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Singla, L. D.

Publications and source records attributed to Singla, L. D..

2 recordsLinked to original sources

Targeted drug delivery using Beeswax derived Albendazole-Loaded Solid Lipid Nanoparticles in Haemonchus contortus, an albendazole tolerant nematode.

Targeted delivery has not been achieved for anthelmintic treatment, resulting in the requirement of excess drugs dose leading to side effects and therapeutic resistance. Gastrointestinal helminths ingest lipid droplets from digestive fluid for energy production, development, and defense. Worms habit inspired us to develop biocompatible, oral administrable, bee-wax derived solid lipid nanoparticles (SLN) with excellent drug (albendazole) loading efficiency of 83.3 {+/-} 6.5 mg/g and sustained-release properties (86.4 {+/-} 3.9 % of drug released within 24 h). Rhodamine B-loaded SLN showed time-dependent release and distribution of dye in vivo in Haemonchous contortus. The intestinal sustained-release property was shown by the particles that caused enhancement of albendazole potency for up to 50 folds. Therefore, this formulation has immense potential as an anthelminthic drug delivery vehicle that will not only be able to reduce the dose but will also reduce the drug-induced side effects by enhancing the bioavailability of the drug. HighlightsO_LIAlbendazole-loaded Solid Lipid Nanoparticles (SLN-A) were formulated using Beeswax as stating material showing high drug loading capacity of 83 mg/g with sustained-release properties and 84 {+/-} 3 % of drug release within 24 h. C_LIO_LISLN-A particles showed 50 fold enhancement of Albendazole activity against Haemonchous contortus worm. C_LIO_LIRhodamine B-loaded SLN particles showed the specific uptake and in-vivo sustained release of dye in the worm. C_LI

microbiology

Targeting the nervous system of the parasitic worm, Haemonchus contortus, with quercetin.

High Prevalence of infection rate, limited choice of drugs and emerging resistance against these leads to an pressing need for the development of new antihelminthic drugs and drug targets. However, limited understanding of the physiology of worms has delayed the process substantially. Here, for the first time, we are reporting the tissue morphology of Haemonchus contortus, and target its nervous system with a quercetin, a naturally occurring flavonoid. Quercetin showed anthelmintic activity against all developmental stages of the nematode. Histological analysis demonstrated damage of various body parts including isthmus, brut, pseudocoele, and other organs. Mechanistic studies revealed the generation of oxidative stress and alteration of the stress response enzyme activities. Importantly, the time-dependent imaging of ROS-generation revealed the neuronal system as the primary target of quercetin in the adult worms, which eventually leads to the paralysis and death of the worms. This work demonstrates neuronal system as a novel drug target for quercetin. O_FIG O_LINKSMALLFIG WIDTH=200 HEIGHT=102 SRC="FIGDIR/small/451932v1_ufig1.gif" ALT="Figure 1"> View larger version (27K): org.highwire.dtl.DTLVardef@9204caorg.highwire.dtl.DTLVardef@789005org.highwire.dtl.DTLVardef@1375539org.highwire.dtl.DTLVardef@1bc4c47_HPS_FORMAT_FIGEXP M_FIG Graphical Abstract Schematic representation showing generation of Reactive Oxygen Stress in the nervous system of H. contortus due to quercetin treatment. C_FIG

biochemistry