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pH-responsive delivery of anti-metastatic niclosamide using mussel inspired polydopamine nanoparticles
Omkar Mhatre1, B Pradeep K Reddy1, Chetna Patnaik2
1Department of Biosciences and Bioengineering (BSBE), Indian Institute of Technology Bombay, Powai, Mumbai, India.
Abstract:
Niclosamide (Nic), an FDA approved antihelminthic drug, is being repurposed as a potent anti-cancer and anti-inflammatory agent. Niclosamide exhibits anti-cancer activity in multiple cancer types, including breast, colon, and prostate cancers. Niclosamide, a BCS II drug, is practically insoluble in water and sparingly soluble in organic solvents (ethanol, dimethyl sulfoxide), leading to limited therapeutic applications, and necessitates the need for a drug carrier. Herein, we report the preparation of polydopamine nanoparticles loaded with niclosamide (Nic-PDA NPs). The designed formulation had a very high loading efficiency (~30%) and entrapment efficiency close to 90%. The average hydrodynamic diameter of Nic-PDA NPs was 146.3 nm, with a narrow size distribution (PDI = 0.039). The formulation exhibited a pH-dependent drug release profile, with ~35% drug released at pH 7.4 after 120 h, compared to > 50% at pH 5.5 in simulated physiological conditions. The NPs exhibited time-dependent cellular uptake and were primarily localized in the cytoplasm. The formulation exhibited comparable cytotoxicity in MDA-MB-231 cells (IC50 = 2.73 μM, 36 h), and inhibited the migration of cancer cells significantly compared to the free drug and unloaded PDA NPs. Furthermore, the unloaded NPs exhibited excellent in vivo compatibility. The study establishes a rigorously optimized protocol for the synthesis of Nic loaded PDA NPs. The biocompatibility, anti-migratory efficacy, and the in vivo non-toxic nature of PDA has been well demonstrated.
Insights
This study developed niclosamide-loaded polydopamine nanoparticles (Nic-PDA NPs) to improve cancer treatment. These nanoparticles show high drug loading, controlled release, and effective anti-cancer activity with good biocompatibility.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Pharmacology
Background:
- Niclosamide (Nic), an FDA-approved antihelminthic, shows promise as an anti-cancer agent but suffers from poor solubility, limiting its therapeutic use.
- Developing effective drug delivery systems is crucial to overcome the poor bioavailability and enhance the efficacy of niclosamide for cancer therapy.
Purpose of the Study:
- To prepare and characterize niclosamide-loaded polydopamine nanoparticles (Nic-PDA NPs) for enhanced anti-cancer applications.
- To evaluate the drug loading, entrapment efficiency, particle characteristics, pH-dependent drug release, cellular uptake, cytotoxicity, and anti-migratory effects of Nic-PDA NPs.
- To assess the in vivo compatibility of the polydopamine nanoparticles.
Main Methods:
- Niclosamide was loaded into polydopamine (PDA) nanoparticles.
- Physicochemical properties including hydrodynamic diameter, size distribution, loading efficiency, and entrapment efficiency were determined.
- In vitro drug release studies were conducted at different pH values (pH 7.4 and pH 5.5).
- Cellular uptake and cytotoxicity assays were performed using MDA-MB-231 cells.
- In vivo compatibility of unloaded PDA nanoparticles was evaluated.
Main Results:
- Nic-PDA NPs were successfully prepared with high loading (~30%) and entrapment (~90%) efficiencies.
- The nanoparticles exhibited an average hydrodynamic diameter of 146.3 nm with narrow size distribution (PDI = 0.039).
- A pH-dependent drug release profile was observed, with higher release at acidic pH (5.5) compared to physiological pH (7.4).
- Nic-PDA NPs demonstrated time-dependent cellular uptake, enhanced cytotoxicity (IC50 = 2.73 μM at 36 h in MDA-MB-231 cells), and significant inhibition of cancer cell migration compared to free niclosamide.
- Unloaded PDA NPs showed excellent in vivo compatibility and were non-toxic.
Conclusions:
- Polydopamine nanoparticles provide an effective carrier for niclosamide, significantly improving its anti-cancer properties.
- The Nic-PDA NP formulation demonstrates potential for enhanced cancer therapy due to improved efficacy, controlled release, and good biocompatibility.
- The optimized protocol for Nic-PDA NP synthesis and the demonstrated safety profile of PDA nanoparticles pave the way for further preclinical investigations.
