Optimized Polyethylene Glycolylated Polymer–Lipid Hybrid Nanoparticles as a Potential Breast Cancer Treatment

Abstract

Purpose: The aim of this work is to optimize a polyethylene glycolated (PEGylated) polymer–lipid hybrid nanoparticulate system for the delivery of anastrozole (ANS) to enhance its biopharmaceutical attributes and overall efficacy. Methods: ANS loaded PEGylated polymer–lipid hybrid nanoparticles (PLNPs) were prepared by a direct emulsification solvent evaporation method. The physical incorporation of PEG was optimized using variable ratios. The produced particles were evaluated to discern their particle size and shape, zeta-potential, entrapment efficiency, and physical stability. The drug-release profiles were studied, and the kinetic model was analyzed. The anticancer activity of the ANS PLNPs on estrogen-positive breast cancer cell lines was determined using flow cytometry. Results: The prepared ANS-PLNPs showed particle sizes in the range of 193.6 ± 2.9 to 218.2 ± 1.9 nm, with good particle size uniformity (i.e., poly-dispersity index of around 0.1). Furthermore, they exhibited relatively low zeta-potential values ranging from −0.50 ± 0.52 to 6.01 ± 4.74. The transmission electron microscopy images showed spherical shape of ANS-PLNPs and the compliance with the sizes were revealed by light scattering. The differential scanning calorimetry DSC patterns of the ANS PLNPs revealed a disappearance of the characteristic sharp melting peak of pure ANS, supporting the incorporation of the drug into the polymeric matrices of the nanoparticles. Flow cytometry showed the apoptosis of MCF-7 cell lines in the presence of ANS-PLNPs. Conclusion: PEGylated polymeric nanoparticles presented a stable encapsulated system with which to incorporate an anticancer drug (ANS) with a high percentage of entrapment efficiency (around 80%), good size uniformity, and induction of apoptosis in MCF-7 cells.

Development of Polymer-Assisted Nanoparticles and Nanogels for Cancer Therapy: An Update

“…MET-PLGA-PEG NPs also induced nuclei fragmentation and apoptosis in the treated cancer cells [122]. Other NPs which were reported to induce apoptosis in cancer cells are Nos-mPEG-PLGA NPs [117], NVA polymeric NPs [136], ANZ-PLNP NPs [118], 3A.1-loaded pH-sensitive NPs [132], CS-CPT-NPs [133], 5FU-Chrysin-PLGA-PEG-PLGA NPs [120], and Gemcitabine-loaded NPs conjugated with linoleic acid [143]. Nos-mPEG-PLGA NPs [117] has antiangiogenic properties while NVA polymeric NPs [136] inhibited cellular proliferation.…”

“…PEG is known to be highly versatile and with the addition of other polymers, it could efficiently enhance drug delivery. For example, DOX-IR780-loaded PEG-PCL NPs improved the delivery of DOX and IR780 to bladder cancer [116] while NOS-mPEG-PLGA NPs [117], ANZ-PLNPs [118], DOX-loaded PEGylated pH-sensitive NPs [119] improved the delivery of drugs to breast cancer. 5FU-Chrysin-PLGA-PEG-PLGA NPs were found to improve the delivery of the drug 5-FU and Chrysin in colon cancer [120].…”

Boosting the Skin Delivery of Curcumin Through Stearic Acid-Ethyl Cellulose Blend Hybrid Nanocarriers-Based Approach for Mitigating Psoriasis

“…The zeta potential of the prepared LPHNPs was measured by Zetasizer (Nano ZS, Malvern Instruments, UK) to assess the surface charge. In every cases, the freeze-dried LPHNPs were dispersed in distilled water (0.1% w/v) and subsequently analyzed [24].…”

In-vitro Investigation of Polymeric Lipid Hybrid Nanoparticles (Plhns) Of a Chemotherapeutic Drug for the Treatment of Glioblastoma Multiforme

“…As per Jiayi Gu et al (2020) studies, Astaxanthin encapsulated lipid-polymer hybrid nanoparticles has a greater effect against cisplatin induced toxicity [13]. As per Salam Massadeh et al (2020) research, Anastrozole was encapsulated by a polyethylene glycolated (PEGylated) polymer-lipid hybrid nanoparticulate device using a direct emulsification solvent evaporation process [14]. It has a better encapsulation efficacy and superior anticancer effects against MCF-7 cell lines.…”