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Updated: Dec 13, 2025
A Tripeptide-Stabilized Nanoemulsion of Oleic Acid
Published on: February 27, 2019
Pyridoclax-loaded nanoemulsion for enhanced anticancer effect on ovarian cancer
Background:
Pyridoclax is an original lead, recently identified as very promising in treatment of chemoresistant ovarian cancers. To correct the unfavorable intrinsic physico-chemical properties of this BCS II drug, a formulation strategy was implied in the drug discovery step. Pyridoclax-loaded nanoemulsions (NEs) were developed to permit its preclinical evaluation.
Results:
The resulting nanoemulsions displayed a mean size of about 100 nm and a high encapsulation efficiency (>95%) at a drug loading of 2 wt%, enabling a 1,000-fold increase of the Pyridoclax apparent solubility. NEs have enabled a sustained release of the drug as assayed by a dialysis bag method. In addition, anti-tumor effects of the Pyridoclax-loaded nanoemulsions (PNEs) showed a 2.5-fold higher activity on chemoresistant ovarian cancer cells than free Pyridoclax. This effect was confirmed by a drastic increase of caspase 3/7 activation from 10 µM PNEs, as newly objectified by real time apoptose imaging. The Pyridoclax bioavailability was kept unchanged after encapsulation in nanoemulsions as determined in a mice model after oral administration.
Conclusion:
Thus, NEs should permit valuable Pyridoclax oral administration, and valorization of this promising anticancer drug by maintaining its original anticancer activity, and by reducing the Pyridoclax therapeutic concentration.
Insights
Nanoemulsions (NEs) enhance the solubility and anticancer activity of Pyridoclax, a promising drug for chemoresistant ovarian cancer. This formulation enables oral administration and reduces therapeutic concentration, improving drug efficacy.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Nanotechnology
Background:
- Pyridoclax shows promise for chemoresistant ovarian cancers.
- Pyridoclax exhibits poor physicochemical properties (BCS II drug).
- Nanoemulsions (NEs) were developed to improve Pyridoclax formulation.
Purpose of the Study:
- To formulate Pyridoclax-loaded nanoemulsions (PNEs).
- To evaluate the preclinical efficacy of PNEs for chemoresistant ovarian cancer.
- To assess the impact of nanoemulsion formulation on Pyridoclax properties and bioavailability.
Main Methods:
- Development of Pyridoclax-loaded nanoemulsions (NEs).
- Characterization of NEs for size, encapsulation efficiency, and drug loading.
- In vitro drug release studies (dialysis bag method).
- In vitro anti-tumor activity assessment on cancer cells.
- Caspase 3/7 activation assay using real-time apoptosis imaging.
- In vivo bioavailability study in a mice model.
Main Results:
- NEs achieved ~100 nm size with >95% encapsulation efficiency and 2 wt% drug loading.
- Pyridoclax apparent solubility increased 1,000-fold with sustained release from NEs.
- PNEs demonstrated 2.5-fold higher anti-tumor activity than free Pyridoclax.
- Significant increase in caspase 3/7 activation observed with PNEs.
- Oral bioavailability of Pyridoclax remained unchanged after nanoemulsion encapsulation.
Conclusions:
- Nanoemulsions facilitate oral administration of Pyridoclax.
- NEs maintain Pyridoclax's anticancer activity and reduce therapeutic concentration.
- This formulation strategy enhances the therapeutic potential of Pyridoclax for ovarian cancer treatment.
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