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Open AccessArticle

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

1
Developmental Medicine Department, King Abdullah International Medical Research Center, King Saud Bin Abdulaziz University for Health Sciences, King Abdulaziz Medical City, Ministry of National Guard-Health Affairs (MNG-HA), Riyadh 11481, Saudi Arabia
2
KACST-BWH Centre of Excellence for Biomedicine, Joint Centers of Excellence Program, King Abdulaziz City for Science and Technology (KACST), Riyadh 11442, Saudi Arabia
3
College of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi Arabia
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King Abdullah International Medical Research Center (KAIMRC), Riyadh 11481, Saudi Arabia
5
Medical Research Core Facility and Platforms, King Abdullah International Medical Research Center (KAIMRC), National Guard Health Affairs (NGHA), P.O. Box 22490, Riyadh 11426, Saudi Arabia
6
Life Sciences and Environment Research Institute, King Abdulaziz City for Science and Technology (KACST), Riyadh 11442, Saudi Arabia
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2020, 12(7), 666; https://doi.org/10.3390/pharmaceutics12070666
Received: 26 March 2020 / Revised: 28 April 2020 / Accepted: 3 July 2020 / Published: 15 July 2020
(This article belongs to the Special Issue Biocompatible Materials in Drug Delivery System in Oncology)
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. View Full-Text
Keywords: anastrozole; poly-caprolactone; PEGylated-polymeric nanoparticles; DSC anastrozole; poly-caprolactone; PEGylated-polymeric nanoparticles; DSC
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MDPI and ACS Style

Massadeh, S.; Omer, M.E; Alterawi, A.; Ali, R.; Alanazi, F.H; Almutairi, F.; Almotairi, W.; Alobaidi, F.F; Alhelal, K.; Almutairi, M.S; Almalik, A.; Obaidat, A.A.; Alaamery, M.; Yassin, A.E. Optimized Polyethylene Glycolylated Polymer–Lipid Hybrid Nanoparticles as a Potential Breast Cancer Treatment. Pharmaceutics 2020, 12, 666. https://doi.org/10.3390/pharmaceutics12070666

AMA Style

Massadeh S, Omer ME, Alterawi A, Ali R, Alanazi FH, Almutairi F, Almotairi W, Alobaidi FF, Alhelal K, Almutairi MS, Almalik A, Obaidat AA, Alaamery M, Yassin AE. Optimized Polyethylene Glycolylated Polymer–Lipid Hybrid Nanoparticles as a Potential Breast Cancer Treatment. Pharmaceutics. 2020; 12(7):666. https://doi.org/10.3390/pharmaceutics12070666

Chicago/Turabian Style

Massadeh, Salam; Omer, Mustafa E; Alterawi, Asmaa; Ali, Rizwan; Alanazi, Fayez H; Almutairi, Fares; Almotairi, Wejdan; Alobaidi, Faris F; Alhelal, Khulud; Almutairi, Mansour S; Almalik, Abdulaziz; Obaidat, Aiman A.; Alaamery, Manal; Yassin, Alaa E. 2020. "Optimized Polyethylene Glycolylated Polymer–Lipid Hybrid Nanoparticles as a Potential Breast Cancer Treatment" Pharmaceutics 12, no. 7: 666. https://doi.org/10.3390/pharmaceutics12070666

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