PLGA nanoparticles for calcitriol delivery

Abstract

Calcitriol, the active metabolite of Vitamin D3, is a potential anticancer agent but exhibits several drawbacks. Therefore, new therapeutic strategies, as specific drug delivery systems, must be developed in order to overcome those limitations. The aim of this work was to prepare poly(lactide-coglycolide) nanoparticles as drug delivery vehicles for calcitriol. Two formulation parameters, vitamin/polymer ratio and sonication time, were firstly studied and discussed using cholecalciferol as a drug model. Then, calcitriol-loaded poly(lactide-coglycolide) nanoparticles with controlled sizes and properties were prepared. The nanoparticles remained stable at storage conditions for several weeks and they were successfully lyophilized to increase their shelf-life using a crioprotectant. In vitro studies using two human cancer cell lines, S2-013 and A549, demonstrated that bare PLGA NPs are biocompatible.