title: Layer-by-layer nanoencapsulation of camptothecin with improved activity.
abstract: 160 nm nanocapsules containing up to 60% of camptothecin in the core and 7-8 polyelectrolyte bilayers in the shell were produced by washless layer-by-layer assembly of heparin and block-copolymer of poly-l-lysine and polyethylene glycol. The outer surface of the nanocapsules was additionally modified with polyethylene glycol of 5 kDa or 20 kDa molecular weight to attain protein resistant properties, colloidal stability in serum and prolonged release of the drug from the capsules. An advantage of the LbL coated capsules is the preservation of camptothecin lactone form with the shell assembly starting at acidic pH and improved chemical stability of encapsulated drug at neutral and basic pH, especially in the presence of albumin that makes such formulation more active than free camptothecin. LbL nanocapsules preserve the camptothecin lactone form at pH 7.4 resulting in triple activity of the drug toward CRL2303 glioblastoma cell.
authors: Institute for Micromanufacturing and Biomedical Engineering Program, Louisiana Tech University, USA.
authors: Gaurav
authors: G
authors: Parekh
authors: Institute for Micromanufacturing and Biomedical Engineering Program, Louisiana Tech University, USA.
authors: Pravin
authors: P
authors: Pattekari
authors: Institute for Micromanufacturing and Biomedical Engineering Program, Louisiana Tech University, USA.
authors: Chaitanya
authors: C
authors: Joshi
authors: Institute for Micromanufacturing and Biomedical Engineering Program, Louisiana Tech University, USA.
authors: Tatsiana
authors: T
authors: Shutava
authors: Institute for Micromanufacturing and Biomedical Engineering Program, Louisiana Tech University, USA.
authors: Mark
authors: M
authors: DeCoster
authors: Department of Pharmaceutical Sciences, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA.
authors: Tatyana
authors: T
authors: Levchenko
authors: Department of Pharmaceutical Sciences, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA.
authors: Vladimir
authors: V
authors: Torchilin
authors: Institute for Micromanufacturing and Biomedical Engineering Program, Louisiana Tech University, USA. Electronic address: ylvov@latech.edu.
authors: Yuri
authors: Y
authors: Lvov
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000494:pharmacology*; D001932:Brain Neoplasms / Q000473:pathology; D002166:Camptothecin / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D004339:Drug Compounding; D004355:Drug Stability; D005909:Glioblastoma / Q000473:pathology; D006493:Heparin / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D006868:Hydrolysis; D007700:Kinetics; D008970:Molecular Weight; D053769:Nanocapsules; D036103:Nanotechnology; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D011107:Polylysine / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D051381:Rats; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D053769:Nanocapsules; D011108:Polymers; D011107:Polylysine; D011092:Polyethylene Glycols; D006493:Heparin; D002166:Camptothecin
keywords: Camptothecin; Cytotoxic; Glioblastoma; Lactone; Layer-by-layer; Nanocapsules