title: Docetaxel-loaded solid lipid nanoparticles: preparation, characterization, in vitro, and in vivo evaluations.
abstract: The aim of the present study was to prepare, characterize, and evaluate solid lipid nanoparticles (SLNs) containing docetaxel (DTX) to improve the efficacy of this chemotherapeutic agent. SLNs containing DTX (SLN-DTX) were prepared by microemulsion and probe sonication techniques. In vitro cytotoxicity of SLN-DTX compared with Taxotere® (TXT) was evaluated on colorectal (C-26) and malignant melanoma (A-375) cell lines. Cellular uptake experiment was also carried out on C-26 cells. In in vivo tests, tumor inhibitory efficacy and survival were compared with TXT on C-26-implanted BALB/c mice. SLN-DTX particle size was 180 nm and PDI of 0.2 with spherical shape. Encapsulation efficacy was more than 98%. SLN-DTX at concentration of 100 μM caused 100% and 99.9% viability reduction in C-26 and A-375 after 48 and 72 h, respectively. The half maximal inhibitory concentration (IC50 ) of SLN-DTX on C-26 and A-375 was respectively 0.769 and 28.132 μM after 24 h. DTX cell uptake from SLN-DTX was remarkably higher than TXT. SLN-DTX showed better tumor inhibitory efficacy and survival at a dose of 10 mg/kg versus 10 and 20 mg/kg TXT. In conclusion, the results of the present study showed that the efficacy of SLN-DTX was better than TXT in cell-uptake and in vivo experiments.
authors.affiliation: School of Pharmacy, Mashhad University of Medical Sciences Mashhad Iran.
authors.forename: Navid
authors.initials: N
authors.lastname: Mosallaei
authors.affiliation: Biotechnology Research Center, School of Pharmacy, Mashhad University of Medical Sciences Mashhad Iran.
authors.forename: Mahmoud Reza
authors.initials: MR
authors.lastname: Jaafari
authors.affiliation: School of Pharmacy, Mashhad University of Medical Sciences Mashhad Iran.
authors.forename: Mohammad Yahya
authors.initials: MY
authors.lastname: Hanafi-Bojd
authors.affiliation: Nanotechnology Research Center, School of Pharmacy, Mashhad University of Medical Sciences Mashhad Iran.
authors.forename: Shiva
authors.initials: S
authors.lastname: Golmohammadzadeh
authors.affiliation: Nanotechnology Research Center, School of Pharmacy, Mashhad University of Medical Sciences Mashhad Iran. Electronic address: malaekehb@mums.ac.ir.
authors.forename: Bizhan
authors.initials: B
authors.lastname: Malaekeh-Nikouei
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D045744:Cell Line, Tumor; D003106:Colon / Q000187:drug effects; D015179:Colorectal Neoplasms / Q000188:drug therapy*; D000077143:Docetaxel; D004337:Drug Carriers / Q000737:chemistry; D005260:Female; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D008545:Melanoma / Q000188:drug therapy; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D012007:Rectum / Q000187:drug effects; D043823:Taxoids / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008055:Lipids; D043823:Taxoids; D000077143:Docetaxel