Formulation, Optimization, and In Vitro Evaluation of Docetaxel-Loaded Cubosomes for Breast Cancer Therapy

Abstract

Author(s): Anil Kumar Y1*, Parimala O2, Dileep Kumar Garnipudi3, Kommu Pradeep4, Srikrishna Theerdhala5, Angilicam Avinash6, Y. Sirisha7, A. Rajesh8

Breast cancer remains a leading cause of cancer-related morbidity and mortality among women worldwide. Docetaxel is a potent taxane used in breast cancer chemotherapy; however, its therapeutic application is limited by poor aqueous solubility, nonspecific distribution, formulation-related adverse effects, and systemic toxicity. The present study aimed to formulate and evaluate docetaxel- loaded cubosomes as a lipid-based nanocarrier system for improving drug delivery and anticancer activity. Cubosomes were prepared using glyceryl monooleate as the lipid phase and poloxamer 407 as the stabilizer through a top-down emulsification and sonication method. Formulation variables were optimized based on particle size, polydispersity index, zeta potential, entrapment efficiency, and drug-loading capacity. The physicochemical and structural characteristics of the optimized formulation were investigated using Fourier-transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, and transmission electron microscopy. In vitro drug release was evaluated using a dialysis membrane method, and the release profile was fitted to appropriate kinetic models. The anticancer activity of docetaxel-loaded cubosomes was assessed in breast cancer cells using cytotoxicity, cellular uptake, and apoptosis assays. The optimized cubosomal formulation demonstrated nanosized particles with a relatively uniform size distribution, high docetaxel entrapment, and sustained drug release compared with the free drug formulation. Docetaxel-loaded cubosomes also produced greater cytotoxic and apoptosis-inducing effects in breast cancer cells, potentially because of enhanced cellular internalization and prolonged intracellular drug availability. These findings suggest that cubosomes may provide a promising delivery platform for improving the pharmaceutical and therapeutic performance of docetaxel in breast cancer treatment.

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