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pH-responsive niosome-based nanocarriers of antineoplastic agents
Viliana Gugleva1, Rositsa Mihaylova2, Georgi Momekov2
1Department of Pharmaceutical Technologies, Faculty of Pharmacy, Medical University of Varna "Prof. Dr Paraskev Stoyanov" 84 Tsar Osvoboditel Str. 9000 Varna Bulgaria.
RSC Advances
|April 12, 2024
Summary
Novel pH-responsive nanocarriers were developed using modified niosomes. These nanocarriers show enhanced drug release in tumors and improved anticancer activity, offering a promising approach for targeted cancer therapy.
Area of Science:
- Nanotechnology
- Materials Science
- Pharmacology
Background:
- Tumor microenvironments exhibit distinct pH differences compared to healthy tissues.
- pH-responsive drug delivery systems can exploit these differences for targeted therapy.
- Niosomes are versatile nanocarriers with potential for drug encapsulation and delivery.
Purpose of the Study:
- To develop novel pH-responsive nanocarriers by modifying conventional niosomes.
- To investigate the physicochemical properties and drug release characteristics of these nanocarriers.
- To evaluate the in vitro cytotoxicity and proapoptotic effects of curcumin-loaded nanocarriers against cancer cell lines.
Main Methods:
- Niosomal vesicles were prepared using the thin film hydration method with Span 60, Span 60/Tween 60, and cholesterol.
- Hexadecyl-poly(acrylic acid) copolymers (HD-PAA) were used to modify niosomes at varying concentrations.
- Physicochemical properties (hydrodynamic diameter, zeta potential, morphology) and pH-responsiveness were assessed.
- Curcumin and calcein were loaded as model drugs to evaluate encapsulation and release.
- Cytotoxicity assays were performed on human malignant cell lines (MJ, T-24, HUT-78).
Main Results:
- The formulation with Span 60/Tween 60/cholesterol/2.5% HD-PAA exhibited optimal physicochemical characteristics.
- Optimal formulation showed a hydrodynamic diameter of 302 nm and a zeta potential of -22.1 mV.
- High curcumin entrapment efficiency of 83% was achieved.
- pH-dependent drug release was observed, with enhanced release at lower pH values.
- Niosomal curcumin demonstrated improved cytotoxic and proapoptotic activity compared to free curcumin.
Conclusions:
- Modified niosomes with HD-PAA copolymers represent effective pH-responsive nanocarriers.
- These nanocarriers facilitate targeted drug release in acidic tumor environments.
- Niosomal curcumin exhibits enhanced anticancer efficacy, suggesting potential for improved cancer treatment.
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