title: Design of high payload PLGA nanoparticles containing melittin/sodium dodecyl sulfate complex by the hydrophobic ion-pairing technique.
abstract: The water-soluble peptide, melittin, was modified with an anionic agent, sodium dodecyl sulfate by hydrophobic ion-pairing. Investigations showed that the formed complex was very soluble in organic solvent, especially, in dimethylsulfoxide and dehydrated alcohol. Furthermore, the physiochemical properties of the complex in the solid state or in an aqueous medium were characterized using octanol/water partition measurement, Fourier transform infrared spectroscopy, and differential scanning calorimetry. The complex was formulated into poly(D,L-lactide-co-glycolide acid) nanoparticles by an emulsion solvent diffusion method. It was found that the nanoparticles of about 130 nm in size can be produced with a high encapsulation efficiency, and the entrapment of nanoparticles prepared with the formed complex increased from about 50% to nearly 100% compared with that for pure melittin. Moreover, the growth inhibitory effects of modified melittin and melittin-loaded nanoparticles in breast cancer MCF-7 cells were not changed comparing with free melittin as determined by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay.
authors.affiliation: Department of Pharmaceutics, School of Pharmaceutical Science, Shenyang Pharmaceutical University, Shenyang, PR China.
authors.forename: Linlin
authors.initials: L
authors.lastname: Yang
authors.forename: Fude
authors.initials: F
authors.lastname: Cui
authors.forename: Kai
authors.initials: K
authors.lastname: Shi
authors.forename: Dongmei
authors.initials: D
authors.lastname: Cun
authors.forename: Rui
authors.initials: R
authors.lastname: Wang
mesh_terms: D001943:Breast Neoplasms / Q000378:metabolism; D002152:Calorimetry, Differential Scanning; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004121:Dimethyl Sulfoxide / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D005260:Female; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D019344:Lactic Acid / Q000737:chemistry*; D008555:Melitten / Q000008:administration & dosage*; D053758:Nanoparticles; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry*; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared; D013501:Surface-Active Agents / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D012997:Solvents; D013501:Surface-Active Agents; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D008555:Melitten; D011100:Polyglycolic Acid; D019344:Lactic Acid; D012967:Sodium Dodecyl Sulfate; D004121:Dimethyl Sulfoxide