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Developing Mixed Micelle Delivery Systems for Aromatase Inhibitors

Sheetal Vermani1, Palwinder Singh1, Varinder Kaur1

  • 1Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.

ACS Omega
|August 8, 2026
PubMed

Insights

A novel nanodrug delivery system using Pluronics enhances the efficacy of compound 1-(a), a potent aromatase inhibitor, for breast cancer therapy. This formulation improves solubility and bioavailability, showing promising therapeutic potential with minimal toxicity.

Area of Science:

  • Pharmaceutical Science
  • Nanotechnology
  • Oncology

Background:

  • Aromatase is a key enzyme in estrogen synthesis and a therapeutic target for estrogen receptor-positive (ER+) breast cancer.
  • Existing aromatase inhibitors have limitations including adverse side effects and poor pharmacokinetics, impacting treatment outcomes.
  • Compound 1-(a) previously showed potent aromatase inhibition (IC50 = 54.0 nM) and tumor growth inhibition.

Purpose of the Study:

  • To evaluate the pharmaceutical viability of compound 1-(a) by assessing its toxicity, bioavailability, and therapeutic efficacy.
  • To develop and optimize a nanodrug delivery system to improve the solubility and pharmacokinetic profile of compound 1-(a).
  • To investigate the in vitro and in vivo performance of the developed nanodrug formulation.

Main Methods:

  • In vivo acute toxicity studies were conducted to assess the safety of compound 1-(a).
  • A mixed micelle-based delivery system using Pluronics P123 and F127 was developed and optimized (2:1 formulation).
  • The nanomicellar formulation's drug loading (8.8%), entrapment efficiency (80%), solubility, stability, cellular uptake (MCF-7, MDA-MB-231), and in vitro drug release were evaluated.

Main Results:

  • Compound 1-(a) demonstrated safety in acute toxicity studies with no significant adverse effects.
  • The optimized Pluronics-based micellar formulation significantly improved compound 1-(a)'s solubility, stability, and cellular uptake.
  • The formulation exhibited sustained drug release characteristics across different pH conditions (1.2, 6.8, 7.4).

Conclusions:

  • Pluronics P123 and F127 form an effective mixed micelle delivery system for the potent aromatase inhibitor compound 1-(a).
  • The developed nanodrug formulation enhances the pharmaceutical properties and therapeutic potential of compound 1-(a) for breast cancer treatment.
  • This study supports the use of Pluronics as a viable drug delivery strategy for potent aromatase inhibitors.

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