Skip to main content
. 2022 Dec 3;14(12):2706. doi: 10.3390/pharmaceutics14122706

Table 4.

In Vitro tested SLN-based TKI formulations.

TKI Ingredients Particle Size Tested Human Cancer Cell Lines Benefits Refs.
brigatinib stearic acid, soya lecithin 176–787 nm lung adenocarcinoma A549 cells sustained release
↑ anticancer effect
[171]
gefitinib Pluronic® F127, lecithin, polyethylene glycol 2000, stearic acid, cholesterol, glucosamine ca. 187 nm lung adenocarcinoma A549 cells ↑ anticancer effect [172]
erlotinib Pluronic® F68, Transcutol®-P, glycerol monostearate 300–800 nm lung adenocarcinoma A549 cells sustained release
↑ anticancer effect
[173]
erlotinib Compritol® ATO 888, Tween® 80, Pluronic® 407 <100 nm lung adenocarcinoma A549 cells ↑ anticancer effect [174]
erlotinib 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(poly- ethylene glycol)-2000], hydrogenated soya phosphatidylcholine, polycaprolactone ca. 170 nm lung adenocarcinoma A549 cells sustained release
↑ anticancer effect
[175]
erlotinib+ paclitaxel Pluronic® 188, methoxy- poly(ethylene glycol)-b- poly(L-aspartic acid sodium, soya lecithin, glyceryl monostearate, didodecyldimethylammonium bromide ca. 195 nm lung adenocarcinoma NCI-H23 cells pH-dependent and sustained release
induction of apoptosis
↑ anticancer effect
[176]
imatinib glyceryl palmitostearate, quillaja saponin, hyaluronic acid ca. 92 nm MCF-7 breast cancer cells sustained release
CD44 targeting
↑ cellular uptake
↑ anticancer effect
[177]
sorafenib 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(poly- ethylene glycol)-2000], folic acid, chitosan, chondroitin sulfate ca. 178 nm hepatocarcinoma SMMC-7721 cells sustained release
induction of apoptosis
↑ anticancer effect
[178]
sorafenib thymidine 3′-(1,2-dipalmitoyl-sn- glycero-3-phosphate), 2′,3′-dioleyl- 5′-deoxy-5′-trimethyl-ammonium-uridine ca. 200 nm hepatocarcinoma HuH7, HepG2 cells
breast cancer MDA-MB-134, T-47D cells
↑ anticancer effect [179]
sorafenib poly(D,L-lactic-co-glycolic acid), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(poly- ethylene glycol)-2000], lecithin ca. 190 nm breast cancer MDA-MB-231 cells
prostate cancer PC3-MM2 cells
sustained release
long-term stability
↑ anticancer effect
[180]
sorafenib + MK-siRNA 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[maleimide- (polyethylene glycol)-2000], cholesterol, polyethylenimine, 1-methyl-4,4-bis[(9Z,12Z)-9,12-octadecadien-1-yloxy] piperidine, egg phosphatidylcoline, SP94 targeting peptide 140–160 nm HepG2 hepatocellular carcinoma cells specific delivery
targeting
↑ drug accumulation
↑ anticancer effect
[181]
sorafenib + selumetinib 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine, 1,2-distearoyl-sn- glycero-3-phosphoethanolamine- N-[maleimide(polyethylene glycol)-2000], poly(D,L-lactic-co- glycolic acid), polyvinyl alcohol, cholesterol, N-acetylgalactos- amine ca. 170 nm hepatocellular carcinoma HepG2, Hep3B cells
glioblastoma DBTRG-05MG cells
induction of apoptosis
↑ anticancer effect
[182]
sorafenib + paclitaxel distearoyl phosphoethanolamine-polyethylene glycol, (1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy- (poly(ethylene glycol)-2000], cetyl palmitate, Pluronic® F68, polyvinyl alcohol ca. 200 nm human glioblastoma U87-MG cells
lung adenocarcinoma A549 cells
↑ drug accumulation
↑ cellular uptake
avoided drug efflux pumps
↑ anticancer effect
[183]
sorafenib + iron oxide cetyl palmitate, Tween® 80, EMG1300 (iron oxide with surfactant) ca. 420 nm HepG2 hepatocellular carcinoma cells magnetically driven accumulation
↑ drug accumulation
↑ cellular uptake
↑ anticancer effect
[184]
sunitinib Roghan Kermanshahi Ghee oil, fat tail sheep, dioctyl sulfosuccinate sodium salt, chitosan, gum tragacanth 110–156 nm acute myeloid leukemia THP-1 cells sustained release
↑ anticancer effect
[185]
sunitinib Phospholipon® 90H, soya lecithin, polyvinyl alcohol, chitosan ca. 439 nm MCF-7 breast cancer cells induction of apoptosis
↑ anticancer effect
[186]
afatinib (1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy- (poly(ethylene glycol)-2000], poly(D,L-lactic-co-glycolic acid), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy- (polyethylene glycol)-2000], lecithin 147–183 nm colorectal adenocarcinoma Caco-2 cells ↑ targeting
pH-sensitive penetration
↑ cellular uptake
↑ anticancer effect
[187]
afatinib 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[carboxy(poly- ethylene glycol)-2000], 1,2-di- stearoyl-sn-glycero-3-phospho- ethanolamine-N-[methoxy(poly- ethylene glycol)-2000], lecithin, tight junction-modulating short peptides FD7/CCD ca. 66 nm lung adenocarcinoma PC9 cells tight junctions perturbation
blood-brain barrier permeation
sustained release
↑ targeting
↑ anticancer effect
[188]
afatinib + cisplatin 1,2-dilauroyl-sn-glycero-3-phosphocholine, 1,2-distearoyl-sn-gly- cero-3-phosphoethanolamine- N-[amino(polyethylene glycol)- 2000], poly(DL-lactide- co-glycolide) ca. 138 nm nasopharyngeal carcinoma HONE1cells reduced cell viability
induction of apoptosis
synergistic efficacy
↑ anticancer effect
[189]