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Silvia Staniscuaski Guterres - One of the best experts on this subject based on the ideXlab platform.
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Polymeric Nanocapsules for Topical Delivery
Percutaneous Penetration Enhancers Chemical Methods in Penetration Enhancement, 2020Co-Authors: Adriana Raffin Pohlmann, Cassia Britto Detoni, Karine Coradini, Karina Paese, Ruy Carlos Ruver Beck, Silvia Staniscuaski GuterresAbstract:Polymeric Nanocapsules represent an interesting carrier system for cutaneous applications. The possibilities of modulating skin penetration/permeation by altering the design of the formulation and the range of applicability are the main subjects under study. With this in mind, this chapter will address methods of nanocapsule preparation and the influence of the polymeric wall, the surface functionalization, and the vehicle on the skin penetration/permeation profile of active substances loaded in polymeric Nanocapsules. Additionally, therapeutic and cosmetic applications of Nanocapsules will also be discussed.
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Preparation and characterization of spray-dried polymeric Nanocapsules
Drug Development and Industrial Pharmacy, 2020Co-Authors: C.r. Muller, Pedro Ros Petrovick, Cecilia Bohns Michalowski, Valquiria Linck Bassani, Adriana Raffin Pohlmann, Silvia Staniscuaski GuterresAbstract:Recently, much interest has been generated by colloidal drug delivery systems such as Nanocapsules because of the possibilities for controlled release, increased drug efficacy, and reduced toxicity after parenteral administration. Nanocapsules of poly-e-caprolactone and Eudragit S90® were prepared. However, these systems present physicochemical instability. To dry these nanocapsule suspensions with the view of obtaining a solid form, the spray-drying process was used. Spray-dried powders of Nanocapsules of poly-e-caprolactone and Eudragit S90® were prepared by atomization in a Buchi 190 Mini-spray dryer using colloidal silicon dioxide as a technological carrier. The morphological analysis of the surface at the powders showed that Nanocapsules remain intact, and no change in particle size was detected after the spray-drying process. These results suggest that this method can be an interesting alternative to dry nanocapsule suspensions.
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Polymeric Nanocapsules: Concepts and Applications
Nanocosmetics and Nanomedicines, 2020Co-Authors: Fernanda S. Poletto, Silvia Staniscuaski Guterres, Ruy Carlos Ruver Beck, Adriana Raffin PohlmannAbstract:This chapter presents an overview of polymeric Nanocapsules for dermatological and cosmetic applications, including their preparation methods, physicochemical characterization and models of supramolecular structures. Polymeric Nanocapsules are advantageous because of their ability to control the release rate and the penetration/permeation of drugs and active ingredients in the skin. These properties can be modulated through manipulating the qualitative and quantitative compositions of formulations. The chemical nature of raw materials can define the supramolecular structures of the nanocapsule core and surface. In addition, polymeric Nanocapsules protect the encapsulated drug or active ingredient from degradation by acting as reservoirs. Aqueous suspensions of polymeric Nanocapsules are directly applied on the skin or used as intermediate products for semisolid formulations, such as hydrogels and emulgels. The rheological characteristics of semisolid formulations can be modified by the presence of Nanocapsules. Polymeric Nanocapsules are valuable devices for skin applications and represent a promising research field in terms of providing products to be explored by industry.
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Labeling the oily core of Nanocapsules and lipid-core Nanocapsules with a triglyceride conjugated to a fluorescent dye as a strategy to particle tracking in biological studies
Nanoscale Research Letters, 2014Co-Authors: Luana Almeida Fiel, Juliane Freitas Bica, Fabrício Figueiró, Renata Vidor Contri, Silvia Staniscuaski Guterres, Ana Maria Oliveira Battastini, Adriana Raffin PohlmannAbstract:The synthesis of novel fluorescent materials represents a very important step to obtain labeled nanoformulations in order to evaluate their biological behavior. The strategy of conjugating a fluorescent dye with triacylglycerol allows that either particles differing regarding supramolecular structure, i.e., nanoemulsions, Nanocapsules, lipid-core Nanocapsules, or surface charge, i.e., cationic Nanocapsules and anionic Nanocapsules, can be tracked using the same labeled material. In this way, a rhodamine B-conjugated triglyceride was obtained to prepare fluorescent polymeric Nanocapsules. Different formulations were obtained, Nanocapsules (NC) or lipid-core Nanocapsules (LNC), using the labeled oil and Eudragit RS100, Eudragit S100, or poly(caprolactone) (PCL), respectively. The rhodamine B was coupled with the ricinolein by activating the carboxylic function using a carbodiimide derivative. Thin layer chromatography, proton nuclear magnetic resonance (1H-NMR), Fourier transform infrared spectroscopy (FTIR), UV-vis, and fluorescence spectroscopy were used to identify the new product. Fluorescent nanocapsule aqueous suspensions were prepared by the solvent displacement method. Their pH values were 4.6 (NC-RS100), 3.5 (NC-S100), and 5.0 (LNC-PCL). The volume-weighted mean diameter (D4.3) and polydispersity values were 150 nm and 1.05 (NC-RS100), 350 nm and 2.28 (NC-S100), and 270 nm and 1.67 (LNC-PCL). The mean diameters determined by photon correlation spectroscopy (PCS) (z-average) were around 200 nm. The zeta potential values were +5.85 mV (NC-RS100), -21.12 mV (NC-S100), and -19.25 mV (LNC-PCL). The wavelengths of maximum fluorescence emission were 567 nm (NC-RS100 and LNC-PCL) and 574 nm (NC-S100). Fluorescence microscopy was used to evaluate the cell uptake (human macrophage cell line) of the fluorescent Nanocapsules in order to show the applicability of the approach. When the cells were treated with the fluorescent Nanocapsules, red emission was detected around the cell nucleus. We demonstrated that the rhodamine B-conjugated triglyceride is a promising new material to obtain versatile dye-labeled nanocarriers presenting different chemical nature in their surfaces.
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Vitamin K1-loaded lipid-core Nanocapsules: Physicochemical characterization and in vitro skin permeation
Skin Research and Technology, 2013Co-Authors: Ana Luiza M. Da Silva, Denise Soledade Jornada, Renata Vidor Contri, Adriana Raffin Pohlmann, Silvia Staniscuaski GuterresAbstract:Background: The incorporation of substances in nanocarriers can modulate and/or manage their delivery profiles (immediate or sustained) and permeation through skin. Consequently, drug nanencapsulation intended for topical treatment can reduce the systemic absorption of the substance. Objective: To obtain and characterize vitamin K1-loaded lipid core Nanocapsules as well as to determine whether the nanoencapsulation influences the skin permeation of this vitamin. Methods: The skin permeation study was performed by means of Franz-type diffusion cells followed by the tape stripping and retention techniques. The vitamin K1-loaded lipid core Nanocapsules were obtained by the preformed polymer precipitation method and the particles were characterized. Results: The Nanocapsules presented average diameter of 211 ± 2 nm, pH of 5.7 ± 0.3, zeta potential of -14.9 ± 0.6 mV and drug content of 10.2 mg/mL (102.1%). The physical stability of the nanocapsule suspension was verified using multiple light backscattering analysis. The amount of vitamin K1 in the dermis after 8 h of drug permeation was higher when the Nanocapsules were applied compared to the control. Moreover, retention in the outermost skin layer and a decrease in the skin permeation to the receptor compartment due to the nanoencapsulation were observed. Conclusion: Thus, nanoencapsulation can lead to the selective permeation of vitamin K1 through the skin. © 2012 John Wiley & Sons A/S.
Adriana Raffin Pohlmann - One of the best experts on this subject based on the ideXlab platform.
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Polymeric Nanocapsules for Topical Delivery
Percutaneous Penetration Enhancers Chemical Methods in Penetration Enhancement, 2020Co-Authors: Adriana Raffin Pohlmann, Cassia Britto Detoni, Karine Coradini, Karina Paese, Ruy Carlos Ruver Beck, Silvia Staniscuaski GuterresAbstract:Polymeric Nanocapsules represent an interesting carrier system for cutaneous applications. The possibilities of modulating skin penetration/permeation by altering the design of the formulation and the range of applicability are the main subjects under study. With this in mind, this chapter will address methods of nanocapsule preparation and the influence of the polymeric wall, the surface functionalization, and the vehicle on the skin penetration/permeation profile of active substances loaded in polymeric Nanocapsules. Additionally, therapeutic and cosmetic applications of Nanocapsules will also be discussed.
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Preparation and characterization of spray-dried polymeric Nanocapsules
Drug Development and Industrial Pharmacy, 2020Co-Authors: C.r. Muller, Pedro Ros Petrovick, Cecilia Bohns Michalowski, Valquiria Linck Bassani, Adriana Raffin Pohlmann, Silvia Staniscuaski GuterresAbstract:Recently, much interest has been generated by colloidal drug delivery systems such as Nanocapsules because of the possibilities for controlled release, increased drug efficacy, and reduced toxicity after parenteral administration. Nanocapsules of poly-e-caprolactone and Eudragit S90® were prepared. However, these systems present physicochemical instability. To dry these nanocapsule suspensions with the view of obtaining a solid form, the spray-drying process was used. Spray-dried powders of Nanocapsules of poly-e-caprolactone and Eudragit S90® were prepared by atomization in a Buchi 190 Mini-spray dryer using colloidal silicon dioxide as a technological carrier. The morphological analysis of the surface at the powders showed that Nanocapsules remain intact, and no change in particle size was detected after the spray-drying process. These results suggest that this method can be an interesting alternative to dry nanocapsule suspensions.
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Polymeric Nanocapsules: Concepts and Applications
Nanocosmetics and Nanomedicines, 2020Co-Authors: Fernanda S. Poletto, Silvia Staniscuaski Guterres, Ruy Carlos Ruver Beck, Adriana Raffin PohlmannAbstract:This chapter presents an overview of polymeric Nanocapsules for dermatological and cosmetic applications, including their preparation methods, physicochemical characterization and models of supramolecular structures. Polymeric Nanocapsules are advantageous because of their ability to control the release rate and the penetration/permeation of drugs and active ingredients in the skin. These properties can be modulated through manipulating the qualitative and quantitative compositions of formulations. The chemical nature of raw materials can define the supramolecular structures of the nanocapsule core and surface. In addition, polymeric Nanocapsules protect the encapsulated drug or active ingredient from degradation by acting as reservoirs. Aqueous suspensions of polymeric Nanocapsules are directly applied on the skin or used as intermediate products for semisolid formulations, such as hydrogels and emulgels. The rheological characteristics of semisolid formulations can be modified by the presence of Nanocapsules. Polymeric Nanocapsules are valuable devices for skin applications and represent a promising research field in terms of providing products to be explored by industry.
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Labeling the oily core of Nanocapsules and lipid-core Nanocapsules with a triglyceride conjugated to a fluorescent dye as a strategy to particle tracking in biological studies
Nanoscale Research Letters, 2014Co-Authors: Luana Almeida Fiel, Juliane Freitas Bica, Fabrício Figueiró, Renata Vidor Contri, Silvia Staniscuaski Guterres, Ana Maria Oliveira Battastini, Adriana Raffin PohlmannAbstract:The synthesis of novel fluorescent materials represents a very important step to obtain labeled nanoformulations in order to evaluate their biological behavior. The strategy of conjugating a fluorescent dye with triacylglycerol allows that either particles differing regarding supramolecular structure, i.e., nanoemulsions, Nanocapsules, lipid-core Nanocapsules, or surface charge, i.e., cationic Nanocapsules and anionic Nanocapsules, can be tracked using the same labeled material. In this way, a rhodamine B-conjugated triglyceride was obtained to prepare fluorescent polymeric Nanocapsules. Different formulations were obtained, Nanocapsules (NC) or lipid-core Nanocapsules (LNC), using the labeled oil and Eudragit RS100, Eudragit S100, or poly(caprolactone) (PCL), respectively. The rhodamine B was coupled with the ricinolein by activating the carboxylic function using a carbodiimide derivative. Thin layer chromatography, proton nuclear magnetic resonance (1H-NMR), Fourier transform infrared spectroscopy (FTIR), UV-vis, and fluorescence spectroscopy were used to identify the new product. Fluorescent nanocapsule aqueous suspensions were prepared by the solvent displacement method. Their pH values were 4.6 (NC-RS100), 3.5 (NC-S100), and 5.0 (LNC-PCL). The volume-weighted mean diameter (D4.3) and polydispersity values were 150 nm and 1.05 (NC-RS100), 350 nm and 2.28 (NC-S100), and 270 nm and 1.67 (LNC-PCL). The mean diameters determined by photon correlation spectroscopy (PCS) (z-average) were around 200 nm. The zeta potential values were +5.85 mV (NC-RS100), -21.12 mV (NC-S100), and -19.25 mV (LNC-PCL). The wavelengths of maximum fluorescence emission were 567 nm (NC-RS100 and LNC-PCL) and 574 nm (NC-S100). Fluorescence microscopy was used to evaluate the cell uptake (human macrophage cell line) of the fluorescent Nanocapsules in order to show the applicability of the approach. When the cells were treated with the fluorescent Nanocapsules, red emission was detected around the cell nucleus. We demonstrated that the rhodamine B-conjugated triglyceride is a promising new material to obtain versatile dye-labeled nanocarriers presenting different chemical nature in their surfaces.
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Vitamin K1-loaded lipid-core Nanocapsules: Physicochemical characterization and in vitro skin permeation
Skin Research and Technology, 2013Co-Authors: Ana Luiza M. Da Silva, Denise Soledade Jornada, Renata Vidor Contri, Adriana Raffin Pohlmann, Silvia Staniscuaski GuterresAbstract:Background: The incorporation of substances in nanocarriers can modulate and/or manage their delivery profiles (immediate or sustained) and permeation through skin. Consequently, drug nanencapsulation intended for topical treatment can reduce the systemic absorption of the substance. Objective: To obtain and characterize vitamin K1-loaded lipid core Nanocapsules as well as to determine whether the nanoencapsulation influences the skin permeation of this vitamin. Methods: The skin permeation study was performed by means of Franz-type diffusion cells followed by the tape stripping and retention techniques. The vitamin K1-loaded lipid core Nanocapsules were obtained by the preformed polymer precipitation method and the particles were characterized. Results: The Nanocapsules presented average diameter of 211 ± 2 nm, pH of 5.7 ± 0.3, zeta potential of -14.9 ± 0.6 mV and drug content of 10.2 mg/mL (102.1%). The physical stability of the nanocapsule suspension was verified using multiple light backscattering analysis. The amount of vitamin K1 in the dermis after 8 h of drug permeation was higher when the Nanocapsules were applied compared to the control. Moreover, retention in the outermost skin layer and a decrease in the skin permeation to the receptor compartment due to the nanoencapsulation were observed. Conclusion: Thus, nanoencapsulation can lead to the selective permeation of vitamin K1 through the skin. © 2012 John Wiley & Sons A/S.
Amr S. Fawzy - One of the best experts on this subject based on the ideXlab platform.
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Chlorhexidine Nanocapsule Drug Delivery Approach to the Resin-Dentin Interface
Journal of Dental Research, 2016Co-Authors: B. M. Priyadarshini, S. Tamil Selvan, T B Lu, Amr S. FawzyAbstract:In this study, we are introducing a new drug-delivery approach to demineralized dentin substrates through microsized dentinal tubules in the form of drug-loaded Nanocapsules. Chlorhexidine (CHX) is widely used in adhesive dentistry due to its nonspecific matrix metalloproteinase inhibitory effect and antibacterial activities. Poly(e-caprolactone) Nanocapsules (nano-PCL) loaded with CHX were fabricated by interfacial polymer deposition at PCL/CHX ratios of 125:10, 125:25, and 125:50. Unloaded Nanocapsules (blank) were fabricated as control. The fabricated Nanocapsules were characterized in vitro in terms of particle size, surface charges, particle recovery, encapsulation efficiency, and drug loading. Nanocapsule morphology, drug inclusion, structural properties, and crystallinity were investigated by scanning and transmission electron microscopes (SEM/TEM), energy-dispersive x-ray analysis, Fourier transform infrared spectroscopy, and x-ray diffraction. Initial screening of the antibacterial activities and...
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Chlorhexidine Nanocapsule Drug Delivery Approach to the Resin-Dentin Interface
Journal of Dental Research, 2016Co-Authors: B. M. Priyadarshini, S. Tamil Selvan, Jennifer Neo, T B Lu, H. Xie, Amr S. FawzyAbstract:In this study, we are introducing a new drug-delivery approach to demineralized dentin substrates through microsized dentinal tubules in the form of drug-loaded Nanocapsules. Chlorhexidine (CHX) is widely used in adhesive dentistry due to its nonspecific matrix metalloproteinase inhibitory effect and antibacterial activities. Poly(ε-caprolactone) Nanocapsules (nano-PCL) loaded with CHX were fabricated by interfacial polymer deposition at PCL/CHX ratios of 125:10, 125:25, and 125:50. Unloaded Nanocapsules (blank) were fabricated as control. The fabricated Nanocapsules were characterized in vitro in terms of particle size, surface charges, particle recovery, encapsulation efficiency, and drug loading. Nanocapsule morphology, drug inclusion, structural properties, and crystallinity were investigated by scanning and transmission electron microscopes (SEM/TEM), energy-dispersive x-ray analysis, Fourier transform infrared spectroscopy, and x-ray diffraction. Initial screening of the antibacterial activities and the cytotoxicity of the Nanocapsules were also conducted. Nanocapsules, as carried on ethanol/water solution, were delivered to demineralized dentin specimens connected to an ex vivo model setup simulating the pulpal pressure to study their infiltration, penetration depth, and retention inside the dentinal tubules by SEM/TEM. Nanocapsules were Ag labeled and delivered to demineralized dentin, followed by the application of a 2-step etch-and-rinse dentin adhesive. CHX-release profiles were characterized in vitro and ex vivo up to 25 d. Spherical Nanocapsules were fabricated with a CHX core coated with a thin PCL shell. The blank Nanocapsules exhibited the largest z-average diameter with negatively charged ζ-potential. With CHX incorporation, the nanocapsule size was decreased with a positive shift in ζ-potential. Nano-PCL/CHX at 125:50 showed the highest drug loading, antibacterial effect, and CHX release both in vitro and ex vivo. SEM and TEM revealed the deep penetration and retention of the CHX-loaded Nanocapsules inside dentinal tubules and their ability to be gradually degraded to release CHX in vitro and ex vivo. Ag-labeled Nanocapsules revealed the close association and even distribution of Nanocapsules throughout the resin tag structure. This study demonstrated the potential of introducing this novel drug-delivery approach to demineralized dentin substrates and the resin-dentin interface with nanosized CHX-loaded Nanocapsules through the microsized dentinal tubules.
Darrell J. Irvine - One of the best experts on this subject based on the ideXlab platform.
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Design of lipid nanocapsule delivery vehicles for multivalent display of recombinant env trimers in HIV vaccination
Bioconjugate Chemistry, 2014Co-Authors: Sharmila Pejawar-gaddy, James M. Kovacs, Dan H Barouch, Bing Chen, Darrell J. IrvineAbstract:Immunization strategies that elicit antibodies capable of neutralizing diverse virus strains will likely be an important part of a successful vaccine against HIV. However, strategies to promote robust humoral responses against the native intact HIV envelope trimer structure are lacking. We recently developed chemically cross-linked lipid Nanocapsules as carriers of molecular adjuvants and encapsulated or surface-displayed antigens, which promoted follicular helper T-cell responses and elicited high-avidity, durable antibody responses to a candidate malaria antigen. To apply this system to the delivery of HIV antigens, Env gp140 trimers with terminal his-tags (gp140T-his) were anchored to the surface of lipid Nanocapsules via Ni-NTA-functionalized lipids. Initial experiments revealed that the large (409 kDa), heavily glycosylated trimers were capable of extracting fluid phase lipids from the membranes of Nanocapsules. Thus, liquid-ordered and/or gel-phase lipid compositions were required to stably anchor trimers to the particle membranes. Trimer-loaded Nanocapsules combined with the clinically relevant adjuvant monophosphoryl lipid A primed high-titer antibody responses in mice at antigen doses ranging from 5 μg to as low as 100 ng, whereas titers dropped more than 50-fold over the same dose range when soluble trimer was mixed with a strong oil-in-water adjuvant comparator. Nanocapsule immunization also broadened the number of distinct epitopes on the HIV trimer recognized by the antibody response. These results suggest that Nanocapsules displaying HIV trimers in an oriented, multivalent presentation can promote key aspects of the humoral response against Env immunogens.
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releasable layer by layer assembly of stabilized lipid Nanocapsules on microneedles for enhanced transcutaneous vaccine delivery
ACS Nano, 2012Co-Authors: Peter C Demuth, James J Moon, Paula T Hammond, Darrell J. IrvineAbstract:Here we introduce a new approach for transcutaneous drug delivery, using microneedles coated with stabilized lipid Nanocapsules, for delivery of a model vaccine formulation. Poly(lactide-co-glycolide) microneedle arrays were coated with multilayer films via layer-by-layer assembly of a biodegradable cationic poly(β-amino ester) (PBAE) and negatively charged interbilayer-cross-linked multilamellar lipid vesicles (ICMVs). To test the potential of these nanocapsule-coated microneedles for vaccine delivery, we loaded ICMVs with a protein antigen and the molecular adjuvant monophosphoryl lipid A. Following application of microneedle arrays to the skin of mice for 5 min, (PBAE/ICMV) films were rapidly transferred from microneedle surfaces into the cutaneous tissue and remained in the skin following removal of the microneedle arrays. Multilayer films implanted in the skin dispersed ICMV cargos in the treated tissue over the course of 24 h in vivo, allowing for uptake of the lipid Nanocapsules by antigen presenti...
Jean-françois Gestin - One of the best experts on this subject based on the ideXlab platform.
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Radiolabeling and targeting of lipidic Nanocapsules for applications in radioimmunotherapy.
The quarterly journal of nuclear medicine and molecular imaging, 2007Co-Authors: Emmanuelle Jestin, François Hindré, Marie Mougin-degraef, Patricia Remaud-le Saëc, Alain Faivre-chauvet, Jacques Barbet, Jean-pierre Benoit, Jean-françois Chatal, Jean-françois GestinAbstract:AIM: Radioimmunotherapy is limited in some cases by the low radioactive doses delivered to tumor cells by antibodies or pretargeted haptens. In order to increase this dose, lipidic Nanocapsules (LNC) with a hydrophobic core are proposed as radionuclide vectors that could be targeted to cancer cells by a bispecific anti-tumor x anti-hapten antibody after incorporation of different haptens in the nanocapsule membrane. METHODS: To bind different radionuclides to the Nanocapsules, several bifunctional chelating agents (BCA) were used to form stable complexes with the radionuclides. Some of them are hydrophilic for LNC shell while others are lipophilic to radiolabel the core. Poly(ethylene glycols) (PEG) were used to increase the residence time in blood. Since PEG can modify haptens recognition by the bispecific antibody and radiolabeling efficiency, haptens, BCA or Bolton-Hunter reagent (BH) were attached to the PEG extremity to optimize accessibility. Specific constructs (DSPE-PEG-haptens, DSPE-PEG-BCA, and DSPE-PEG-BH) were synthesized to develop these new radiolabeled vector formulations. Large amounts of PEG have been introduced by a postinsertion method without important change in nanocapsule size and properties. The nanocapsule core was radiolabeled with a lipophilic [(99m)Tc]SSS complex. RESULTS: Serum stability studies showed that this (99m)Tc-labeling method was efficient for at least 20 h. Concerning the nanocapsule surface, several methods have been performed for (111)In-labeling by using DSPE-PEG-DTPA and for (125)I-labeling with DSPE-PEG-BH. CONCLUSIONS: The Nanocapsules labeling feasibility with a variety of radionuclides and their stability were demonstrated in this paper.
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Radiolabeling and targeting of lipidic Nanocapsules for applications in radioimmunotherapy.
Quarterly Journal of Nuclear Medicine and Molecular Imaging, 2007Co-Authors: Emmanuelle Jestin, François Hindré, Mougin-degraef M, Remaud-le Saëc P, Chatal Jf, Alain Faivre-chauvet, Jacques Barbet, Jean-pierre Benoit, Jean-françois GestinAbstract:Aim. Radioimmunotherapy is limited in some cases by the low radioactive doses delivered to tumor cells by antibodies or pretargeted haptens. In order to increase this dose, lipidic Nanocapsules (LNC) with a hydrophobic core are proposed as radionuclide vectors that could be targeted to cancer cells by a bispecific anti-tumor × anti-hapten antibody after incorporation of different haptens in the nanocapsule membrane. Methods. To bind different radionuclides to the Nanocapsules, several bifunctional chelating agents (BCA) were used to form stable complexes with the radionuclides. Some of them are hydrophilic for LNC shell while others are lipophilic to radiolabel the core. Poly(ethylene glycols) (PEG) were used to increase the residence time in blood. Since PEG can modify haptens recognition by the bispecific antibody and radiolabeling efficiency, haptens, BCA or Bolton-Hunter reagent (BH) were attached to the PEG extremity to optimize accessibility. Specific constructs (DSPE-PEG-haptens, DSPE-PEG-BCA, and DSPE-PEG-BH) were synthesized to develop these new radiolabeled vector formulations. Large amounts of PEG have been introduced by a postinsertion method without important change in nanocapsule size and properties. The nanocapsule core was radiolabeled with a lipophilic [ 99m Tc]SSS complex. Results. Serum stability studies showed that this 99m Tclabeling method was efficient for at least 20 h. Concerning the nanocapsule surface, several methods have been performed for 111 In-labeling by using DSPE-PEG-DTPA and for 125 I-labeling with DSPE-PEG-BH. Conclusions. The Nanocapsules labeling feasibility with a variety of radionuclides and their stability were demonstrated in this paper.
