From the results it´s clear that anovel nanoparticle drug-polymer conjugate has been synthesized...
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From the results it´s clear that anovel nanoparticle drug-polymer conjugate has been synthesized with suitable properties for light activated therapy. This new chitosan nanocarrier is hydrophilic an forms stable nanoparticles with average diameter of 216 nm. The chemical properties of the TEG-TPP-PIP-chitosan nanocarrier can be utilized in targeted drug delivery such as photochemical internalization (PCI). E-mail: [email protected] Chitosan used for the synthesis (95% DD, 95 cp) was provided from Genis EHF, Iceland. All other chemicals were commercially available. To analyze the synthesized compounds, 1H NMR, 13C NMR spectra were recorded on a Bruker Avance 400 MHz NMR Spectrometer. Mass spectra were recorded on a Bruker micrOTOF-Q instrument with ESI. UV-Vis measurements were recorded on a Perkin-Elmer Lambda 25 UV-Vis. All DLS and zeta potential measurements were performed on a Nanotrac wave-Zeta (ZS), (Microtrac, USA). Conclusion Introduction Aim Materials and Methods The main objective of this research was to synthesize neutral amphiphilic nanocarriers (drug- polymer conjugates) with suitable properties for photochemical internalization (PCI). RESULTS The decrease in TER values was associated with increased paracellular permeability of FITC-labeled dextran 4 kDa with the highest increase in permeability obtained after treatment with QuatButyl followed closely by QuatHexyl, than QuatPropyl and finally TMC (Figure 3). PEGylated chitosan nanocarriers for light activated cancer therapy - Synthesis and characterization Ingolfur Magnusson 1 , Elvar Örn Viktorsson 1 , Vivek S. Gaware 1 , Mar Masson 1 1 Faculty of Pharmaceutical Sciences, University of Iceland, Reykjavik, Iceland. In recent decades, derivatives of natural carbohydrate polymers like chitosan have received attention for their possible utilization in nanoscale drug delivery systems. Such systems could be used to overcome some of the problems associated with many traditional anti-cancer agents, such as low solubility and ineffective tumor targeting[1]. Drug-polymer conjugates have now become well-established nanoscale systems which can be utilized in cancer therapy to improve solubility of lipophilic drugs in order to achieve more specific tumor targeting by taking advantage of the enhanced permeability and retention (EPR) effect[2]. In the current study, lipophilic photosensitizer and polar derivatives of triethyleneglycol (TEG) were attached to the backbone of TBDMS-O-protected chitosan. Nucleophilic and electrophilic substitutions were utilized for these reactions and reductive alkylation was also attempted. Figure 2. 1 H NMR of TEGylated-TPP-piperazine chitosan nanocarrier $ % $TXHRXV SKDVH &+&O SKDVH Figure 3. Size distibution measurment of Chitosan nanoparicles measured by DLS Figure 4. Partition experiment A) TPP-PIP in organic phase B) TEGylated TPP-PIP- chitosan in aqueous phase NMR spetra in figure 2 shows that the chitosan polymer synthesized, has TEG and tetraphenylporphyrine (TPP) in it´s backbone. DLS measurment shows that the chitosan material forms nanoparticles with avarge diameiter of 216 nm and Z-potential of 86,82 mV. The partion experiment indicates that the chitosan polymer is watersoluble and that the TPP-PIP moiety is lipophilic.
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Transcript of From the results it´s clear that anovel nanoparticle drug-polymer conjugate has been synthesized...
From the results it´s clear that anovel nanoparticle drug-polymer conjugate has been synthesized with suitable properties for light activated therapy. This new chitosan nanocarrier is hydrophilic an forms stable nanoparticles with average diameter of 216 nm. The chemical properties of the TEG-TPP-PIP-chitosan nanocarrier can be utilized in targeted drug delivery such as photochemical internalization (PCI).
E-mail: [email protected]
Chitosan used for the synthesis (95% DD, 95 cp) was provided from Genis EHF, Iceland. All other chemicals were commercially available. To analyze the synthesized compounds, 1H NMR, 13C NMR spectra were recorded on a Bruker Avance 400 MHz NMR Spectrometer. Mass spectra were recorded on a Bruker micrOTOF-Q instrument with ESI. UV-Vis measurements were recorded on a Perkin-Elmer Lambda 25 UV-Vis. All DLS and zeta potential measurements were performed on a Nanotrac wave-Zeta (ZS), (Microtrac, USA).
Conclusion
Introduction
Aim
Materials and Methods
The main objective of this research was to synthesize neutral amphiphilic nanocarriers (drug-polymer conjugates) with suitable properties for photochemical internalization (PCI).
RESULTS The decrease in TER values was associated with increased paracellular permeability of FITC-labeled dextran 4 kDa with the highest increase in permeability obtained after treatment with QuatButyl followed closely by QuatHexyl, than QuatPropyl and finally TMC (Figure 3).
PEGylated chitosan nanocarriers for light activatedcancer therapy - Synthesis and characterization
Ingolfur Magnusson1, Elvar Örn Viktorsson1, Vivek S. Gaware1, Mar Masson1
1Faculty of Pharmaceutical Sciences, University of Iceland, Reykjavik, Iceland.
In recent decades, derivatives of natural carbohydrate polymers like chitosan have received attention for their possible utilization in nanoscale drug delivery systems. Such systems could be used to overcome some of the problems associated with many traditional anti-cancer agents, such as low solubility and ineffective tumor targeting[1]. Drug-polymer conjugates have now become well-established nanoscale systems which can be utilized in cancer therapy to improve solubility of lipophilic drugs in order to achieve more specific tumor targeting by taking advantage of the enhanced permeability and retention (EPR) effect[2]. In the current study, lipophilic photosensitizer and polar derivatives of triethyleneglycol (TEG) were attached to the backbone of TBDMS-O-protected chitosan. Nucleophilic and electrophilic substitutions were utilized for these reactions and reductive alkylation was also attempted.
Figure 2. 1H NMR of TEGylated-TPP-piperazine chitosan nanocarrier
$ %
$ TXHRXV SKDVH
&+&O
SKDVH
Figure 3. Size distibution measurment of Chitosan nanoparicles measured by DLS
Figure 4. Partition experimentA) TPP-PIP in organic phaseB) TEGylated TPP-PIP- chitosanin aqueous phase
NMR spetra in figure 2 shows that the chitosan polymer synthesized, has TEG and tetraphenylporphyrine (TPP) in it´s backbone. DLS measurment shows that the chitosan material forms nanoparticles with avarge diameiter of 216 nm and Z-potential of 86,82 mV. The partion experiment indicates that the chitosan polymer is watersoluble and thatthe TPP-PIP moiety is lipophilic.
