Safe and efficient pH sensitive tumor targeting modified liposomes with minimal cytotoxicity

Area of Science:

• Biomaterials Science
• Drug Delivery Systems
• Nanotechnology

Background:

• Liposomes offer biocompatibility but often lack controlled release at physiological pH.
• Polyaspartic acid (PASP) derivatives can be modified for pH-sensitivity.
• Developing stable, pH-responsive drug carriers is crucial for targeted cancer therapy.

Purpose of the Study:

• To develop novel pH-sensitive liposomes (OPLPs) using octylamine-grafted polyaspartic acid (PASP-g-C8).
• To evaluate the stability, pH-responsive drug release, and tumor-targeting efficacy of OPLPs.
• To assess the in vitro tumor inhibition and cytotoxicity of the OPLPs.

Main Methods:

• Synthesis of PASP-g-C8 and its modification onto liposomes to form OPLPs.
• Drug release studies were conducted at physiological (pH 7.4) and tumor-mimicking (pH 5.0) conditions.
• In vitro cytotoxicity and tumor inhibition assays were performed on tumor and normal cells.

Main Results:

• OPLPs exhibited enhanced stability and controlled drug release compared to PASP-modified liposomes (PLPs) at pH 7.4.
• OPLPs demonstrated significantly faster drug release at pH 5.0, indicating pH-sensitivity.
• In vitro studies showed OPLPs achieved 65% tumor cell inhibition with 100% normal cell survival after 48 hours.

Conclusions:

• PASP-g-C8 modified liposomes (OPLPs) represent a promising pH-sensitive drug delivery system.
• OPLPs offer improved stability and targeted drug release in tumor microenvironments.
• The developed OPLPs show high tumor inhibition efficacy with minimal impact on normal cells, suggesting potential for cancer therapy.