title: Preparation and physicochemical characterization of a novel paclitaxel-loaded amphiphilic aminocalixarene nanoparticle platform for anticancer chemotherapy.
abstract: OBJECTIVE
  This paper describes the development and optimization of a nanoparticle delivery platform for the anticancer agent, paclitaxel, using a novel amphiphilic carrier, tetrahexyloxy-tetra-p-aminocalix[4]arene (A4C(6) ).
  
  
  METHODS
  Nanoparticles were successfully prepared at pH4 by an emulsion evaporation method whereby an organic phase containing paclitaxel: A4C(6) (molar ratio 1:10) was dispersed by probe sonication into an aqueous phase containing 0.5% w/v polyvinyl alcohol as stabilizer.
  
  
  RESULTS
  The drug-loaded nanoparticles had a mean size of 78.7±20.7nm, surface potential of 38.3±7.67mV, and paclitaxel loading and encapsulation efficiencies of 69.1±5.3µg drug/mg carrier and 50.4±3.2%, respectively. Transmission electron micrographs showed discrete particles with no evidence of agglomeration. In-vitro dissolution into phosphate buffered saline supplemented with 4% bovine serum albumin showed 32.7±3.9%, 82.6±5.3% and 91.0±6.0% of the encapsulated paclitaxel load was released at 5, 72 and 120h, respectively.
  
  
  CONCLUSIONS
  This is the first report on the use of amino-substituted amphiphilic calixarenes for the encapsulation of anticancer agents. The nanoparticles produced were significantly smaller than, but had comparable drug loads to the Abraxane nanoparticles, and have the potential to achieve targeted delivery of paclitaxel to tumour tissues.
authors.affiliation: Pharmacy, School of Medicine and Pharmacology, University of Western Australia, Crawley, WA, Australia.
authors.forename: Clare
authors.initials: C
authors.lastname: Weeden
authors.forename: Karel J
authors.initials: KJ
authors.lastname: Hartlieb
authors.forename: Lee Yong
authors.initials: LY
authors.lastname: Lim
mesh_terms: D000068196:Albumin-Bound Paclitaxel; D000418:Albumins / Q000008:administration & dosage / Q000737:chemistry; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000737:chemistry; D047250:Calixarenes / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D017239:Paclitaxel / Q000008:administration & dosage* / Q000737:chemistry; D010316:Particle Size; D011142:Polyvinyl Alcohol / Q000737:chemistry; D012710:Serum Albumin, Bovine / Q000737:chemistry; D013997:Time Factors
chemical_list: D000068196:Albumin-Bound Paclitaxel; D000418:Albumins; D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D005079:Excipients; D047250:Calixarenes; D012710:Serum Albumin, Bovine; D011142:Polyvinyl Alcohol; D017239:Paclitaxel