Chitosan amphiphiles provide new drug delivery opportunities

Uchegbu, Ijeoma F.; Carlos, Margarida Isabel Simão; McKay, Cameron; Hou, Xueliang; Schätzlein, Andreas

doi:10.1002/pi.4721

Cited by 28 publications

(30 citation statements)

References 58 publications

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“…58 Higher colloidal stability and kinetically low dissociation allow the DOX-GCPQ nanoformulation to circulate in the blood for longer time and thus, significantly increase its accumulation at the target site due to enhanced permeation by passive targeting and retention effect. 40 Furthermore, slow drug release from nanoformulation is advantageous to localize cytotoxic drug to tumor site. 48 Henceforth, DOX-GCPQ nanoformulation showed significant improvement in tumor accumulation as compared to the free DOX.…”

Section: Resultsmentioning

confidence: 99%

“…The synthesized GCPQ was able to self-assemble at low critical micelle concentration (CMC) into particles of colloidal size that also indicated its colloidal stability. 40 DOX was loaded into GCPQ by probe sonication. To achieve the optimized GCPQ nanoparticle with desired features such as size ,100 nm, PDI value ,1, zeta potential $25 mV, and loading 80%, parameters such as drug amount, polymer amount, sonication speed, and the sonication parameters were manipulated since these factors have reported to affect the size of the nanoparticles.…”

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Doxorubicin-loaded quaternary ammonium palmitoyl glycol chitosan polymeric nanoformulation: uptake by cells and organs

Kanwal¹,

Bukhari²,

Rana

et al. 2018

IJN

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PurposeThis study was aimed to develop doxorubicin-loaded quaternary ammonium palmitoyl glycol chitosan (DOX–GCPQ) nanoformulation that could enable DOX delivery and noninvasive monitoring of drug accumulation and biodistribution at tumor site utilizing self-florescent property of doxorubicin.Materials and methodsDOX–GCPQ amphiphilic polymeric nanoformulations were prepared and optimized using artificial neural network (ANN) and characterized for surface morphology by atomic force microscopy, particle size with polydispersity index (PDI), and zeta potential by dynamic light scattering. Fourier transformed infrared (FTIR) and X-ray diffractometer studies were performed to examine drug polymer interaction. The ANN-optimized nanoformulation was investigated for in vitro release, cellular, tumor, and tissue uptake.ResultsThe optimized DOX–GCPQ nanoformulation was anionic spherical micelles with the hydrodynamic particle size of 97.8±1.5 nm, the PDI of <0.3, the zeta potential of 28±2 mV, and the encapsulation efficiency of 80%±1.5%. Nanoformulation demonstrated a sustained release pattern over 48 h, assuming Weibull model. Fluorescence microscopy revealed higher uptake of DOX–GCPQ in human rhabdomyosarcoma (RD) cells as compared to free DOX. In vitro cytotoxicity assay indicated a significant cytotoxicity of DOX–GCPQ against RD cells as compared to DOX and blank GCPQ (P<0.05). DOX–GCPQ exhibited low IC50 (1.7±0.404 µmol) when compared to that of DOX (3.0±0.968 µmol). In skin tumor xenografts, optical imaging revealed significantly lower DOX–GCPQ in heart and liver (P<0.05) and accumulated mainly in tumor (P<0.05) as compared to other tissues.ConclusionThe features of nanoformulation, ie, small particle size, sustained drug release, and enhanced cellular uptake, potential to target tumor passively coupled with the possibility of monitoring of tumor localization by optical imaging may make DOX–GCPQ an efficient nanotheranostic system.

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Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Doxorubicin-loaded quaternary ammonium palmitoyl glycol chitosan polymeric nanoformulation: uptake by cells and organs

Kanwal¹,

Bukhari²,

Rana

et al. 2018

IJN

View full text Add to dashboard Cite

show abstract

“…The 6-O-glycol unit enables GCPQ to produce micelles at neutral pH, as chitosan is insoluble in neutral media and is only soluble at acid pH, whereas GC is soluble at neutral pH. 27 GCPQ48 shows some interesting rheological behaviour ( Figs. 4 and 5) forming transient micellar networks at high concentration (Fig.…”

Section: Discussionmentioning

confidence: 99%

Physical Characterisation and Long-Term Stability Studies on Quaternary Ammonium Palmitoyl Glycol Chitosan (GCPQ)—A New Drug Delivery Polymer

Chooi

Carlos

Soundararajan

et al. 2014

Journal of Pharmaceutical Sciences

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“…CS is a renewable and sustainable cationic biopolymer derived from alkaline partial deacetylation of chitin, one of the most abundant biopolymers in nature and acquired from crustacean and insect exoskeletons. Additionally, CS can be obtained from enzymatic extraction of Aspergillus niger mycelia originated from the industrial production of citric acid and from cultivated edible mushrooms, like Agaricus bisporus [13]. CS is a non-toxic, biocompatible and biodegradable hydrophilic polymer with low immunogenicity that received FDA approval for wound dressings as well as in dietary application.…”

Section: Introductionmentioning

confidence: 99%

Staggered Herringbone Microfluid Device for the Manufacturing of Chitosan/TPP Nanoparticles: Systematic Optimization and Preliminary Biological Evaluation

Chiesa

Greco

Riva

et al. 2019

IJMS

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Chitosan nanoparticles (CS NPs) showed promising results in drug, vaccine and gene delivery for the treatment of various diseases. The considerable attention towards CS was owning to its outstanding biological properties, however, the main challenge in the application of CS NPs was faced during their size-controlled synthesis. Herein, ionic gelation reaction between CS and sodium tripolyphosphate (TPP), a widely used and safe CS cross-linker for biomedical application, was exploited by a microfluidic approach based on a staggered herringbone micromixer (SHM) for the synthesis of TPP cross-linked CS NPs (CS/TPP NPs). Screening design of experiments was applied to systematically evaluate the main process and formulative factors affecting CS/TPP NPs physical properties (mean size and size distribution). Effectiveness of the SHM-assisted manufacturing process was confirmed by the preliminary evaluation of the biological performance of the optimized CS/TPP NPs that were internalized in the cytosol of human mesenchymal stem cells through clathrin-mediated mechanism. Curcumin, selected as a challenging model drug, was successfully loaded into CS/TPP NPs (EE% > 70%) and slowly released up to 48 h via the diffusion mechanism. Finally, the comparison with the conventional bulk mixing method corroborated the efficacy of the microfluidics-assisted method due to the precise control of mixing at microscales.

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Chitosan amphiphiles provide new drug delivery opportunities

Abstract: Chitosan amphiphiles self‐assemble into nanoparticles that are used for drug delivery. These chitosan amphiphile nanoparticles significantly enhance the oral absorption of hydrophobic drugs such as cyclosporine A for example.

Cited by 28 publications

References 58 publications

Doxorubicin-loaded quaternary ammonium palmitoyl glycol chitosan polymeric nanoformulation: uptake by cells and organs

Doxorubicin-loaded quaternary ammonium palmitoyl glycol chitosan polymeric nanoformulation: uptake by cells and organs

Physical Characterisation and Long-Term Stability Studies on Quaternary Ammonium Palmitoyl Glycol Chitosan (GCPQ)—A New Drug Delivery Polymer

Staggered Herringbone Microfluid Device for the Manufacturing of Chitosan/TPP Nanoparticles: Systematic Optimization and Preliminary Biological Evaluation

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