title: Preparation and characterization of amphiphilic calixarene nanoparticles as delivery carriers for paclitaxel.
abstract: Two types of amphoteric calix[n]arene carboxylic acid (CnCA) derivative, i.e., calix[6]arene hexa-carboxylic acid (C6HCA) and calix[8]arene octo-carboxylic acid (C8OCA), were synthesized by introducing acetoxyls into the hydroxyls of calix[n]arene (n=6, 8). C6HCA and C8OCA nanoparticles (NPs) were prepared successfully using the dialysis method. CnCA NPs had regular spherical shapes with an average diameter of 180-220 nm and possessed negative charges of greater than -30 mV. C6HCA 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. C6HCA and C8OCA 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 C8OCA NPs had a slower release rate compared with C6HCA NPs. These favorable properties of CnCA NPs make them promising nanocarriers for tumor-targeted drug delivery.
authors.affiliation: Department of Pharmacy, Xuzhou Medical College; Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical College, 209 Tongshan Road 221004, P. R. China.
authors.forename: Zi-Ming
authors.initials: ZM
authors.lastname: Zhao
authors.forename: Yu
authors.initials: Y
authors.lastname: Wang
authors.forename: Jin
authors.initials: J
authors.lastname: Han
authors.forename: Hui-Dong
authors.initials: HD
authors.lastname: Zhu
authors.forename: Lin
authors.initials: L
authors.lastname: An
mesh_terms: D000818:Animals; D047250:Calixarenes / Q000008:administration & dosage / Q000138:chemical synthesis*; D002417:Cattle; D004337:Drug Carriers / Q000008:administration & dosage / Q000138:chemical synthesis*; D016503:Drug Delivery Systems / Q000379:methods; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D017239:Paclitaxel / Q000008:administration & dosage / Q000138:chemical synthesis*; D010316:Particle Size; D013501:Surface-Active Agents / Q000008:administration & dosage / Q000138:chemical synthesis*
chemical_list: D004337:Drug Carriers; D013501:Surface-Active Agents; D047250:Calixarenes; D017239:Paclitaxel