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QbD Enabled Azacitidine Loaded Liposomal Nanoformulation and Its In Vitro Evaluation
Prashant Kesharwani1, Shadab Md2,3, Nabil A Alhakamy2,3
1Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, India.
Polymers
|January 16, 2021
Summary
This study developed azacitidine-loaded liposomes (AZA-LIPO) to improve breast cancer chemotherapy. The optimized AZA-LIPO showed enhanced cell uptake and effectiveness compared to free azacitidine, suggesting potential as a novel drug delivery system.
Area of Science:
- * Pharmaceutical Nanotechnology
- * Cancer Chemotherapy
- * Drug Delivery Systems
Background:
- * Azacitidine (AZA) is a DNA methyltransferase inhibitor used for myelodysplastic syndrome and breast cancer.
- * Poor aqueous solubility and low log P of AZA limit its efficacy due to inadequate cancer cell permeation and controlled release.
- * Development of advanced drug delivery systems is crucial to overcome AZA's limitations in cancer treatment.
Purpose of the Study:
- * To formulate and optimize azacitidine-loaded liposomes (AZA-LIPO) for enhanced breast cancer chemotherapy.
- * To evaluate the physicochemical properties, in vitro drug release, and cellular effects of AZA-LIPO.
- * To assess the potential of AZA-LIPO as an efficient anti-cancer drug delivery system.
Main Methods:
- * Liposomes encapsulating azacitidine (AZA-LIPO) were prepared using the thin-film hydration technique.
- * Formulations were optimized using Box-Behnken design (BBD).
- * Characterization included FTIR, DSC, particle size analysis, surface charge, PDI, drug loading, entrapment efficiency, TEM, XRD, in vitro release studies, and hemolytic toxicity assays. In vitro evaluation used MCF-7 breast cancer cells.
Main Results:
- * Optimized AZA-LIPO exhibited a mean particle size of 127 nm, with high entrapment efficiency (85.2%) and drug loading (6.82%).
- * In vitro release studies demonstrated a burst release within 2 hours followed by sustained release for 36 hours, showing pH-dependent behavior.
- * AZA-LIPO significantly enhanced cellular uptake and viability in MCF-7 cells compared to free AZA, reducing Bcl2 expression while increasing Bax and caspase-3 activity.
Conclusions:
- * Formulated biocompatible AZA-LIPO nano-formulations represent a promising strategy for improving breast cancer chemotherapy.
- * The optimized liposomal delivery system enhances AZA's anti-cancer efficacy through improved cellular internalization and apoptosis induction.
- * Further preclinical and clinical studies are warranted to establish AZA-LIPO as an effective therapeutic agent for breast cancer treatment.
