Development and characterization of stable proanthocyanidin-loaded PLAROsomes as a potential drug carrier system for augmenting anticancer activity

Abstract

The aim of the present study was to develop potential drug carrier system formulations, namely PLAROsomes for the delivery of Proanthocyanidin (PACY), isolated from the extract of dried grape seeds. The PLAROsomes loaded with PACY were prepared using the thin film hydration method. The influence of various process parameters and material attributes was investigated using the design of experiments (DoE). The PACY-loaded PLAROsomes were characterized using hyphenated tools. The in-vitro anticancer activities of PACY-loaded PLAROsomes were confirmed using the Trypan blue method, MTT method, and flow cytometric analysis on MCF-7 cells. The polymer-to-lipid ratio, among various process parameters and material attributes, significantly influenced the average particle size. Additionally, it played a crucial role in determining the percentage of PACY released from PACY-loaded PLAROsomes. The size of the PACY-loaded PLAROsomes ranged from 40 to 300 nm, and the optimized batch demonstrated a drug entrapment efficiency of 86.38±0.22%. PACY-loaded PLAROsomes exhibited improved in vitro anticancer activities against MCF-7 breast cancer cell lines compared to PACY. PACY-loaded PLAROsomes showed greater activity at lower concentrations in cytotoxicity studies, as supported by apoptosis analysis. Therefore, PLAROsomes could present a promising drug carrier system for delivering PACY in breast cancer treatment, offering a sustained release effect.