title: 2-Hydroxypropyl-β-cyclodextrin-modified SLN of paclitaxel for overcoming p-glycoprotein function in multidrug-resistant breast cancer cells.
abstract: OBJECTIVE
  This study aimed to evaluate the potential of solid lipid nanoparticles (SLNs) of paclitaxel (PTX) modified with a 2-hydroxypropyl-β-cyclodextrin system to enhance cellular accumulation of PTX into p-glycoprotein (p-gp)-expressing cells.
  
  
  METHODS
  The PTX-loaded-SLNs consisted of lipid (stearic acid) and surfactants (lecithin and poloxamer 188) and were then modified with 2-hydroxypropyl-β-cyclodextrin by a sonication method.
  
  
  RESULTS
  In terms of cytotoxicity, PTX-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin showed higher cytotoxicity than other formulations. In particular, the cellular uptake of PTX from PTX-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin was about 5.8- and 1.5-fold higher than that from PTX solution and unmodified PTX-loaded SLNs in MCF-7/ADR cells, respectively. After a 4-h incubation, clear fluorescence images inside cells were observed over time. When PTX-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin were incubated with MCF-7/ADR cells for 4 h, cellular uptake of PTX increased 1.7-fold versus that of PTX in the presence of verapamil.
  
  
  CONCLUSIONS
  These results suggest that optimized SLNs modified with 2-hydroxypropyl-β-cyclodextrin may have potential as an oral drug delivery system for PTX.
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Yuseong-gu, Daejeon, South Korea.
authors.forename: Jong-Suep
authors.initials: JS
authors.lastname: Baek
authors.forename: Cheong-Weon
authors.initials: CW
authors.lastname: Cho
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001692:Biological Transport / Q000187:drug effects; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D002121:Calcium Channel Blockers / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D018432:Drug Resistance, Multiple / Q000187:drug effects; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D005079:Excipients / Q000737:chemistry; D005260:Female; D006801:Humans; D061986:MCF-7 Cells; D053758:Nanoparticles / Q000737:chemistry*; D009363:Neoplasm Proteins / Q000378:metabolism; D017239:Paclitaxel / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D013229:Stearic Acids / Q000737:chemistry; D013501:Surface-Active Agents / Q000737:chemistry; D014465:Ultrasonics; D014700:Verapamil / Q000494:pharmacology; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: C513055:ABCB1 protein, human; D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000972:Antineoplastic Agents, Phytogenic; D002121:Calcium Channel Blockers; D005079:Excipients; D009363:Neoplasm Proteins; D013229:Stearic Acids; D013501:Surface-Active Agents; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; C031183:stearic acid; D014700:Verapamil; D017239:Paclitaxel