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Review
. 2021 Oct 14;13(10):1686.
doi: 10.3390/pharmaceutics13101686.

Chitosan Nanoparticles at the Biological Interface: Implications for Drug Delivery

Noorjahan Aibani  1 , Raj Rai  1 , Parth Patel  1 , Grace Cuddihy  1 , Ellen K Wasan  1
Affiliations
Review

Chitosan Nanoparticles at the Biological Interface: Implications for Drug Delivery

Noorjahan Aibani et al. Pharmaceutics. .

Abstract

The unique properties of chitosan make it a useful choice for various nanoparticulate drug delivery applications. Although chitosan is biocompatible and enables cellular uptake, its interactions at cellular and systemic levels need to be studied in more depth. This review focuses on the various physical and chemical properties of chitosan that affect its performance in biological systems. We aim to analyze recent research studying interactions of chitosan nanoparticles (NPs) upon their cellular uptake and their journey through the various compartments of the cell. The positive charge of chitosan enables it to efficiently attach to cells, increasing the probability of cellular uptake. Chitosan NPs are taken up by cells via different pathways and escape endosomal degradation due to the proton sponge effect. Furthermore, we have reviewed the interaction of chitosan NPs upon in vivo administration. Chitosan NPs are immediately surrounded by a serum protein corona in systemic circulation upon intravenous administration, and their biodistribution is mainly to the liver and spleen indicating RES uptake. However, the evasion of RES system as well as the targeting ability and bioavailability of chitosan NPs can be improved by utilizing specific routes of administration and covalent modifications of surface properties. Ongoing clinical trials of chitosan formulations for therapeutic applications are paving the way for the introduction of chitosan into the pharmaceutical market and for their toxicological evaluation. Chitosan provides specific biophysical properties for effective and tunable cellular uptake and systemic delivery for a wide range of applications.

Keywords: biodistribution; biological; cellular uptake; chitosan nanoparticles; intracellular.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Modes of cellular uptake and eventual fate of chitosan in cells.
Figure 2
Figure 2
Effect of particle size on cellular uptake pathways depicting energy dependent uptake of larger sized NPs and passive uptake of small NPs.
Figure 3
Figure 3
Lifespan of chitosan nanoparticles.
See this image and copyright information in PMC

References

    1. Calvo P., Remuñán-López C., Vila-Jato J.L., Alonso M.J. Novel Hydrophilic Chitosan-Polyethylene Oxide Nanoparticles as Protein Carriers. J. Appl. Polym. Sci. 1997;63:125–132. doi: 10.1002/(SICI)1097-4628(19970103)63:1<125::AID-APP13>3.0.CO;2-4. - DOI
    1. Calvo P., Vila-Jato J.L., Alonso M.J. Evaluation of Cationic Polymer-Coated Nanocapsules as Ocular Drug Carriers. Int. J. Pharm. 1997;153:41–50. doi: 10.1016/S0378-5173(97)00083-5. - DOI
    1. Berthold A., Cremer K., Kreuter J. Preparation and Characterization of Chitosan Microspheres as Drug Carrier for Prednisolone Sodium Phosphate as Model for Anti-Inflammatory Drugs. J. Control Release. 1996;39:17–25. doi: 10.1016/0168-3659(95)00129-8. - DOI
    1. Ojeda-Hernández D.D., Canales-Aguirre A.A., Matias-Guiu J., Gomez-Pinedo U., Mateos-Díaz J.C. Potential of Chitosan and Its Derivatives for Biomedical Applications in the Central Nervous System. Front. Bioeng. Biotechnol. 2020;8:389. doi: 10.3389/fbioe.2020.00389. - DOI - PMC - PubMed
    1. Wang W., Meng Q., Li Q., Liu J., Zhou M., Jin Z., Zhao K. Chitosan Derivatives and Their Application in Biomedicine. Int. J. Mol. Sci. 2020;21:487. doi: 10.3390/ijms21020487. - DOI - PMC - PubMed

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