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Nanoparticle formulation of ormeloxifene for pancreatic cancer
Sheema Khan1, Neeraj Chauhan1, Murali M Yallapu1
1Department of Pharmaceutical Sciences and Center for Cancer Research, University of Tennessee Health Science Center, Memphis, TN, USA.
Abstract:
Pancreatic cancer is the fourth most prevalent cancer with about an 85% mortality rate; thus, an utmost need exists to discover new therapeutic modalities that would enhance therapy outcomes of this disease with minimal or no side effects. Ormeloxifene (ORM), a synthetic molecule, has exhibited potent anti-cancer effects through inhibition of important oncogenic and proliferation signaling pathways. However, the anti-cancer efficacy of ORM can be further improved by developing its nanoformulation, which will also offer tumor specific targeted delivery. Therefore, we have developed a novel ORM encapsulated poly(lactic-co-glycolic acid) nanoparticle (NP) formulation (PLGA-ORM NP). This formulation was characterized for particle size, chemical composition, and drug loading efficiency, using various physico-chemical methods (TEM, FT-IR, DSC, TGA, and HPLC). Because of its facile composition, this novel formulation is compatible with antibody/aptamer conjugation to achieve tumor specific targeting. The particle size analysis of this PLGA-ORM formulation (∼100 nm) indicates that this formulation can preferentially reach and accumulate in tumors by the Enhanced Permeability and Retention (EPR) effect. Cellular uptake and internalization studies demonstrate that PLGA-ORM NPs escape lysosomal degradation, providing efficient endosomal release to cytosol. PLGA-ORM NPs showed remarkable anti-cancer potential in various pancreatic cancer cells (HPAF-II, AsPC-1, BxPC-3, Panc-1, and MiaPaca) and a BxPC-3 xenograft mice model resulting in increased animal survival. PLGA-ORM NPs suppressed pancreatic tumor growth via suppression of Akt phosphorylation and expression of MUC1, HER2, PCNA, CK19 and CD31. This study suggests that the PLGA-ORM formulation is highly efficient for the inhibition of pancreatic tumor growth and thus can be valuable for the treatment of pancreatic cancer in the future.
Insights
Researchers developed a novel Ormeloxifene (ORM) nanoparticle formulation using poly(lactic-co-glycolic acid) (PLGA) to target pancreatic cancer. This PLGA-ORM nanoparticle formulation demonstrated significant anti-cancer potential, inhibiting tumor growth and increasing survival in preclinical models.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Pancreatic cancer has a high mortality rate, necessitating novel therapeutic strategies.
- Ormeloxifene (ORM) shows anti-cancer properties by inhibiting key oncogenic pathways.
- Enhancing ORM delivery through nanoformulations can improve efficacy and enable targeted therapy.
Purpose of the Study:
- To develop and characterize a novel Ormeloxifene (ORM) encapsulated poly(lactic-co-glycolic acid) nanoparticle (PLGA-ORM NP) formulation.
- To evaluate the anti-cancer efficacy and tumor-targeting potential of the PLGA-ORM NPs in pancreatic cancer models.
Main Methods:
- Physicochemical characterization of PLGA-ORM NPs using TEM, FT-IR, DSC, TGA, and HPLC.
- In vitro studies on pancreatic cancer cell lines (HPAF-II, AsPC-1, BxPC-3, Panc-1, MiaPaca) for cellular uptake and endosomal escape.
- In vivo efficacy assessment in a BxPC-3 xenograft mice model, including survival analysis and tumor growth inhibition.
- Analysis of molecular targets including Akt phosphorylation, MUC1, HER2, PCNA, CK19, and CD31 expression.
Main Results:
- PLGA-ORM NPs were successfully synthesized with a particle size of approximately 100 nm, suitable for tumor accumulation via the EPR effect.
- The formulation demonstrated efficient cellular uptake and endosomal escape, bypassing lysosomal degradation.
- PLGA-ORM NPs significantly inhibited pancreatic cancer cell proliferation and tumor growth in vivo, leading to increased animal survival.
- The treatment suppressed key oncogenic markers, including Akt phosphorylation, MUC1, HER2, PCNA, CK19, and CD31.
Conclusions:
- The novel PLGA-ORM nanoparticle formulation is a promising strategy for targeted pancreatic cancer therapy.
- This formulation exhibits potent anti-cancer activity by inhibiting tumor growth and associated molecular pathways.
- PLGA-ORM NPs offer a valuable platform for future development in pancreatic cancer treatment.
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