Preparation and characterization of amphiphilic calixarene nanoparticles as delivery carriers for paclitaxel

Article abstract of DOI:10.1248/cpb.c14-00699

Two types of amphoteric calix[n]arene carboxylic acid (CnCA) derivative, i.e., calix[6]arene hexa-carboxylic acid (C ₆ HCA) and calix[8]arene octo-carboxylic acid (C ₈OCA), were synthesized by introducing acetoxyls into the hydroxyls of calix[n]arene (n-6, 8). C₆HCA and C₈ OCA nanoparticles (NPs) were prepared successfully using the dialysis method. C nCA NPs had regular spherical shapes with an average diameter of 180-220 nm and possessed negative charges of greater than -30 mV. C₆ HCA and C₈OCA NPs were stable in 4.5% bovine serum albumin solutions and buffers (pH 5-9), with a low critical aggregation concentration value of 5.7 mg?L-^-1 and 4.0 mg?L-^-1, respectively. C₆ HCA and C₈ OCA NPs exhibited good paclitaxel (PTX) loading capacity, with drug loading contents of 7.5% and 8.3%, respectively. The overall in vitro release behavior of PTX from the CnCA NPs was sustained, and C ₈ OCA NPs had a slower release rate compared with C₆ HCA NPs. These favorable properties of CnCA NPs make them promising nanocarriers for tumortargeted drug delivery.