Novel Nanotherapeutic Systems Based on PEGylated Squalene Micelles for Enhanced In Vitro Activity of Methotrexate and Cytarabine

Nanomedicine has garnered significant attention due to the advantages it offers in the treatment of cancer-related disorders, some of the deadliest diseases affecting human lives. Conventional medication formulations often encounter issues of instability or insolubility in biological environments, r...

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Bibliographic Details
Published in:Polymers 2023-11, Vol.15 (21), p.4225
Main Authors: Craciun, Bogdan-Florin, Sandu, Isabela-Andreea, Peptanariu, Dragos, Pinteala, Mariana
Format: Article
Language:English
Subjects:
Anticancer properties
Bioavailability
Biocompatibility
Biological effects
Cancer
Care and treatment
Charge efficiency
Clinical trials
Computer industry
Cytarabine
Drugs
Encapsulation
Health aspects
Lipids
Methotrexate
Micelles
NMR
Nuclear magnetic resonance
Phosphates
Physiology
Potassium
Saline solutions
Sodium
Software
Surface charge
Surface stability
Sustained release
Toxicity
Ultrasonic imaging
Ultrasonic testing
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Summary:Nanomedicine has garnered significant attention due to the advantages it offers in the treatment of cancer-related disorders, some of the deadliest diseases affecting human lives. Conventional medication formulations often encounter issues of instability or insolubility in biological environments, resulting in low bioavailability. Nanocarriers play a crucial role in transporting and safeguarding drugs at specific sites of action, enabling gradual release under particular conditions. This study focuses on methotrexate (MTx) and cytarabine (Cyt), essential antitumoral drugs, loaded into PEGylated squalene micellar structures to enhance therapeutic effectiveness and minimize drawbacks. The micelles were prepared using ultrasound-assisted methods in both water and phosphate buffer saline solutions. Evaluation of drug-loaded micelles encompassed parameters such as particle size, colloidal stability, surface charge, morphology, encapsulation efficiency, drug loading capacity, and in vitro release profiles under simulated physiological and tumoral conditions. In vitro cell inhibition studies conducted on MCF-7 and HeLa cell lines demonstrated higher antitumoral activity for the drug-encapsulated micelles compared to free drugs. The encapsulation effectively addressed the burst effect, providing sustained release for at least 48 h while enhancing the drug’s protection under physiological conditions.
ISSN:2073-4360
2073-4360
DOI:10.3390/polym15214225