Formulation and in vitro characterization of poly(dl-lactide-co-glycolide)/Eudragit RLPO or RS30D nanoparticles as an oral carrier of levofloxacin hemihydrate.
The main objective of this study was to design positively charged Levofloxacin Hemihydrate (Levo-h)-loaded nanoparticles with improved entrapment efficiency and antibacterial activity. PLGA alone or in combinations with Eudragit® RLPO or RS30D with or without positively charged inducing agent; 1,2-dioleoyl-3-trimethylammonium-propane, chloride salt (DOTAP); were used for preparation of nanoparticles. Blending between PLGA and Eudragit® RLPO or RS30D with inclusion of DOTAP caused a marked increase in entrapment efficiency and switched zeta potential from negative to positive. Nanoparticle formulations; NR3 (Levo-h:PLGA:Eudragit® RLPO; 1:1:1 w/w with DOTAP) and NS3 (Levo-h:PLGA:Eudragit® RS30D; 1:1:1 w/w with DOTAP) that possess high positive zeta potential (59.3 ± 7.5 and 55.1 ± 8.2 mV, respectively) and Efficient Levo-h entrapment (89.54 ± 1.5 and 77.65 ± 1.8%, respectively) were selected for further examinations; in vitro release, physical stability and microbiological study. NR3 and NS3 showed significant sustained release of Levo-h. NR3 and NS3 exhibited good stability after storage at room temperature. Microbiological assay showed strengthened antibacterial activity of NR3 against both types of gram-negative bacteria (E. coli, Ps. aeruginosa) and of NS3 against Ps. aeruginosa compared to free Levo-h solution. NR3 and NS3 appear to be promising oral delivery system for Levo-h.
a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Zagazig University , Zagazig , Egypt and.
Azza A
AA
Hasan
a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Zagazig University , Zagazig , Egypt and.
Shereen A
SA
Sabry
a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Zagazig University , Zagazig , Egypt and.
Marwa H
MH
Abdallah
b Microbiology and Immunology Department, Faculty of Pharmacy , Egyptian Russian University , Badr City , Egypt.
Dalia A
DA
El-Damasy
D000180:Acrylic Resins / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D000284:Administration, Oral; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D004926:Escherichia coli / Q000187:drug effects / Q000502:physiology; D006801:Humans; D064704:Levofloxacin / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D008826:Microbial Sensitivity Tests / Q000379:methods; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D011108:Polymers / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics
D000180:Acrylic Resins; D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D011108:Polymers; C050528:Eudragit RS; C058665:Eudragit RL; D064704:Levofloxacin
Eudragit; levofloxacin hemihydrate; nanoparticles; oral; poly(dl-lactide-co-glycolide); zeta potential