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A Chitosan-PLGA based catechin hydrate nanoparticles used in targeting of lungs and cancer treatment |
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| Institution: | 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 |
| 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. |
| 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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