title: Sequentially dual-targeting vector with nano-in-micro structure for improved docetaxel oral delivery in vivo.
abstract: OBJECTIVE
  In this study, we constructed a novel vector (BioPf-M-loaded Alg-microparticles [Alg-BioPf-M]) with nano-in-micro structure to improve the oral absorption of docetaxel (DTX) by sequentially dual-targeting functions toward intestine and sodium-dependent multivitamin transporter based on entrapping biotin-modified micelles into alginate microparticles.
  
  
  METHODS
  A series of characteristics of this system was investigated, such as drug release, cellular uptake, transport pathway and the comprehensive in vivo studies including pharmacokinetic studies, anti-tumor activity and toxicity study.
  
  
  RESULTS
  The bioavailability of DTX-loaded Alg-BioPf-M was 27.4-fold higher than that of free DTX after oral administration and achieved superior tumor inhibition of 84.6% against sarcoma 180 tumors.
  
  
  CONCLUSIONS
  These results demonstrated that the Alg-BioPf-M was a promising vector for oral delivery of DTX.
authors.affiliation: Ministry of Educational (MOE) Key Laboratory of Macromolecular Synthesis & Functionalization, Department of Polymer Science & Engineering, Zhejiang University, Hangzhou 310027, China.
authors.forename: Yurun
authors.initials: Y
authors.lastname: Shen
authors.affiliation: College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
authors.forename: Mengying
authors.initials: M
authors.lastname: Hu
authors.affiliation: Ministry of Educational (MOE) Key Laboratory of Macromolecular Synthesis & Functionalization, Department of Polymer Science & Engineering, Zhejiang University, Hangzhou 310027, China.
authors.forename: Liyan
authors.initials: L
authors.lastname: Qiu
mesh_terms: D000284:Administration, Oral; D000464:Alginates / Q000737:chemistry / Q000378:metabolism; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D045744:Cell Line, Tumor; D000077143:Docetaxel; D016503:Drug Delivery Systems; D005260:Female; D020723:Glucuronic Acid / Q000737:chemistry / Q000378:metabolism; D006603:Hexuronic Acids / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D008813:Mice, Inbred ICR; D008823:Micelles; D053758:Nanoparticles / Q000737:chemistry*; D061848:Optical Imaging; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry; D043823:Taxoids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D014018:Tissue Distribution
chemical_list: D000464:Alginates; D000970:Antineoplastic Agents; D006603:Hexuronic Acids; D008823:Micelles; D043823:Taxoids; D020442:Poloxamer; D000077143:Docetaxel; D020723:Glucuronic Acid
keywords: bioavailability; biotin; docetaxel; oral cancer therapy; targeting drug delivery