Optimized Polyethylene Glycolylated Polymer–Lipid Hybrid Nanoparticles as a Potential Breast Cancer Treatment
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 (PLN...
| Main Authors: | , , , , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-07-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/12/7/666 |
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| author | Salam Massadeh Mustafa E Omer Asmaa Alterawi Rizwan Ali Fayez H Alanazi Fares Almutairi Wejdan Almotairi Faris F Alobaidi Khulud Alhelal Mansour S Almutairi Abdulaziz Almalik Aiman A. Obaidat Manal Alaamery Alaa Eldeen Yassin |
| author_facet | Salam Massadeh Mustafa E Omer Asmaa Alterawi Rizwan Ali Fayez H Alanazi Fares Almutairi Wejdan Almotairi Faris F Alobaidi Khulud Alhelal Mansour S Almutairi Abdulaziz Almalik Aiman A. Obaidat Manal Alaamery Alaa Eldeen Yassin |
| author_sort | Salam Massadeh |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-10T18:27:58Z |
| format | Article |
| id | doaj.art-c35938661f2342e59056e8d2eec71079 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T18:27:58Z |
| publishDate | 2020-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-c35938661f2342e59056e8d2eec710792023-11-20T06:51:43ZengMDPI AGPharmaceutics1999-49232020-07-0112766610.3390/pharmaceutics12070666Optimized Polyethylene Glycolylated Polymer–Lipid Hybrid Nanoparticles as a Potential Breast Cancer TreatmentSalam Massadeh0Mustafa E Omer1Asmaa Alterawi2Rizwan Ali3Fayez H Alanazi4Fares Almutairi5Wejdan Almotairi6Faris F Alobaidi7Khulud Alhelal8Mansour S Almutairi9Abdulaziz Almalik10Aiman A. Obaidat11Manal Alaamery12Alaa Eldeen Yassin13Developmental 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 ArabiaCollege of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi ArabiaCollege of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi ArabiaMedical Research Core Facility and Platforms, King Abdullah International Medical Research Center (KAIMRC), National Guard Health Affairs (NGHA), P.O. Box 22490, Riyadh 11426, Saudi ArabiaCollege of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi ArabiaCollege of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi ArabiaCollege of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi ArabiaCollege of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi ArabiaCollege of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi ArabiaDevelopmental 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 ArabiaKACST-BWH Centre of Excellence for Biomedicine, Joint Centers of Excellence Program, King Abdulaziz City for Science and Technology (KACST), Riyadh 11442, Saudi ArabiaCollege of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi ArabiaDevelopmental 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 ArabiaCollege of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi ArabiaPurpose: 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.https://www.mdpi.com/1999-4923/12/7/666anastrozolepoly-caprolactonePEGylated-polymeric nanoparticlesDSC |
| spellingShingle | Salam Massadeh Mustafa E Omer Asmaa Alterawi Rizwan Ali Fayez H Alanazi Fares Almutairi Wejdan Almotairi Faris F Alobaidi Khulud Alhelal Mansour S Almutairi Abdulaziz Almalik Aiman A. Obaidat Manal Alaamery Alaa Eldeen Yassin Optimized Polyethylene Glycolylated Polymer–Lipid Hybrid Nanoparticles as a Potential Breast Cancer Treatment Pharmaceutics anastrozole poly-caprolactone PEGylated-polymeric nanoparticles DSC |
| title | Optimized Polyethylene Glycolylated Polymer–Lipid Hybrid Nanoparticles as a Potential Breast Cancer Treatment |
| title_full | Optimized Polyethylene Glycolylated Polymer–Lipid Hybrid Nanoparticles as a Potential Breast Cancer Treatment |
| title_fullStr | Optimized Polyethylene Glycolylated Polymer–Lipid Hybrid Nanoparticles as a Potential Breast Cancer Treatment |
| title_full_unstemmed | Optimized Polyethylene Glycolylated Polymer–Lipid Hybrid Nanoparticles as a Potential Breast Cancer Treatment |
| title_short | Optimized Polyethylene Glycolylated Polymer–Lipid Hybrid Nanoparticles as a Potential Breast Cancer Treatment |
| title_sort | optimized polyethylene glycolylated polymer lipid hybrid nanoparticles as a potential breast cancer treatment |
| topic | anastrozole poly-caprolactone PEGylated-polymeric nanoparticles DSC |
| url | https://www.mdpi.com/1999-4923/12/7/666 |
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