A Chitosan-PLGA based catechin hydrate nanoparticles used in targeting of lungs and cancer treatment |
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| Affiliation: | 1. Department of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia;2. Department of Pharmaceutical Chemistry, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia;3. Department of Natural Products and Alternative Medicine, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia;4. Department of Pharmaceutics, School of Medical and Allied Sciences, Galgotias University, Gautam Budh Nagar, Greater Noida 201310, India |
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| Abstract: | ObjectiveTo prepare a novel Chitosan (CS)-coated-PLGA-NPs of catechin hydrate (CTH) and to improve lungs bioavailability via direct nose to lungs-delivery for the comparative assessment of a pulmokinetics study by the first-time UHPLC-MS/MS developed method in the treatment of lungs cancer via anticancer activities on H1299 lung cancer cells.Material and methodsPLGA-NPs was prepared by solvent evaporation (double emulsion) method followed by coated with chitosan (CS) and evaluated based on release and permeation of drug, a comparative pulmokinetics study with their anticancer activities on H1299 lung cancer cells.ResultsThe particle size, PDI and ZP of the optimized CAT-PLGA-NPs and CS-CAT-PLGA-NPs were determined 124.64 ± 12.09 nm and 150.81 ± 15.91 nm, 0.163 ± 0.03 and 0.306 ± 0.03, –3.94 ± 0.19 mV and 26.01 ± 1.19 mV respectively. Furthermore, higher entrapment efficiency was observed for CS-CAT PLGA NPs. The release pattern of the CS-CAT-PLGA NPs was found to favor the release of entrapped CAT within the cancer microenvironment. CS-CAT-PLGA-NPs exposed on H1299 cancer cells upto 24.0 h was found to be higher cytotoxic as compared to CAT-solution (CAT-S). CS-CAT-PLGA-NPs showed higher apoptosis of cancer cells after their exposure as compared to CAT-S. CS-CTH-PLGA-NPs showed tremendous mucoadhesive-nature as compared to CTH-S and CS-CTH-PLGA NPs by retention time (RT) of 0.589 min, and m/z of 289.21/109.21 for CTH alongwith RT of 0.613 min and m/z of 301.21/151.21 was found out for IS (internal standard), i.e. Quercetin). Likewise, for 1–1000 ng mL−1 (linear range) of % accuracy (92.01–99.31%) and %CV (inter & intra-day, i.e. 2.14–3.33%) was determined. The improved Cmax with AUC0–24 was observed extremely significant (p < 0.001) via i.n. as compared oral and i.v. in the wistar rat’s lungs. The CS-approach was successfully designed and safely delivered CAT to the lungs without causing any risk.ConclusionCS-CTH-PLGA-NPs were showed a significant role (p < 0.001) for the enhancement of lungs-bioavailability and potentially promising approach to treat lung cancers. CS-CTH-PLGA-NPs did not cause any toxicity, it showed safety and have no obvious toxic-effects on the rat’s lungs and does not produce any mortality followed by no abnormal findings in the treated-rats. |
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| Keywords: | Catechin hydrate CS-CTH-PLGA-NPs Lung cancer Apoptosis UHPLC-MS/MS Lungs comparative pulmokinetics CTH" },{" #name" :" keyword" ," $" :{" id" :" k0040" }," $$" :[{" #name" :" text" ," _" :" Catechin hydrate CS" },{" #name" :" keyword" ," $" :{" id" :" k0050" }," $$" :[{" #name" :" text" ," _" :" chitosan NPs" },{" #name" :" keyword" ," $" :{" id" :" k0060" }," $$" :[{" #name" :" text" ," _" :" nanoparticles CS-CTH-PLGA-NPs" },{" #name" :" keyword" ," $" :{" id" :" k0070" }," $$" :[{" #name" :" text" ," _" :" chitosan-coated catechin hydrate-loaded-PLGA-nanoparticles PVA" },{" #name" :" keyword" ," $" :{" id" :" k0080" }," $$" :[{" #name" :" text" ," _" :" polyvinyl alcohol DCM" },{" #name" :" keyword" ," $" :{" id" :" k0090" }," $$" :[{" #name" :" text" ," _" :" dichloromethane UHPLC-MS/MS" },{" #name" :" keyword" ," $" :{" id" :" k0100" }," $$" :[{" #name" :" text" ," _" :" ultra high performance liquid chromatography mass spectroscopy and mass spectroscopy ESI" },{" #name" :" keyword" ," $" :{" id" :" k0110" }," $$" :[{" #name" :" text" ," _" :" Electrospray ionization PDI" },{" #name" :" keyword" ," $" :{" id" :" k0120" }," $$" :[{" #name" :" text" ," _" :" polydispersity index SEM" },{" #name" :" keyword" ," $" :{" id" :" k0130" }," $$" :[{" #name" :" text" ," _" :" scanning electron microscope TEM" },{" #name" :" keyword" ," $" :{" id" :" k0140" }," $$" :[{" #name" :" text" ," _" :" transmission electron microscope LC" },{" #name" :" keyword" ," $" :{" id" :" k0150" }," $$" :[{" #name" :" text" ," _" :" loading capacity EE" },{" #name" :" keyword" ," $" :{" id" :" k0160" }," $$" :[{" #name" :" text" ," _" :" entrapment efficiency DSC" },{" #name" :" keyword" ," $" :{" id" :" k0170" }," $$" :[{" #name" :" text" ," _" :" differential scanning calorimetry PBS" },{" #name" :" keyword" ," $" :{" id" :" k0180" }," $$" :[{" #name" :" text" ," _" :" phosphate buffered solution CC" },{" #name" :" keyword" ," $" :{" id" :" k0190" }," $$" :[{" #name" :" text" ," _" :" calibration curve IS" },{" #name" :" keyword" ," $" :{" id" :" k0200" }," $$" :[{" #name" :" text" ," _" :" internal standard CH-S" },{" #name" :" keyword" ," $" :{" id" :" k0210" }," $$" :[{" #name" :" text" ," _" :" catechin-hydrate-suspension LLOQ" },{" #name" :" keyword" ," $" :{" id" :" k0220" }," $$" :[{" #name" :" text" ," _" :" liquid–liquid extraction: LLE: lower limit of quantification LLOQQC" },{" #name" :" keyword" ," $" :{" id" :" k0230" }," $$" :[{" #name" :" text" ," _" :" lower limit of quantification for quality control MQC" },{" #name" :" keyword" ," $" :{" id" :" k0240" }," $$" :[{" #name" :" text" ," _" :" low quality control: LQC: middle quality control HQC" },{" #name" :" keyword" ," $" :{" id" :" k0250" }," $$" :[{" #name" :" text" ," _" :" high quality control maximum plasma concentration Kel" },{" #name" :" keyword" ," $" :{" id" :" k0270" }," $$" :[{" #name" :" text" ," _" :" elimination rate constant half-life AUC" },{" #name" :" keyword" ," $" :{" id" :" k0300" }," $$" :[{" #name" :" text" ," _" :" area under curve LOD" },{" #name" :" keyword" ," $" :{" id" :" k0310" }," $$" :[{" #name" :" text" ," _" :" lower limit of detection LOQ" },{" #name" :" keyword" ," $" :{" id" :" k0320" }," $$" :[{" #name" :" text" ," _" :" lower limit of quantitation ANOVA" },{" #name" :" keyword" ," $" :{" id" :" k0330" }," $$" :[{" #name" :" text" ," _" :" analysis of variance |
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