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Heparin appended ADH-anionic polysaccharide nanoparticles for site-specific delivery of usnic acid.
- Source :
-
International journal of pharmaceutics [Int J Pharm] 2019 Feb 25; Vol. 557, pp. 238-253. Date of Electronic Publication: 2018 Dec 27. - Publication Year :
- 2019
-
Abstract
- The intention of present research work is to formulate usnic acid (UA) loaded heparin modified gellan gum (HAG) nanoparticles (NPs). HAG copolymer based conjugation was synthesized and characterized by <superscript>1</superscript> H NMR and FT-IR spectroscopy. Plain and UA loaded HAG NPs were prepared via nanoprecipitation technique. NPs were typified and further characterized for particle size, polydispersity index, entrapment efficiency, zeta potential, atomic force microscopy, differential scanning calorimetry, X-ray diffraction analysis, and in-vitro release. In-vitro tube formation assay, tumorsphere assay, autophagy assay, DNA cleavage assay, internalization by confocal and FACS based internalization analysis, caspase assay and cell cycle assay were performed for biological activity. Obtained experimental results explored that HAG NPs displayed a sustained release of UA (95.67% in 48 h) compared to gellan gum NPs (96.12% in 8 h). In cytotoxicity studies, UA loaded HAG NPs exhibited an enormous cytotoxic potential against A549 cancer cells. In the in vivo bio-distribution study, using albino rat model the free UA concentration was found 7.09 ± 0.9%, 2.7 ± 1.5%, 7.5 ± 2.1, 9.2 ± 2%, and 6.25 ± 1.3% post two hours of intravenous administration, however, in the case of UA loaded HAG NPs the obtained level was 4.1 ± 1.10, 7.7 ± 1.30%, 2.21 ± 0.29%, 1.85 ± 0.25%, 2.2 ± 0.78%, 2.9 ± 1.21% respectively, in heart, lung, liver, spleen, intestine and kidney. The overall anticancer study and result of internalization deciphered the higher anticancer potential of UA loaded HAG NPs.<br /> (Copyright © 2018 Elsevier B.V. All rights reserved.)
- Subjects :
- A549 Cells
Adipates chemistry
Adipates pharmacokinetics
Animals
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacokinetics
Apoptosis drug effects
Benzofurans chemistry
Benzofurans pharmacokinetics
Cell Cycle drug effects
Drug Carriers chemistry
Drug Carriers pharmacokinetics
Drug Liberation
Erythrocytes drug effects
Hematologic Tests
Hemolysis drug effects
Heparin chemistry
Heparin pharmacokinetics
Humans
Male
Nanoparticles chemistry
Polysaccharides, Bacterial chemistry
Polysaccharides, Bacterial pharmacokinetics
Rats
Adipates administration & dosage
Antineoplastic Agents administration & dosage
Benzofurans administration & dosage
Drug Carriers administration & dosage
Heparin administration & dosage
Nanoparticles administration & dosage
Polysaccharides, Bacterial administration & dosage
Subjects
Details
- Language :
- English
- ISSN :
- 1873-3476
- Volume :
- 557
- Database :
- MEDLINE
- Journal :
- International journal of pharmaceutics
- Publication Type :
- Academic Journal
- Accession number :
- 30594688
- Full Text :
- https://doi.org/10.1016/j.ijpharm.2018.12.049