Quantitative structure-property relationship (QSPR) modeling of drug-loaded polymeric micelles via genetic function approximation

PLoS One. 2015 Mar 17;10(3):e0119575. doi: 10.1371/journal.pone.0119575. eCollection 2015.

Abstract

Self-assembled nano-micelles of amphiphilic polymers represent a novel anticancer drug delivery system. However, their full clinical utilization remains challenging because the quantitative structure-property relationship (QSPR) between the polymer structure and the efficacy of micelles as a drug carrier is poorly understood. Here, we developed a series of QSPR models to account for the drug loading capacity of polymeric micelles using the genetic function approximation (GFA) algorithm. These models were further evaluated by internal and external validation and a Y-randomization test in terms of stability and generalization, yielding an optimization model that is applicable to an expanded materials regime. As confirmed by experimental data, the relationship between microstructure and drug loading capacity can be well-simulated, suggesting that our models are readily applicable to the quantitative evaluation of the drug-loading capacity of polymeric micelles. Our work may offer a pathway to the design of formulation experiments.

Publication types

  • Research Support, Non-U.S. Gov't
  • Validation Study

MeSH terms

  • Algorithms
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / therapeutic use
  • Drug Carriers / chemistry*
  • Micelles
  • Quantitative Structure-Activity Relationship*

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Micelles

Grants and funding

This work was financially supported by National Natural Science Foundation of China (No.21176090), Team Project of Natural Science Foundation of Guangdong Province, China (No.S2011030001366), Specialized Research Fund for the Doctoral Program of Higher Education of China (No.20130172110009), and Fundamental Research Funds for the Central Universities, China (No.2013ZP0010, 2013ZZ0059, 2014ZP0020). The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.