Fabrication of versatile targeted lipopolymersomes for improved camptothecin efficacy against colon adenocarcinoma in vitro and in vivo

ABSTRACT

Background

Hybrid vesicular systems (lipopolymersomes) are promising platforms for minimizing the liposomes and polymersomes disadvantages in terms of chemotherapeutic transportation. In this regard, lipopolymersome has been designed to integrate the advantage of both polymersomes and liposomes to enable better structural integrity of the bilayer after encapsulation of hydrophobic drugs while maintaining the soft nature of liposomes, superior serum stability, and high encapsulation efficiency of cargos in the bilayer segment.

Research design and Methods

In the present study, we reported preparation and characterization of five camptothecin (CPT)-loaded lipopolymersomal formulations composed of poly (ethylene glycol)–poly (lactic acid) (PEG-PLA) and dipalmitoylphosphatidylcholine (DPPC) at different molar ratios using film rehydration method. Afterward, the preferred formulation was tagged with AS1411 DNA aptamer in order to evaluate the therapeutic index using nucleolin-positive colon cancer cell lines (HT29 and C26).

Results

The obtained data indicated that the prepared CPT-loaded lipopolymersome at a PEG-PLA: DPPC ratio of 75:25 exhibited superior stability and high loading capacity compared to other systems. Moreover, high cytotoxicity of the aptamer-targeted lipopolymersome and increased tumor accumulation were observed in comparison with non-targeted one.

Conclusions

The designed polymer-rich lipopolymersomal platform offers bright future for the development of potent nanomedicine against cancer.

ABSTRACT

KEYWORDS:

• Hybrid
• lipopolymersome
• camptothecin
• colon cancer
• as1411
• nanomedicine

Supplementary material

Supplemental data for this article can be accessed here.

Acknowledgments

The authors are grateful for the Mashhad University of Medical Sciences. This study was based on the PhD thesis of Mahsa Zahiri.

Declaration of interest

The author(s) have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Author contributions

Mahsa Zahiri: Methodology, Investigation, Data curation, Formal analysis, Validation, Writing - original draft. Seyed Mohammad Taghdisi: Formal analysis, Writing - review & editing. Khalil Abnous: Formal analysis, Writing - review & editing. Mohammad Ramezani: Supervision. Mona Alibolandi: Funding acquisition, Methodology, Project administration, Conceptualization, Supervision.

Additional information

Funding

This paper was funded by the Mashhad University of Medical Sciences (Grant No: 950160).