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Updated: Aug 27, 2025
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Design, Fabrication and Evaluation of Stabilized Polymeric mixed micelles for Effective Management in Cancer Therapy
Padakanti Sandeep Chary1, Naveen Rajana1, Geetanjali Devabattula2
1Pharmaceutical Nanotechnology Research Laboratory, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Hyderabad, Telangana, India, 500 037.
Purpose:
Cancer is one of the most common and fatal disease, chemotherapy is the major treatment against many cancer types. The anti-apoptotic BCL-2 protein's expression was increased in many cancer types and Venetoclax (VLX; BCL-2 inhibitor) is a small molecule, which selectively inhibits this specified protein. In order to increase the clinical performance of this promising inhibitor as a repurposed drug, polymeric mixed micelles formulations approach was explored.
Methods:
The Venetoclax loaded polymeric mixed micelles (VPMM) were prepared by using Pluronic® F-127 and alpha tocopherol polyethylene glycol 1000 succinate (TPGS) as excipients by thin film hydration method and characteristics. The percentage drug loading capacity, entrapment efficiency and in-vitro drug release studies were performed using HPLC method. The cytotoxicity assay, cell uptake and anticancer activities were evaluated in two different cancer cells i.e. MCF-7 (breast cancer) and A-549 (lung cancer).
Results:
Particle size, polydispersity index and zeta potential of the VPMM was found to be 72.88 ± 0.09 nm, 0.078 ± 0.009 and -4.29 ± 0.24 mV, respectively. The entrapment efficiency and %drug loading were found to be 80.12 ± 0.23% and 2.13% ± 0.14%, respectively. The IC50 of VLX was found to be 4.78, 1.30, 0.94 µg/ml at 24, 48 and 72 h, respectively in MCF-7 cells and 1.24, 0.68, and 0.314 µg/ml at 24, 48, and 72 h, respectively in A549 cells. Whereas, IC50 of VPMM was found to be 0.42, 0.29, 0.09 µg/ml at 24, 48 and 72 h, respectively in MCF-7 cells and 0.85, 0.13, 0.008 µg/ml at 24, 48 and 72 h in A549 cells, respectively, indicating VPMM showing better anti-cancer activity compared to VLX. The VPMM showed better cytotoxicity which was further proven by other assays and explained the anti-cancer activity is shown through the generation of ROS, nuclear damage,apoptotic cell death and expression of caspase-3,7, and 9 activities in apoptotic cells.
Conclusion:
The current investigation revealed that the Venetoclax loaded polymeric mixed micelles (VPMM) revealed the enhanced therapeutic efficacy against breast and lung cancer in vitro models.
Insights
This study developed Venetoclax loaded polymeric mixed micelles (VPMM) to improve cancer treatment. VPMM demonstrated enhanced anti-cancer efficacy against breast and lung cancer cells in vitro.
Area of Science:
- Nanotechnology in drug delivery
- Cancer therapeutics
- Pharmacology
Background:
- Cancer remains a leading cause of mortality, with chemotherapy as a primary treatment.
- Increased expression of the anti-apoptotic BCL-2 protein is observed in various cancers.
- Venetoclax (VLX) is a BCL-2 inhibitor with potential for repurposed drug applications.
Purpose of the Study:
- To explore polymeric mixed micelles formulations for enhanced clinical performance of Venetoclax.
- To develop and characterize Venetoclax loaded polymeric mixed micelles (VPMM).
Main Methods:
- VPMM were formulated using Pluronic® F-127 and TPGS via thin film hydration.
- Drug loading, entrapment efficiency, and in-vitro release were quantified using HPLC.
- Cytotoxicity, cell uptake, and anti-cancer activities were assessed in MCF-7 (breast) and A-549 (lung) cancer cells.
Main Results:
- VPMM exhibited optimal particle size (72.88 nm), PDI (0.078), and zeta potential (-4.29 mV).
- High entrapment efficiency (80.12%) and drug loading (2.13%) were achieved.
- VPMM demonstrated significantly enhanced cytotoxicity and anti-cancer activity compared to VLX alone, inducing ROS generation, nuclear damage, and apoptosis via caspase activation.
Conclusions:
- Venetoclax loaded polymeric mixed micelles (VPMM) show enhanced therapeutic efficacy.
- VPMM represent a promising drug delivery system for breast and lung cancers.
