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Characteristics of Molecularly Engineered Anticancer Drug Conjugated Organic Nanomicelles for Site-Selective Cancer
Nishant Kumar Jain1, Shalini Dimri2,3, Rajendra Prasad1
1Department of Biosciences and Bioengineering, Indian Institute of Technology Bombay (IIT-B), Powai, Mumbai, India.
Abstract:
Site-selective uptake and specific biodistribution of chemotherapeutic drugs are essential prerequisites for targeted cancer therapy. Especially, antibody and peptide conjugated drugs have been attempted as localized therapeutic agents. However, the characteristics of drug conjugated nanosystems are less explored, which are limited with their toxicity, low therapeutic efficacy, complicated synthesis, and high costs. Herein, we report a biocompatible (about 95%) molecularly engineered anticancer drug conjugated nanomicelles (∼200 nm in size) for site-selective CD44 overexpressed cancer cell rupture and tumor growth inhibition. Microscopic analysis demonstrates the distinct visualization of organic-organic interfaces (∼5 nm), which are corroborated with spectroscopic measurements confirmed the conjugation of niclosamide drug with hyaluronic acid (NIC-HA). Uniformly distributed hemocompatible (about 99%) organic nanomicelles exhibit the cellular membrane and cytoplasmic targeting with significant cellular rupture (IC50 of 4 μM for MDA MB 231 cells) indicating their inherent targeting ability for cancer cells and cancer stem cells. An inclusive in vitro and in vivo analysis for targeted antitumor activity (HT1080 tumor xenograft model) of NIC-HA nanoconjugates (∼24.6% loading) exhibited promising cancer cell death and tumor growth inhibition (60%, p < 0.05) due to STAT-3 signaling pathway inhibition and induction of apoptosis in CD44-positive triple negative breast cancer cells.
Insights
Molecularly engineered nanomicelles conjugated with niclosamide and hyaluronic acid (NIC-HA) demonstrate targeted cancer cell rupture and tumor growth inhibition. This biocompatible nanodrug effectively targets CD44-overexpressing cancer cells, offering a promising approach for cancer therapy.
Area of Science:
- Biotechnology
- Nanomedicine
- Oncology
Background:
- Targeted cancer therapy requires site-selective drug delivery and biodistribution.
- Existing antibody/peptide-conjugated drugs face challenges like toxicity, low efficacy, and high costs.
- Drug-conjugated nanosystems' characteristics remain underexplored.
Purpose of the Study:
- To develop a biocompatible nanomicelle system for targeted cancer therapy.
- To investigate the site-selective uptake and efficacy of anticancer drug-conjugated nanomicelles.
- To evaluate the potential of niclosamide-hyaluronic acid nanoconjugates (NIC-HA) for CD44-positive cancer treatment.
Main Methods:
- Synthesis of molecularly engineered anticancer drug-conjugated nanomicelles (NIC-HA) with a size of approximately 200 nm.
- Microscopic and spectroscopic analyses to confirm drug conjugation and nanomicelle structure.
- In vitro cytotoxicity assays (MDA MB 231 cells) and in vivo antitumor activity studies (HT1080 tumor xenograft model).
Main Results:
- NIC-HA nanomicelles exhibited high biocompatibility (95%) and hemocompatibility (99%).
- Significant cellular rupture observed in CD44-overexpressing cancer cells (IC50 of 4 μM).
- In vivo studies showed 60% tumor growth inhibition (p < 0.05) via STAT-3 inhibition and apoptosis induction.
Conclusions:
- Biocompatible NIC-HA nanomicelles demonstrate effective targeting of CD44-positive cancer cells.
- The nanoconjugates induce significant cancer cell death and inhibit tumor growth.
- NIC-HA nanomicelles represent a promising platform for targeted triple-negative breast cancer therapy.
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