyl-sn-glycero-3-phosphocholine, hydrogenated soya phosphatidylcholine, cholesterol ca. 107 nm renal carcinoma cells sustained release
↑ cellular uptake
↑ anticancer effect
[140]
afatinib 1,2-distearoyl-sn-glycero-3-phosphocholine, 1,2-dioleoyl-sn-glycero- 3-phosphoethanolamine, 1,2-dioleoyl-sn-glycero-3-phosphocholine, 1,2-dioleoyl-3-trimethylammo- nium-propane chloride, cholesteryl hemisuccinate 46–57 nm lung adenocarcinoma H-1975, H-1650, HCC-827 cells ↑ tumor-targetability
induction apoptosis in H-1975 cells
↑ anticancer effect
[141]