Self-assembled polymeric nanoparticle of PEGylated chitosan-ceramide conjugate for systemic delivery of paclitaxel
- Authors
- Battogtokh, Gantumur; Ko, Young Tag
- Issue Date
- Nov-2014
- Publisher
- TAYLOR & FRANCIS LTD
- Keywords
- Ceramide; chitosan; paclitaxel; PEGylation; polymeric nanoparticle
- Citation
- JOURNAL OF DRUG TARGETING, v.22, no.9, pp.813 - 821
- Journal Title
- JOURNAL OF DRUG TARGETING
- Volume
- 22
- Number
- 9
- Start Page
- 813
- End Page
- 821
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/12135
- DOI
- 10.3109/1061186X.2014.930469
- ISSN
- 1061-186X
- Abstract
- Chitosan has been widely explored as one of the most favorable biomaterials for various pharmaceutical applications due to its biodegradability and biocompatibility. Here, we report novel PEGylated-chitosan-ceramide (PEG-CS-CE) that forms stable polymeric nanoparticles capable of functioning as efficient carriers of hydrophobic drug molecules. The chitosan-ceramide conjugate (CS-CE) was linked with amine-polyethyleneglycol (NH2-PEG(2000)) by using dicyclohexylcarbodiimide/N-hydroxysuccinimide (DCC-NHS) to obtain PEG-CS-CE that could exhibit steric stabilization in biological environments. The structure of the conjugate was determined by proton (H-1) NMR and FT-IR spectrometry. Under suitable conditions, the PEG-CS-CE self-assembled to form colloidally stable nanoparticles with a mean diameter of similar to 200 nm. Further, hydrophobic anti-tumor agent paclitaxel (PTX) was incorporated into the polymeric nanoparticle with 90% loading efficiency and 11.3% loading capacity via an emulsion-solvent evaporation method. The PTX-loaded PEG-CS-CE nanoparticle showed sustained release and exhibited higher cellular uptake and a comparable cytotoxic efficacy to that of free PTX on B16F10 melanoma and MCF-7 human breast adenocarcinoma cell lines. The empty nanoparticle showed no toxicity, indicating that the co-polymer is safe to use in drug delivery. The polymeric nanoparticle PEG-CS-CE developed by us represent promising nanocarriers of hydrophobic drug molecules.
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