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.

Novel amoxicillin nanoparticles formulated as sustained release delivery system for poultry use

“…This is thought to be related to the low clearance and the length of the half‐life of amoxicillin‐loaded nps. In some studies, it has been reported that surfactants and polymers incorporated into the formulation cause prolonging half‐life of drugs by reducing reticuloendothelial system‐mediated clearance and opsonization of nanoparticles (Chaudhari et al., ; Mustafa, Devi, & Pai, ; Parveen & Sahoo, ). As a result of the evaluation based on the comparative plasma drug concentration–time curves, it was found that amoxicillin nps slowly releases in the gastrointestinal tract and provides steady‐state drug concentration for a longer period of time.…”

Lipid Nanoparticles-Encapsulated YF4: A Potential Therapeutic Oral Peptide Delivery System for Hypertension Treatment

“…PLGA nanoparticles, as a safe drug-loading system, can effectively slow the drug release and protect drugs from gastrointestinal degradation (Lozoya-Agullo et al, 2017; Mustafa et al, 2017). Then coating the lipid membrane on the particles can further protect the drugs from GI and improve the contact between the nanoparticles and the small intestinal epithelial cells, which may achieve the goal of prolonging the circulation in the blood.…”

Innovative Therapeutic and Delivery Approaches Using Nanotechnology to Correct Splicing Defects Underlying Disease

“…Another polymer frequently mixed with PLGA is polyethylene glycol (PEG) ( Zhang et al, 2014 ). PEG is a nonionic biocompatible polymer coated onto the surfaces of nanoparticles that prevents recognition and destruction of these carriers by the mononuclear phagocyte system (MPS), thereby increasing the plasma half-lives of the nanoparticles ( Mustafa et al, 2017 ). Furthermore, PEGylation of nanoparticles improves their stability by reducing intermolecular aggregation and the accessibility of the target site ( Gref et al, 2000 ).…”