title: Effect of PEG and water-soluble chitosan coating on moxifloxacin-loaded PLGA long-circulating nanoparticles.
abstract: Moxifloxacin (MOX) is a Mycobacterium tuberculosis DNA gyrase inhibitor. Due to its intense hydrophilicity, MOX is cleared from the body within 24 h and required for repetitive doses which may then result in hepatotoxicity and acquisition of MOX resistant-TB, related with its use. To overcome the aforementioned limitations, the current study aimed to develop PLGA nanoparticles (PLGA NPs), to act as an efficient carrier for controlled delivery of MOX. To achieve a substantial extension in blood circulation, a combined design, affixation of polyethylene glycol (PEG) to MOX-PLGA NPs and adsorption of water-soluble chitosan (WSC) (cationic deacetylated chitin) to particle surface, was rose for surface modification of NPs. Surface modified NPs (MOX-PEG-WSC NPs) were prepared to provide controlled delivery and circulate in the bloodstream for an extended period of time, thus minimizing dosing frequency. In vivo pharmacokinetic and in vivo biodistribution following oral administration were investigated. NP surface charge was closed to neutral +4.76 mV and significantly affected by the WSC coating. MOX-PEG-WSC NPs presented striking prolongation in blood circulation, reduced protein binding, and long-drawn-out the blood circulation half-life with resultant reduced liver sequestration vis-à-vis MOX-PLGA NPs. The studies, therefore, indicate the successful formulation development of MOX-PEG-WSC NPs that showed sustained release behavior from nanoparticles which indicates low frequency of dosing.
authors: Pharmaceutics Division, Faculty of Pharmacy, Al-Ameen College of Pharmacy, Near Lal Bagh Main gate, Hosur Road, Bangalore, Karnataka, 560027, India.
authors: Sanaul
authors: S
authors: Mustafa
authors: Pharmaceutics Division, Faculty of Pharmacy, Al-Ameen College of Pharmacy, Near Lal Bagh Main gate, Hosur Road, Bangalore, Karnataka, 560027, India. vkusumdevi@yahoomail.com.
authors: V Kusum
authors: VK
authors: Devi
authors: Pharmaceutics Division, Faculty of Pharmacy, Al-Ameen College of Pharmacy, Near Lal Bagh Main gate, Hosur Road, Bangalore, Karnataka, 560027, India.
authors: Roopa S
authors: RS
authors: Pai
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D048271:Chitosan / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D065546:Drug Liberation; D024841:Fluoroquinolones / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D019344:Lactic Acid / Q000008:administration & dosage / Q000737:chemistry; D008297:Male; D046529:Microscopy, Electron, Transmission; D000077266:Moxifloxacin; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry / Q000648:ultrastructure; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D011100:Polyglycolic Acid / Q000008:administration & dosage / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D017208:Rats, Wistar; D012995:Solubility; D014018:Tissue Distribution; D059005:Topoisomerase II Inhibitors / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D014867:Water
chemical_list: D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D024841:Fluoroquinolones; D059005:Topoisomerase II Inhibitors; D014867:Water; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; D048271:Chitosan; D000077266:Moxifloxacin
keywords: Chitosan; Long circulating nanoparticles; Moxifloxacin; Resistant TB