Preparation and testing of cefquinome-loaded poly lactic-co-glycolic acid microspheres for lung targeting

Abstract

The aim of this study was to prepare cefquinome-loaded poly lactic-co-glycolic acid (PLGA) microspheres and to evaluate their in vitro and in vivo characteristics. Microspheres were prepared using a spry drier and were characterized in terms of morphology, size, drug-loading coefficient, encapsulation ratio and in vitro release. The prepared microspheres were spherical with smooth surfaces and uniform size (12.4 ± 1.2 μm). The encapsulation efficiency and drug loading of cefquinome was 91.6 ± 2.6 and 18.3 ± 1.3%, respectively. In vitro release of cefquinome from the microspheres was sustained for 36 h. In vivo studies identified the lung as the target tissue and the region of maximum cefquinome release. A partial lung inflammation was observed but disappeared spontaneously as the microspheres were removed through in vivo decay. The sustained cefquinome release from the microspheres revealed its applicability as a drug delivery system that minimized exposure to healthy tissues while increasing the accumulation of therapeutic drug at the target site. These results indicated that the spray-drying method of loading cefquinome into PLGA microspheres is a straightforward method for lung targeting in animals.

Rutin Attenuates Vancomycin-Induced Nephrotoxicity by Ameliorating Oxidative Stress, Apoptosis, and Inflammation in Rats

“…For light microscopy examination of histological sections, the right kidneys from 5 rats in each group were processed and fixed in 10% neutral buffered formalin. The formalin fixed tissue was embedded in paraffin, sliced into 4-m tissue sections and stained with hematoxylin-eosin (H&E) (48,49). Five coded sections from each group were evaluated blindly by a pathologist who was not revealed of the treatment scheme implemented as described previously (50).…”

Cefquinome-loaded microsphere formulations againstKlebsiella pneumoniainfection during experimental infections

“…CEQ is unsuitable for in vivo use due to its short biological half-life and toxicity (Wang et al., 2014 ). To alleviate these effects and give sustained delivery of therapeutic agents to the lungs, particulate delivery systems such as liposomes and polymeric nano- and micro-particles have been used (Chi et al., 2015 ; Zhang et al., 2015 ; Qu et al., 2017 ). Biodegradable microspheres have been extensively studied for almost half a century and encapsulation using PLA particles is a successful practice in both clinical and research settings (Khairnar et al., 2014 ; De Clercq et al., 2016 ).…”

“…Microsphere drug delivery systems (or microspheres) are an alternative to uncomplexed drug delivery and provide a slower intracellularly release of therapeutic drug doses (Liu et al., 2003 ). Biodegradable polymers such as polylactic acid (PLA), polylactic-co-glycolic acid (PLGA) and albumin have been used for microsphere encapsulation matrices and are biologically inert and nontoxic (Okada et al., 1995 ; Qu et al., 2017 ). The rate and extent of drug release from microspheres is dependent upon the particle size, extent of crosslinking as well as the physiochemical properties of the drug (Deng et al., 1999 ).…”

Chlorogenic acid prevents vancomycin‐induced nephrotoxicity without compromising vancomycin antibacterial properties

“…The samples were dewaxed in xylene and dehydrated in serial dilutions of alcohol and then processed in paraffin. These samples were then cut at 4 μm thicknesses using a microtome and counter‐stained with hematoxylin and eosin (H and E) for histopathological analysis by light microscopy (Qu et al, 2017, 2018). The slides were examined by a pathologist‐blinded to the treatment groups and a semiquantitative assessment of renal histological damage was performed and a semi‐quantitative score (SQS) was used as described (Roberts et al, 2015).…”

“…The samples were dewaxed in xylene and dehydrated in serial dilutions of alcohol and then processed in paraffin. These samples were then cut at 4 μm thicknesses using a microtome and counter-stained with hematoxylin and eosin (H and E) for histopathological analysis by light microscopy (Qu et al, 2017(Qu et al, , 2018.…”