Tamoxifen-loaded PLA/DPPE-PEG lipid-polymeric nanocapsules for inhibiting the growth of estrogen-positive human breast cancer cells through cell cycle arrest

Abstract

The strategy of drug encapsulation with biocompatible polymeric nanocapsules could be a promising approach to improve the delivery of poorly water-soluble drugs for cancer therapy. The aim of this study was to investigate the drug delivery of tamoxifen from biocompatible nanocapsules made of poly (D,L-lactide) (PLA) c o r e a n d 1 , 2 -d i p a l m i t o y l -s n -g l y c e r o -3phosphoethanolamine-N-[methoxy(polyethyleneglycol)-2000] (DPPE-PEG) shell in the treatment of breast cancer.The analytical techniques such as FTIR, XRD, SEM, and TEM were used to investigate the structure of nanocapsules. Tamoxifen drug encapsulation efficiency and loading percentages as well as release kinetics at different pH values and temperatures were used to confirm the appropriate performance of these novel nanocapsules. The maximum tamoxifen release occurred at 40°C, pH = 4. Based on the SEM and TEM images, the sizes of nanocapsules were between 57 and 159 nm. In order to investigate the anticancer effects and cytotoxicity of encapsulated tamoxifen in PLA/DPPE-PEG nanocapsules, the tetrazolium-based colorimetric (MTT) assay and cell cycle arrest analysis on MCF-7 breast cancer cell were performed. Also, cell cycle-related gene expressions of p53 and p21 in treated MCF-7 cells with tamoxifen-loaded PLA/DPPE-PEG nanocapsules were evaluated. The results of MTT cell proliferation experiments exhibited an increase in the cytotoxicity of tamoxifen nanocapsules on MCF-7 cell line compared with free tamoxifen. The 1.2-fold increase in the G1 stage compared with the control group in the cell cycle arrest protocol as well as the notable overexpression of p53 and p21 genes suggested that these nanocapsules arrested cell cycle in MCF-7 cells.

Folic Acid-decorated and PEGylated Graphene Quantum Dots as efficient Tamoxifen delivery system against breast cancer cells: in vitro studies

“…Therefore, the loaded TMXs on the FAconjugated GQDs nanocarriers were entered into MCF-7 cells with endocytosis via the folate receptor and TMX release process of TMX-FPG exhibited the controlled release behavior similar to the previous reports [42]. A comparison between the results of the present study and our ndings in the previous study showed that the toxicity of loaded TMX on FPGs was approximately 1.84 times higher than that of loaded TMX on PLA/DPPE-PEG lipid polymeric nano-capsules [43]. In addition, TMX-FPG showed 2.4 times more toxicity in the same exposure time on MCF-7 cells than loaded TMX on gelatin [44].…”

Layer-by-Layer Nanoparticles of Tamoxifen and Resveratrol for Dual Drug Delivery System and Potential Triple-Negative Breast Cancer Treatment

“…Additionally, the bands at 1735.52 cm −1 , 1582.84 cm −1 , and 1498.18 cm −1 were because of carboxylic C=O, aromatic C–C, and C=C ring stretching, respectively. Absorptions at 1299.47 cm −1 , 1235.25 cm −1 , and 1122.88 cm −1 were because of aromatic C–O stretching [ 55 ].…”

Dual-targeting and specific delivery of tamoxifen to cancer cells by modified magnetic nanoparticles using hyaluronic acid and folic acid

“…Hence, the use of lower TMX doses utilizing nano-based drug delivery systems can be beneficial to reducing drug toxicity and providing more efficient drug distribution [30] . For nano-carrier systems, drug loading efficiency is a significant parameter, especially for hydrophobic drugs with common side effects [31] . To reveal the potential of the Fe 3 O 4 -DPN-HA-FA NPs for the delivery of controlled TMX, the loading capacity and in vitro release amount were calculated.…”