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Published on: August 23, 2024
Honokiol nanomicellar formulation produced increased oral bioavailability and anticancer effects in triple negative
Chandraiah Godugu1, Ravi Doddapaneni2, Mandip Singh3
1College of Pharmacy Pharmaceutical Sciences, Florida A & M University, Tallahassee, FL 32307, USA; Department of Regulatory Toxicology, National Institute of Pharmaceutical Education and Research, Balanagar, Hyderabad, Telangana 500037 India.
Abstract:
Triple negative breast cancer (TNBC), owing to its aggressive behavior and toxicity associated with available chemotherapy; currently no suitable therapy is available. Honokiol (HNK) is a promising anticancer drug but has poor bioavailability. In the current study, we evaluated the anticancer effects of an oral Honokiol nanomicellar (NM) formulation (size range of 20-40nm) in vitro against various TNBC cells lines. Cytotoxicity, clonogenic and wound healing assays demonstrated the promising anticancer effects. In vitro Caco-2 permeability studies suggested increased absorption of Honokiol. Compared to HNK-FD, nanomicellar formulations resulted in significant increase in the oral bioavailability. Cmax (4.06 and 3.60-fold) and AUC (6.26 and 5.83-fold) were significantly increased in comparison to oral 40 and 80mg/kg free drug respectively. Further, anticancer effects of these formulations were studied in BALB/c nude mice transplanted with orthotopic MDA-MB-231 cell induced xenografts. After 4 weeks of daily administration of HNK-NM formulation, significant reduction in the tumor volumes and weights compared to free drug (p<0.001) treated groups was observed. Surprisingly, in some of the animals (25%), the treatment resulted in complete eradication of tumors. Increased apoptosis and antiangiogenic effect was observed in HNK-NM groups compared to free drug and untreated control animals. This is the first report demonstrating that HNK-FD possesses anticancer effects against TNBC.
Insights
Oral Honokiol nanomicellar (NM) formulation shows significant anticancer effects against triple-negative breast cancer (TNBC). This novel formulation enhances Honokiol bioavailability and demonstrates tumor reduction, even complete eradication, in preclinical models.
Area of Science:
- Oncology
- Pharmacology
- Nanotechnology
Background:
- Triple-negative breast cancer (TNBC) is aggressive with limited effective therapies.
- Honokiol (HNK) shows anticancer potential but suffers from poor oral bioavailability.
- Developing enhanced drug delivery systems is crucial for TNBC treatment.
Purpose of the Study:
- To evaluate the in vitro and in vivo anticancer efficacy of an oral Honokiol nanomicellar (NM) formulation against TNBC.
- To assess the impact of nanomicellar formulation on Honokiol's oral bioavailability.
- To investigate the mechanisms of action, including apoptosis and antiangiogenesis.
Main Methods:
- In vitro assays (cytotoxicity, clonogenic, wound healing) using TNBC cell lines.
- In vitro Caco-2 permeability studies to assess drug absorption.
- Pharmacokinetic studies to determine oral bioavailability (Cmax, AUC) compared to free drug.
- In vivo xenograft studies in BALB/c nude mice with orthotopic MDA-MB-231 tumors.
Main Results:
- Honokiol NM formulation exhibited significant in vitro anticancer activity against TNBC cells.
- Nanomicellar formulation markedly increased Honokiol's oral bioavailability (4-6 fold).
- In vivo studies showed significant reduction in tumor volume and weight; 25% complete tumor eradication observed.
- Increased apoptosis and antiangiogenic effects were noted in HNK-NM treated groups.
Conclusions:
- Oral Honokiol nanomicellar formulation is a promising strategy for TNBC treatment.
- The NM formulation overcomes Honokiol's bioavailability limitations, enhancing its efficacy.
- This study provides the first evidence of HNK-NM's potent anticancer effects against TNBC.
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