title: Preparation and characterization of pH-sensitive camptothecin-cis-aconityl grafted chitosan oligosaccharide nanomicelles.
abstract: Camptothecin (CPT) was introduced to water-soluble chitosan oligosaccharide (CHO) using cis-aconityl (CA), as a pH-sensitive linker, to develop a new hydrophobic structure, i.e. CPTCACHO. The triple conjugates were synthesized in three ratios (5%, 7.5%, and 10%) and characterized by Fourier transform infrared (FT-IR) and proton nuclear magnetic resonance (1HNMR). Thermo gravimetric analysis and critical micelle concentration (CMC) assessments were performed. Prepared nano-micelles were analyzed for particle size, polydispersity index (PDI), drug release and in vitro cytotoxicity. CPTCACHO 7.5% micelles as optimum micelles had a mean diameter of 50nm (observed by transmission electron microscopy), a zeta potential of +45.9mV, and a CMC of about 9.97×10-5g/L. The release results showed that CPTCACHO 7.5% has the burst release at acidic pH, and cytotoxicity study indicated that IC50of CPTCACHO 7.5% for MCF-7 cell line was 0.8μg/mL. These properties altogether make CPTCACHO micelles, as a pH sensitive cargo with inherent cytotoxicity, a potential candidate for hydrophobic anticancer drugs.
authors.affiliation: Department of pharmaceutics, School of pharmacy, Kermanshah University of Medical Sciences, Kermanshah, 6734667149, Iran.
authors.forename: Reza
authors.initials: R
authors.lastname: Tahvilian
authors.affiliation: Department of pharmaceutics, School of pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran; Student Research Committee, Kermanshah University of Medical Sciences, Kermanshah 6734667149, Iran.
authors.forename: Babak
authors.initials: B
authors.lastname: Tajani
authors.affiliation: Department of pharmaceutics, School of pharmacy, Kermanshah University of Medical Sciences, Kermanshah, 6734667149, Iran.
authors.forename: Komail
authors.initials: K
authors.lastname: Sadrjavadi
authors.affiliation: Department of pharmaceutics, School of pharmacy, Kermanshah University of Medical Sciences, Kermanshah, 6734667149, Iran; Medical biology Research Center, Kermanshah University of Medical Sciences, Kermanshah, Iran. Electronic address: a.fattahi.a@gmail.com.
authors.forename: Ali
authors.initials: A
authors.lastname: Fattahi
mesh_terms: D000156:Aconitic Acid / Q000737:chemistry*; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology*; D002166:Camptothecin / Q000737:chemistry / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers; D004339:Drug Compounding / Q000379:methods; D065546:Drug Liberation; D006801:Humans; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D020128:Inhibitory Concentration 50; D007700:Kinetics; D061986:MCF-7 Cells; D008823:Micelles; D010316:Particle Size
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D008823:Micelles; D048271:Chitosan; D000156:Aconitic Acid; D002166:Camptothecin
keywords: Camptothecin; Chitosan oligosaccharide; pH sensitive nanomicelles