ABSTRACT
The objective of the present study was to develop superparamagnetic chitosan(CS) � dextran sulfate(DS) hydrogels as a intelligent drug system for effective carrying of Chlorin E6(chn E6) photosensitizer to cancer cells. This system can be detectable by magnetic Resonance Imaging technique. The study shows that the lifetime of the triplet state for chn E6 photosensitizer is significantly increase when encapsulate into hydrogel. In addition to the possible enhancement of 1O2 generation, other advantages to incorporating chn E6 -based PS agents into hydrogel include the ability to solubilize these generally hydrophobic agents, the small and uniform size of hydrogels, and potential for passive targeting of solid tumors via the enhanced permeation and retention effect decreasing systemic photosensitization.
Subject(s)
Drug Carriers/chemistry , Hydrogel, Polyethylene Glycol Dimethacrylate/chemical synthesis , Light , Magnetics , Nanoparticles/chemistry , Porphyrins/chemical synthesis , Capsules , Cell Line, Tumor , Cells, Cultured , Chlorophyllides , Humans , Hydrogel, Polyethylene Glycol Dimethacrylate/chemistry , Hydrogel, Polyethylene Glycol Dimethacrylate/pharmacokinetics , Microscopy, Electron, Scanning , Particle Size , Porphyrins/chemistry , Porphyrins/pharmacokineticsABSTRACT
The objective of the present study was to develop carboxymethyl starch (CMS) and dextran sulfate (DS) hydrogels that are able to efficiently encapsulate 5-,10-,15-,20-tetrakis(meso-hydroxyphenyl)porphyrin (mTHPP), a porphyrin-based PS agent. The study showed that the lifetime of the triplet state for porphyrin PS is significantly increase when encapsulate into hydrogel. In addition to the possible enhancement of ¹O2 generation, other advantages to incorporating porphyrin-based PS agents into hydrogel include the ability to solubilize these generally hydrophobic agents, the small and uniform size of hydrogels, and potential for passive targeting of solid tumors via the enhanced permeation and retention effect decreasing systemic photosensitization. This novel type of carboxymethyl starch (CMS) hydrogel using dextran sulfate (DS) as a polyanionic polymer was developed to achieve complex coacervation for the incorporation and controlled release of an anti-angiogenesis hexapeptide, this was the first report describing the use of DS to formulate CMS based hydrogels.
Subject(s)
Hydrogels/chemistry , Hydrogels/chemical synthesis , Neoplasms/therapy , Photochemotherapy , Porphyrins/chemistry , Starch/analogs & derivatives , Amylases/metabolism , Chemistry Techniques, Synthetic , Dextran Sulfate/chemistry , Drug Carriers/chemical synthesis , Drug Carriers/chemistry , Photosensitizing Agents/chemistry , Photosensitizing Agents/therapeutic use , Porphyrins/therapeutic use , Starch/chemistry , ViscosityABSTRACT
A novel drug delivery system for the treatment of brain tumors was formulated by methotrexate (MTX)-loaded polymeric nanoparticles (NPs) based on Glycol chitosan (GCS) and Dextran sulfate (DS). The physicochemical properties of resulting particles were investigated, evidencing the contribution of these nanoparticles for brain targeting. In vitro release of MTX was also evaluated. The GCS-DS nanoparticles have been developed based on the modulation of ratio show promise as a system for controlled delivery of the drug to the brain.
Subject(s)
Brain Neoplasms/drug therapy , Chitosan/chemical synthesis , Dextran Sulfate/chemical synthesis , Nanoparticles/chemistry , Chitosan/chemistry , Drug Compounding , Hydrogen-Ion Concentration , Methotrexate/therapeutic use , Molecular Weight , Nanoparticles/ultrastructure , TemperatureABSTRACT
Local drug delivery strategies have gained momentum recently as a promising modality in cancer therapy. In order to deliver Letrozole (LTZ) at the tumor site in therapeutically relevant concentrations, acetyl-polyamidoamine (Ac-PAMAM)-thiolated chitosan (TCS) films were fabricated. LTZ could be loaded at 31% wt/wt in films, which were translucent and flexible. Physicochemical characterization of LTZ via thermal technique revealed information on solid-state properties of LTZ as well as thiolated chitosan in films. While thiolated chitosan was in amorphous form, LTZ seemed to be present in both amorphous and crystalline forms in film. The lack of formulation-induced local inflammatory responses of LTZ-acetyl-polyamidoamine (Ac-PAMAM)-thiolated chitosan (TCS) films a new paradigm for localized chemotherapy based on breast delivery systems.
Subject(s)
Chitosan , Drug Carriers , Hydrogels , Nitriles , Sulfhydryl Compounds , Triazoles , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Breast Neoplasms/therapy , Chemistry, Pharmaceutical/methods , Chitosan/chemical synthesis , Chitosan/chemistry , Drug Carriers/chemical synthesis , Drug Carriers/chemistry , Drug Stability , Hydrogels/chemical synthesis , Hydrogels/chemistry , Hydrogels/metabolism , Letrozole , Nanoparticles/chemistry , Nanoparticles/ultrastructure , Nitriles/metabolism , Sulfhydryl Compounds/chemical synthesis , Sulfhydryl Compounds/chemistry , Tensile Strength/physiology , Triazoles/metabolismABSTRACT
The main objective of this study was to develop a local, oral mucoadhesive metronidazole benzoate (MET) delivery system that can be applied and removed by the patient for the treatment of periodontal diseases. The results of present study revealed that the retention time of MET at its absorption site could be increased by formulating it into nanoparticles using thiolated chitosan (TCS)-poly(methacrylic acid) (PMAA). The nanoparticles of MET prepared from TCS-PMAA may represent a useful approach for targeting its release at its site of absorption, sustaining its release and improving its oral availability.
Subject(s)
Chitosan , Drug Delivery Systems , Nanoparticles , Polymethacrylic Acids , Adhesiveness , Chitosan/analogs & derivatives , Chitosan/chemical synthesis , Chitosan/chemistry , Differential Thermal Analysis , Humans , Metronidazole/administration & dosage , Metronidazole/pharmacokinetics , Mouth Mucosa/metabolism , Nanoparticles/chemistry , Nanoparticles/ultrastructure , Polymethacrylic Acids/chemical synthesis , Polymethacrylic Acids/chemistryABSTRACT
The purpose of this study was to examine chitosan (CS)-carboxymethyl starch (CMS) nanoparticles as drug delivery system to the colon. The 5-aminosalicylic acid (5-ASA) was chosen as model drug molecule. CS-CMS nanoparticles were formulated by a complex coacervation process under mild conditions. The influence of process variables, including the two ionic polymers, on particle size, and nanoparticles entrapment of 5-ASA was studied. In vitro release of 5-ASA was also evaluated, and the integrity of 5-ASA in the release fraction was assessed using sodium dodecyl sulfate-polyacrylamide gel electrophoresis. The release of 5-ASA from nanoparticle was based on the ion-exchange mechanism. The CS-CMS nanoparticles developed based on the modulation of ratio show promise as a system for controlled delivery of drug to the colon.
Subject(s)
Chitosan/analogs & derivatives , Colon , Drug Delivery Systems , Nanoparticles , Starch/analogs & derivatives , Aminosalicylic Acid/administration & dosage , Aminosalicylic Acid/pharmacokinetics , Chitosan/chemical synthesis , Chitosan/chemistry , Colon/metabolism , Nanoparticles/chemistry , Nanoparticles/ultrastructure , Pharmaceutic Aids/chemical synthesis , Pharmaceutic Aids/chemistry , Starch/chemical synthesis , Starch/chemistryABSTRACT
The main aim of this research was to develop and evaluate a multiparticulate system of Ac-poly(amidoamine)(PAMAM)(G4)-chitosan (CS) hydrogels exploiting pH-sensitive and specific biodegradability properties for colon-targeted delivery of 5-aminosalicylic acid (5-ASA). All formulations were evaluated for particle size, encapsulation efficiency, swellability, and in vitro drug release. The size of the hydrogel was found to nanorange. The integrity of 5-ASA in the release fraction was assessed using sodium dodecyl sulfate-polyacrylamide gel electrophoresis. The CS-Ac-PAMAM hydrogel was developed based on the modulation of ratio show promise as a system for controlled delivery of drug.
