title: In-vitro and in-vivo assessment of dextran-appended cellulose acetate phthalate nanoparticles for transdermal delivery of 5-fluorouracil.
abstract: The aim of this research was transdermal delivery of 5-fluorouracil (5-FU) using dextran-coated cellulose acetate phthalate (CAP) nanoparticulate formulation. CAP nanoparticles were prepared using drug-polymer ratio (1:1 to 1:3) and surfactant ratio (2.5, 5 and 10%). Dextran coating was made using aminodextran. The results showed that the optimized CAP nanoparticles (CNs) and dextran-coated CAP nanoparticles represented core-corona nanoparticles with the mean diameter of 75 ± 3 and 79 ± 2 nm, respectively, and entrapment efficiency was 82.5 ± 0.06 and 78.2 ± 0.12, respectively. Dextran-coated nanoparticles (FDCNs) and CAP nanoparticles (FCNs) showed in vitro 5-FU release upto 31 h and 8 h, respectively. Moreover, the cumulative amount of 5-FU penetrated through excised skin from FDCNs was 2.94 folds than that of the FU cream. Concentration of 5-FU in epidermis and dermis were also studied. In dermis, concentration of 5-FU was found higher in case of FDCN formulation than plain FU cream. FDCNs were found more hemocompatible in comparison to FCNs. The hematological data recommended that FDCNs formulation was less immunogenic compared to FU creams formulation. In blood level study, FDCNs exhibited 153, 12, 16.66 and 16.24-fold higher values for area under the curve, Tmax, Cmax and mean residence time (MRT) compared with those of FU cream, respectively. The in-vitro cytotoxicity was assessed using the MCF-7 by the MTT test and was compared to the plain 5-FU solution. All the detailed evidence showed that FDCNs could provide a promising tuning as a transdermal delivery system of 5-FU.
authors.affiliation: a Drug Delivery and Nanotechnology Laboratories, Department of Pharmaceutics , Guru Ramdas Khalsa Institute of Science and Technology Pharmacy Kukrikheda , Barela , Madhya Pradesh , India.
authors.forename: Ashish
authors.initials: A
authors.lastname: Garg
authors.affiliation: a Drug Delivery and Nanotechnology Laboratories, Department of Pharmaceutics , Guru Ramdas Khalsa Institute of Science and Technology Pharmacy Kukrikheda , Barela , Madhya Pradesh , India.
authors.forename: Gopal
authors.initials: G
authors.lastname: Rai
authors.affiliation: a Drug Delivery and Nanotechnology Laboratories, Department of Pharmaceutics , Guru Ramdas Khalsa Institute of Science and Technology Pharmacy Kukrikheda , Barela , Madhya Pradesh , India.
authors.forename: Santram
authors.initials: S
authors.lastname: Lodhi
authors.affiliation: a Drug Delivery and Nanotechnology Laboratories, Department of Pharmaceutics , Guru Ramdas Khalsa Institute of Science and Technology Pharmacy Kukrikheda , Barela , Madhya Pradesh , India.
authors.forename: Alok P
authors.initials: AP
authors.lastname: Jain
authors.affiliation: a Drug Delivery and Nanotechnology Laboratories, Department of Pharmaceutics , Guru Ramdas Khalsa Institute of Science and Technology Pharmacy Kukrikheda , Barela , Madhya Pradesh , India.
authors.forename: Awesh K
authors.initials: AK
authors.lastname: Yadav
mesh_terms: D000279:Administration, Cutaneous; D002482:Cellulose / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D003911:Dextrans / Q000008:administration & dosage* / Q000737:chemistry; D004337:Drug Carriers; D016503:Drug Delivery Systems; D005472:Fluorouracil / Q000008:administration & dosage* / Q000737:chemistry; D006801:Humans; D053758:Nanoparticles / Q000737:chemistry*; D013501:Surface-Active Agents / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D003911:Dextrans; D004337:Drug Carriers; D013501:Surface-Active Agents; D002482:Cellulose; C011708:cellulose acetate phthalate; D005472:Fluorouracil
keywords: 5-fluorouracil; CAP nanoparticles; dextran appended; in-vitro cytotoxicity, transdermal delivery