# Extremely long tumor retention, on-demand releasing Nano-Taxel for eradicating ovarian cancers

> **NIH NIH R44** · THERANOSTEC, INC. · 2020 · $1,496,599

## Abstract

Treatment of late-stage ovarian cancer remains one of the greatest challenges for gynecologic oncologists.
The clinical efficacy of paclitaxel (PTX), a first-line chemotherapy, is limited due to its severe adverse effect
and poor drug exposure and delivery to target tissues. Abraxane® (Albumin-bound paclitaxel, particle size
~130 nm) was designed to overcome the dose-limiting toxicity of standard PTX. However, Abraxane® does not
function as a true nanoparticle, because the control over drug properties, such as release rates, is not possible
with this formulation. The safety and effectiveness of Abraxane® in ovarian cancer patients have not been
established. New nanocarriers able to minimize the premature drug release in blood circulation while releasing
drug on-demand at tumor site have profound impact on the improvement of the efficacy and toxicity profile of
the chemotherapeutic drugs. It has also been reported that smaller nanoparticles such as 30 nm micelles could
penetrate poorly permeable tumors for a better anti-tumor effect. The smart PTX loaded micellar nanoparticles
(Nano-Taxel) with smaller size (~20 nm), extremely long tumor retention (at least 12 days), and on-demand
drug releasing properties to be developed in this proposal may offer better efficacy and toxicity profile against
ovarian cancer, therefore have great commercial potentials to lead to a marketable PTX-nanoformulation for
the treatment of ovarian cancer. The overall goal of this proposal is to develop highly effective and less toxic
micellar formulation of PTX (Nano-Taxel) against ovarian cancer in preclinical animal models in Phase I
studies, and perform current good manufacturing practice (cGMP) production & IND-enabling pharmacology
and toxicology studies in Phase II studies that will eventually lead to an IND filing to the FDA for a first-inhuman
phase I clinical trial. Our hypotheses are: (i) The smaller and extremely long tumor retention micelle
formulation of PTX, compared to its free form are more efficacious and less toxic against ovarian cancer; (ii)
The on-demand drug releasing properties of Nano-Taxel achieved by boronate crosslinking strategy will
minimize the premature drug release during circulation but allow instant drug release at tumor sites or in tumor
cells, therefore will greatly improve the efficacy and toxicity profile; and (iii) OA02, a highly potent targeting
ligand, when decorated on the surface of Nano-Taxel to facilitate the in vivo delivery to ovarian cancer, will
further improve its therapeutic index. State-of-the-art design of nanocarriers via engineering telodendrimers
with well-defined structures represents the frontier development of the nanomedicine, in terms of ease of largescale
production, fine-tunable and highly reproducible structure and properties. It will address many
translational barriers of nanotherapeutic agents. The use of boronate crosslinked micelles with extremely long
tumor retention and on-demand drug releasing propertie...

## Key facts

- **NIH application ID:** 10003187
- **Project number:** 5R44CA228645-03
- **Recipient organization:** THERANOSTEC, INC.
- **Principal Investigator:** Tzu-yin Lin
- **Activity code:** R44 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $1,496,599
- **Award type:** 5
- **Project period:** 2018-09-19 → 2024-02-29

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10003187

## Citation

> US National Institutes of Health, RePORTER application 10003187, Extremely long tumor retention, on-demand releasing Nano-Taxel for eradicating ovarian cancers (5R44CA228645-03). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10003187. Licensed CC0.

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