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. 2022 Jun 10:2022:4438518.
doi: 10.1155/2022/4438518. eCollection 2022.

PEGylated Protamine Letrozole Nanoparticles: A Promising Strategy to Combat Human Breast Cancer via MCF-7 Cell Lines

Muhammad Tafhim Khan  1 , Zia Uddin  1 , Muhammad Arslan Javed  2 , Nabi Shah  1 , Hamid Bashir  3 , Ahson Jabbar Shaikh  4 , Muhammad Shahid Riaz Rajoka  5 , Muhammad Imran Amirzada  1 , Muhammad Hassham Hassan Bin Asad  1   6   7
Affiliations

PEGylated Protamine Letrozole Nanoparticles: A Promising Strategy to Combat Human Breast Cancer via MCF-7 Cell Lines

Muhammad Tafhim Khan et al. Biomed Res Int. .

Abstract

The objective of the study was to develop PEGylated protamine letrozole nanoparticles to combat human breast cancer by modifying the release pattern of letrozole. Breast cancer is amongst the most prevalent diseases in women due to overactivity of human epidermal growth factor receptor 2 (HER2). PEG-protamine letrozole nanoparticle formulation was designed and optimized to alter the release pattern of the drug. The size, morphology, and structure of PEG-protamine letrozole NP were characterized by FTIR, XRD, Zetasizer, and SEM analysis. The result showed the PEG-protamine letrozole nanoparticles were irregular in shape and have size ranging from 258 nm to 388 nm, polydispersity index 0.114 to 0.45, zeta potential of 11.2 mV, and entrapment efficiency 89.93%. XRD studies have confirmed that the crystal structure of letrozole has become amorphous. The drug release study maintained the prolonged release for 72 hours. Moreover, the PEG-protamine letrozole NPs displayed a strong anticancer action compared to MCF-7 cells with an IC50 70 μM for letrozole and 50 μM for PEG-protamine letrozole NPs. Overall, our results indicate that letrozole PEG-protamine NPs alter the release profile of letrozole, which could be an excellent approach for overcoming letrozole resistance in human breast cancer.

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Conflict of interest statement

The authors have found no conflict of interest.

Figures

Figure 1
Figure 1
FTIR spectra of protamine, polyethylene glycol (PEG), PEG-protamine complex (PPC), letrozole, blank nanoparticles, and letrozole-loaded nanoparticles.
Figure 2
Figure 2
XRD analysis for letrozole, blank nanoparticles, and drug-loaded PPC.
Figure 3
Figure 3
Particle size and zeta potential of PGE-letrozole formulations.
Figure 4
Figure 4
Scanning electron microscope (SEM) analysis of nanoparticle formulations F1-F4.
Figure 5
Figure 5
In vitro release study of letrozole from PEG-protamine complex nanoparticles at different pH (6.8 and 7.4).
Figure 6
Figure 6
In vitro cytotoxicity assay of letrozole and PEG-protamine letrozole nanoparticle on human breast cells MCF-7.
See this image and copyright information in PMC

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