title: Albumin anchored docetaxel lipid nanoemulsion for improved targeting efficiency - preparation, characterization, cytotoxic, antitumor and in vivo imaging studies.
abstract: The aim was to develop albumin anchored docetaxel lipid nanoemulsion (ALNE) for improving tumor targeted delivery. The O/W lipid nanoemulsion, LNEs were prepared by homogenization and ultrasonication processes. The size of globules and zeta potential were measured by Malvern Zetasizer. Albumin was coupled to stearylamine containing lipid nanoemulsion (SALNE) globules using water soluble EDC reaction. The drug content and entrapment efficiencies for the LNEs were determined by the high-performance liquid chromatography. The in vitro cytotoxic studies of the delivery systems were performed on MCF-7 and Hela cells. The IC 50 values of ALNE on both the cell lines were statistically significant. The in vivo antitumor activity was tested on solid tumors induced in C57BL/6 mice. This study revealed that the percentage tumor inhibition for the groups treated with DLNE, SALNE and ALNE when compared with untreated control was found to be 55.62 ± 5.41%, 54.27 ± 4.85% and 80.01 ± 2.74%, respectively. Furthermore, in vivo distribution studies were carried out in breast cancer MDA-MB231 xenografted Balb/c mice. The LNEs were loaded with fluorescent DiD oil and the distribution in different organs after 6 h was tracked using Caliper life sciences in vivo imaging system. The studies revealed that ALNE was superior in tumor targeting activity when compared with DLNE and SALNE by 3.04 and 2.26 folds, respectively. The average radiance values of ALNE on the tumor tissue were statistically significant when compared with DLNE, SALNE at p < 0.01. In addition, this strategy can become a platform technology for other lipophilic drugs to target tumors.
authors.affiliation: a Nanotechnology Research Lab, Department of Pharmaceutics , University College of Pharmaceutical Sciences, Kakatiya University , Warangal , Telangana , India .
authors.forename: Syed
authors.initials: S
authors.lastname: Muzammil Afzal
authors.affiliation: b National Institute of Pharmaceutical Education and Research , Balanagar , Hyderabad , India , and.
authors.forename: V G M
authors.initials: VG
authors.lastname: Naidu
authors.affiliation: c National Center for Laboratory Animal Sciences , National Institute of Nutrition , Tarnaka , Hyderabad , India.
authors.forename: N
authors.initials: N
authors.lastname: Harishankar
authors.affiliation: a Nanotechnology Research Lab, Department of Pharmaceutics , University College of Pharmaceutical Sciences, Kakatiya University , Warangal , Telangana , India .
authors.forename: Veerabrahma
authors.initials: V
authors.lastname: Kishan
mesh_terms: D000418:Albumins / Q000737:chemistry* / Q000378:metabolism; D000818:Animals; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical; D000077143:Docetaxel; D004337:Drug Carriers; D016503:Drug Delivery Systems; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D051379:Mice; D008810:Mice, Inbred C57BL; D053758:Nanoparticles / Q000737:chemistry*; D043823:Taxoids / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D023041:Xenograft Model Antitumor Assays
chemical_list: D000418:Albumins; D004337:Drug Carriers; D008055:Lipids; D043823:Taxoids; D000077143:Docetaxel
keywords: Albumin tagged docetaxel lipid emulsion; antitumor study; fluorescent imaging study; improved tumor delivery; tumor targeting