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2000
Volume 21, Issue 18
  • ISSN: 1570-1808
  • E-ISSN: 1875-628X

Abstract

Introduction

To address the issues of liposomal instability and enhance the delivery of docetaxel (DTX) to breast cancer cells, the development of polyethylene glycol (PEG)-coated proliposomes was proposed, utilizing a thin film hydration technique followed by lyophilization with an appropriate cryoprotectant. Various compositions of phospholipid, cholesterol, and docetaxel were optimized, and the PEG was used in a 1.3:1 ratio of the phospholipid.

Methods

The liposomes were converted to proliposomes using a lyophilizer. The optimized formulation possesses a particle size of 117.0 ± 9.78 nm, with a polydispersity index (PDI) of 0.265 ± 0.094, drug entrapment (DE) of 96.0± 6.14%, and drug loading (DL) of 9.20 ± 3.17%. study demonstrated a controlled release pattern consistent with the Higuchi model, alongside significantly lower protein binding relative to free DTX, indicating a potential reduction in side effects.

Results

Cell viability study demonstrated increased cytotoxicity of PEG-DTX proliposomes (PEG-DTX PL) against MDA-MB-231 cells, evidenced by a lower IC (4.677 μg/mL) relative to free DTX, underscoring the promise of this nanocarrier for targeted therapy.

Conclusion

The findings are promising as a simple and scalable carrier comprising general and biocompatible materials that can provide a safe surfactant free nanosystem with improved efficacy and performance.

© 2024 Bentham Science Publishers
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Development, Optimization, Characterization, and In-vitro Assessment of PEG-coated Docetaxel-loaded Proliposomes for Delivery to Breast Cancer Cells
Letters in Drug Design & Discovery 21, 4556 (2024); https://doi.org/10.2174/0115701808355340241223072643
/content/journals/lddd/10.2174/0115701808355340241223072643
/content/journals/lddd/10.2174/0115701808355340241223072643
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  • Article Type:     Research Article
Keyword(s): anticancer agents; biocompatible; controlled release; Docetaxel; drug delivery; protein binding

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