Novel Anticancer Triple Formula Based on Aptamer-Conjugated PEGylated Nanoliposomes

Background Cancer remains a leading cause of death worldwide, necessitating the development of affordable and innovative therapies to reduce its human and economic burden. Objectives In this study, we aimed to develop a synergistic anticancer formula encapsulated in nanoliposomes to enhance efficacy...

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Main Authors: Ali Al-Samydai PhD, Hamdi Nsairat PhD, Moath Alqaraleh PhD, Maha N. Abu Hajleh PhD, Areej Jaber PhD, Lidia Al-Halaseh PhD, Hanan Azzam MS, Qasim Khalid Alazzawi PhD, Israa Al-Ani PhD, Simone Carradori PhD, Walhan Alshaer PhD
Format: Article
Language:English
Published: SAGE Publishing 2025-07-01
Series:Technology in Cancer Research & Treatment
Online Access:https://doi.org/10.1177/15330338251356548
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author Ali Al-Samydai PhD
Hamdi Nsairat PhD
Moath Alqaraleh PhD
Maha N. Abu Hajleh PhD
Areej Jaber PhD
Lidia Al-Halaseh PhD
Hanan Azzam MS
Qasim Khalid Alazzawi PhD
Israa Al-Ani PhD
Simone Carradori PhD
Walhan Alshaer PhD
author_facet Ali Al-Samydai PhD
Hamdi Nsairat PhD
Moath Alqaraleh PhD
Maha N. Abu Hajleh PhD
Areej Jaber PhD
Lidia Al-Halaseh PhD
Hanan Azzam MS
Qasim Khalid Alazzawi PhD
Israa Al-Ani PhD
Simone Carradori PhD
Walhan Alshaer PhD
author_sort Ali Al-Samydai PhD
collection DOAJ
description Background Cancer remains a leading cause of death worldwide, necessitating the development of affordable and innovative therapies to reduce its human and economic burden. Objectives In this study, we aimed to develop a synergistic anticancer formula encapsulated in nanoliposomes to enhance efficacy and minimize side effects. Additionally, we explored the effect of aptamer conjugation on the efficacy and stability of the formula. Methods The Etoricoxib-β-cyclodextrin complex was prepared using the kneading method, and nanoliposomes were developed via thin film hydration. The AS1411 aptamer was conjugated to the nanoliposomes to target nucleolin, a protein overexpressed in cancer cells. The etoricoxib-β-cyclodextrin complex was characterized using proton nuclear magnetic resonance, and various liposome properties, including size, encapsulation efficiency, and stability, were optimized. The release profiles of the active compounds were evaluated using high-performance liquid chromatography, and their cytotoxicity was assessed in human cancer cell lines. Results The nanoliposomes co-loaded with the three agents and their aptamer-conjugated counterpart showed optimal characteristics, with particle sizes of 133.3 ± 1.45 nm and 174.8 ± 4.78 nm, and zeta potentials of −15.26 ± 1.80 mV and −15.66 ± 2.57 mV, respectively. The encapsulation efficiencies were 88.63% (raloxifene), 41.73% (etoricoxib), and 39.26% (naringin) without the aptamer, and 81.99%, 36.66%, and 38.33%, respectively, with the aptamer. The IC 50 of the formula for the three co-loaded agents was 167.4 µg/mL for A549 cells and 2.6 µg/mL for MCF-7 cells. Cytotoxicity was further enhanced using their aptamer conjugate, particularly against the MDA-MB-231 cell line. Conclusion The novel triple-drug-loaded, aptamer-conjugated nanoliposome formula may be a future cancer treatment strategy.
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series Technology in Cancer Research & Treatment
spelling doaj-art-68b098d11bfa4830bcbf0b3badee48ce2025-08-20T03:29:26ZengSAGE PublishingTechnology in Cancer Research & Treatment1533-03382025-07-012410.1177/15330338251356548Novel Anticancer Triple Formula Based on Aptamer-Conjugated PEGylated NanoliposomesAli Al-Samydai PhD0Hamdi Nsairat PhD1Moath Alqaraleh PhD2Maha N. Abu Hajleh PhD3Areej Jaber PhD4Lidia Al-Halaseh PhD5Hanan Azzam MS6Qasim Khalid Alazzawi PhD7Israa Al-Ani PhD8Simone Carradori PhD9Walhan Alshaer PhD10 Faculty of Pharmacy, Pharmacological and Diagnostic Research Center, , Amman, Jordan Faculty of Pharmacy, Pharmacological and Diagnostic Research Center, , Amman, Jordan Department of Medical Laboratory Sciences, Faculty of Science, , Al-Salt, Jordan Department of Cosmetic Science, Faculty of Allied Medical Sciences, Pharmacological and Diagnostic Research Centre, , Amman, Jordan Faculty of Pharmacy, Pharmacological and Diagnostic Research Center, , Amman, Jordan Department of Pharmaceutical Chemistry, Faculty of pharmacy, , Al-Karak, Jordan Faculty of Pharmacy, Pharmacological and Diagnostic Research Center, , Amman, Jordan Faculty of Pharmacy, Pharmacological and Diagnostic Research Center, , Amman, Jordan Faculty of Pharmacy, Pharmacological and Diagnostic Research Center, , Amman, Jordan Department of Pharmacy “G. d'Annunzio”, University of Chieti-Pescara, Chieti, Italy Cell Therapy Center, , Amman, JordanBackground Cancer remains a leading cause of death worldwide, necessitating the development of affordable and innovative therapies to reduce its human and economic burden. Objectives In this study, we aimed to develop a synergistic anticancer formula encapsulated in nanoliposomes to enhance efficacy and minimize side effects. Additionally, we explored the effect of aptamer conjugation on the efficacy and stability of the formula. Methods The Etoricoxib-β-cyclodextrin complex was prepared using the kneading method, and nanoliposomes were developed via thin film hydration. The AS1411 aptamer was conjugated to the nanoliposomes to target nucleolin, a protein overexpressed in cancer cells. The etoricoxib-β-cyclodextrin complex was characterized using proton nuclear magnetic resonance, and various liposome properties, including size, encapsulation efficiency, and stability, were optimized. The release profiles of the active compounds were evaluated using high-performance liquid chromatography, and their cytotoxicity was assessed in human cancer cell lines. Results The nanoliposomes co-loaded with the three agents and their aptamer-conjugated counterpart showed optimal characteristics, with particle sizes of 133.3 ± 1.45 nm and 174.8 ± 4.78 nm, and zeta potentials of −15.26 ± 1.80 mV and −15.66 ± 2.57 mV, respectively. The encapsulation efficiencies were 88.63% (raloxifene), 41.73% (etoricoxib), and 39.26% (naringin) without the aptamer, and 81.99%, 36.66%, and 38.33%, respectively, with the aptamer. The IC 50 of the formula for the three co-loaded agents was 167.4 µg/mL for A549 cells and 2.6 µg/mL for MCF-7 cells. Cytotoxicity was further enhanced using their aptamer conjugate, particularly against the MDA-MB-231 cell line. Conclusion The novel triple-drug-loaded, aptamer-conjugated nanoliposome formula may be a future cancer treatment strategy.https://doi.org/10.1177/15330338251356548
spellingShingle Ali Al-Samydai PhD
Hamdi Nsairat PhD
Moath Alqaraleh PhD
Maha N. Abu Hajleh PhD
Areej Jaber PhD
Lidia Al-Halaseh PhD
Hanan Azzam MS
Qasim Khalid Alazzawi PhD
Israa Al-Ani PhD
Simone Carradori PhD
Walhan Alshaer PhD
Novel Anticancer Triple Formula Based on Aptamer-Conjugated PEGylated Nanoliposomes
Technology in Cancer Research & Treatment
title Novel Anticancer Triple Formula Based on Aptamer-Conjugated PEGylated Nanoliposomes
title_full Novel Anticancer Triple Formula Based on Aptamer-Conjugated PEGylated Nanoliposomes
title_fullStr Novel Anticancer Triple Formula Based on Aptamer-Conjugated PEGylated Nanoliposomes
title_full_unstemmed Novel Anticancer Triple Formula Based on Aptamer-Conjugated PEGylated Nanoliposomes
title_short Novel Anticancer Triple Formula Based on Aptamer-Conjugated PEGylated Nanoliposomes
title_sort novel anticancer triple formula based on aptamer conjugated pegylated nanoliposomes
url https://doi.org/10.1177/15330338251356548
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