2017
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Dalmoro, Annalisa; Cascone, Sara; Lamberti, Gaetano; Barba, Anna Angela Encapsulation of Active Molecules in Microparticles Based on Natural Polysaccharides Journal Article Natural Product Communications, 12 (6), pp. 863-866, 2017, ISSN: 1934-578X. Abstract | Links | BibTeX | Tags: Micro and Nano Vectors, microencapsulation, ultrasonic atomization @article{NPC01,
title = {Encapsulation of Active Molecules in Microparticles Based on Natural Polysaccharides},
author = {Annalisa Dalmoro and Sara Cascone and Gaetano Lamberti and Anna Angela Barba},
url = {http://www.naturalproduct.us/index.asp
https://www.gruppotpp.it/wp-content/uploads/2017/06/Dalmoro-et-al-NPC-126-863-866-2017-Abstract-1.pdf},
issn = {1934-578X},
year = {2017},
date = {2017-07-31},
journal = {Natural Product Communications},
volume = {12},
number = {6},
pages = {863-866},
abstract = {This mini-review is focused on an engineering approach to produce polysaccharides-based microparticles for nutraceutical and pharmaceutical purposes. A brief introduction about the fundamental properties of polysaccharides and their use as microsystems in food, cosmetics, and pharmaceutics, and a summary of the most important methods of preparation are described. Then, a novel method based on the ultrasonic atomization of solutions of the two most used polysaccharides, alginate and chitosan, followed by ionotropic gelation to produce enteric microsystems for oral administration and, in particular, the basic mechanisms of the encapsulation of molecules with different size and hydrophilicity, are investigated. This mini-review will show therefore the pathway to correctly design a polysaccharide microcarrier for the encapsulation of active molecules with different properties: from the choice of materials features, to the selection and the optimization of production methods with the aim to reduce costs and energy (ionotropic gelation coupled to ultrasonic atomization), to the control of the final carrier size (by purposely developed predictive models), at last to the optimization of encapsulation properties (predicting by model the drug leakage and providing different solutions to avoid it).},
keywords = {Micro and Nano Vectors, microencapsulation, ultrasonic atomization},
pubstate = {published},
tppubtype = {article}
}
This mini-review is focused on an engineering approach to produce polysaccharides-based microparticles for nutraceutical and pharmaceutical purposes. A brief introduction about the fundamental properties of polysaccharides and their use as microsystems in food, cosmetics, and pharmaceutics, and a summary of the most important methods of preparation are described. Then, a novel method based on the ultrasonic atomization of solutions of the two most used polysaccharides, alginate and chitosan, followed by ionotropic gelation to produce enteric microsystems for oral administration and, in particular, the basic mechanisms of the encapsulation of molecules with different size and hydrophilicity, are investigated. This mini-review will show therefore the pathway to correctly design a polysaccharide microcarrier for the encapsulation of active molecules with different properties: from the choice of materials features, to the selection and the optimization of production methods with the aim to reduce costs and energy (ionotropic gelation coupled to ultrasonic atomization), to the control of the final carrier size (by purposely developed predictive models), at last to the optimization of encapsulation properties (predicting by model the drug leakage and providing different solutions to avoid it). |
Barba, Anna Angela; Cascone, Sara; Caccavo, Diego; Lamberti, Gaetano; Chiarappa, Gianluca; Abrami, Michela; Grassi, Gabriele; Grassi, Mario; Tomaiuolo, Giovanna; Guido, Stefano; Brucato, Valerio; Carfì Pavia, Francesco ; Ghersi, Giulio; La Carrubba, Vincenzo ; Abbiati, Roberto Andrea; Manca, Davide Engineering approaches in siRNA delivery Journal Article International Journal of Pharmaceutics, 525 (2), pp. 343–358, 2017. Abstract | Links | BibTeX | Tags: Micro and Nano Vectors @article{Barba2017,
title = {Engineering approaches in siRNA delivery},
author = {Anna Angela Barba and Sara Cascone and Diego Caccavo and Gaetano Lamberti and Gianluca Chiarappa and Michela Abrami and Gabriele Grassi and Mario Grassi and Giovanna Tomaiuolo and Stefano Guido and Valerio Brucato and Francesco {Carf\`{i} Pavia} and Giulio Ghersi and Vincenzo {La Carrubba} and Roberto Andrea Abbiati and Davide Manca},
url = {http://www.sciencedirect.com/science/article/pii/S0378517317301138},
doi = {10.1016/j.ijpharm.2017.02.032},
year = {2017},
date = {2017-06-20},
journal = {International Journal of Pharmaceutics},
volume = {525},
number = {2},
pages = {343\textendash358},
abstract = {siRNAs are very potent drug molecules, able to silence genes involved in pathologies development. siRNAs have virtually an unlimited therapeutic potential, particularly for the treatment of inflammatory diseases. However, their use in clinical practice is limited because of their unfavorable properties to interact and not to degrade in physiological environments. In particular they are large macromolecules, negatively charged, which undergo rapid degradation by plasmatic enzymes, are subject to fast renal clearance/hepatic sequestration, and can hardly cross cellular membranes. These aspects seriously impair siRNAs as therapeutics. As in all the other fields of science, siRNAs management can be advantaged by physical-mathematical descriptions (modeling) in order to clarify the involved phenomena from the preparative step of dosage systems to the description of drug-body interactions, which allows improving the design of delivery systems/processes/therapies. This review analyzes a few mathematical modeling approaches currently adopted to describe the siRNAs delivery, the main procedures in siRNAs vectors’ production processes and siRNAs vectors’ release from hydrogels, and the modeling of pharmacokinetics of siRNAs vectors. Furthermore, the use of physical models to study the siRNAs vectors’ fate in blood stream and in the tissues is presented. The general view depicts a framework maybe not yet usable in therapeutics, but with promising possibilities for forthcoming applications.},
keywords = {Micro and Nano Vectors},
pubstate = {published},
tppubtype = {article}
}
siRNAs are very potent drug molecules, able to silence genes involved in pathologies development. siRNAs have virtually an unlimited therapeutic potential, particularly for the treatment of inflammatory diseases. However, their use in clinical practice is limited because of their unfavorable properties to interact and not to degrade in physiological environments. In particular they are large macromolecules, negatively charged, which undergo rapid degradation by plasmatic enzymes, are subject to fast renal clearance/hepatic sequestration, and can hardly cross cellular membranes. These aspects seriously impair siRNAs as therapeutics. As in all the other fields of science, siRNAs management can be advantaged by physical-mathematical descriptions (modeling) in order to clarify the involved phenomena from the preparative step of dosage systems to the description of drug-body interactions, which allows improving the design of delivery systems/processes/therapies. This review analyzes a few mathematical modeling approaches currently adopted to describe the siRNAs delivery, the main procedures in siRNAs vectors’ production processes and siRNAs vectors’ release from hydrogels, and the modeling of pharmacokinetics of siRNAs vectors. Furthermore, the use of physical models to study the siRNAs vectors’ fate in blood stream and in the tissues is presented. The general view depicts a framework maybe not yet usable in therapeutics, but with promising possibilities for forthcoming applications. |
Dalmoro, Annalisa; Sitenkov, Alexander Y; Cascone, Sara; Lamberti, Gaetano; Barba, Anna Angela; Moustafine, Rouslan I Hydrophilic drug encapsulation in shell-core microcarriers by two stage polyelectrolyte complexation method Journal Article International Journal of Pharmaceutics, 518 (1-2), pp. 50–58, 2017. Abstract | Links | BibTeX | Tags: Micro and Nano Vectors @article{Dalmoro2017,
title = {Hydrophilic drug encapsulation in shell-core microcarriers by two stage polyelectrolyte complexation method},
author = {Annalisa Dalmoro and Alexander Y. Sitenkov and Sara Cascone and Gaetano Lamberti and Anna Angela Barba and Rouslan I. Moustafine},
url = {http://www.sciencedirect.com/science/article/pii/S037851731631198X},
doi = {10.1016/j.ijpharm.2016.12.056},
year = {2017},
date = {2017-02-25},
journal = {International Journal of Pharmaceutics},
volume = {518},
number = {1-2},
pages = {50\textendash58},
abstract = {In this study a protocol exploiting the combination of the ultrasonic atomization and the complexation between polyelectrolytes was developed to efficiently encapsulate a hydrophilic chemotherapeutic agent essentially used in the treatment of colon cancer, 5-fluorouracil, in enteric shell-core alginate-based microcarriers. The atomization assisted by ultrasound allowed to obtain small droplets by supplying low energy and avoiding drug degradation. In particular microcarriers were produced in a home-made apparatus where both the core (composed of alginate, drug, and Pluronic F127) and shell (composed of only alginate) feed were separately sent to the coaxial ultrasonic atomizer where they were nebulized and placed in contact with the complexation bulk. With the aim to obtain microstructured particles of alginate encapsulating 5-fluorouracil, different formulations of the first complexation bulk were tested; at last an emulsion made of a calcium chloride aqueous solution and dichloromethane allowed to reach an encapsulation efficiency of about 50%. This result can be considered very interesting considering that in literature similar techniques gave 5-fluorouracil encapsulation efficiencies of about 10%.
Since a single complexation stage was not able to assure microcarriers gastroresistance, the formulation of a second complexation bulk was evaluated. The solution of cationic and pH-insoluble Eudragit® RS 100 in dichloromethane was chosen as bulk of second-stage complexation obtaining good enteric properties of shell-core microcarriers, i.e. a 5-FU cumulative release at pH 1 (simulating gastric pH) lower than 35%. The formation of interpolyelectrolyte complex (IPEC) between countercharged polymers and the chemical stability of 5-FU in microcarriers were confirmed by FTIR analysis, the presence of an amorphous dispersion of 5-FU in prepared microparticles was also confirmed by DSC. Finally, shell-core enteric coated microcarriers encapsulating 5-fluorouracil were used to prepare tablets, which can be potentially used as oral administration dosage systems for their 5-fluorouracil slower release.},
keywords = {Micro and Nano Vectors},
pubstate = {published},
tppubtype = {article}
}
In this study a protocol exploiting the combination of the ultrasonic atomization and the complexation between polyelectrolytes was developed to efficiently encapsulate a hydrophilic chemotherapeutic agent essentially used in the treatment of colon cancer, 5-fluorouracil, in enteric shell-core alginate-based microcarriers. The atomization assisted by ultrasound allowed to obtain small droplets by supplying low energy and avoiding drug degradation. In particular microcarriers were produced in a home-made apparatus where both the core (composed of alginate, drug, and Pluronic F127) and shell (composed of only alginate) feed were separately sent to the coaxial ultrasonic atomizer where they were nebulized and placed in contact with the complexation bulk. With the aim to obtain microstructured particles of alginate encapsulating 5-fluorouracil, different formulations of the first complexation bulk were tested; at last an emulsion made of a calcium chloride aqueous solution and dichloromethane allowed to reach an encapsulation efficiency of about 50%. This result can be considered very interesting considering that in literature similar techniques gave 5-fluorouracil encapsulation efficiencies of about 10%.
Since a single complexation stage was not able to assure microcarriers gastroresistance, the formulation of a second complexation bulk was evaluated. The solution of cationic and pH-insoluble Eudragit® RS 100 in dichloromethane was chosen as bulk of second-stage complexation obtaining good enteric properties of shell-core microcarriers, i.e. a 5-FU cumulative release at pH 1 (simulating gastric pH) lower than 35%. The formation of interpolyelectrolyte complex (IPEC) between countercharged polymers and the chemical stability of 5-FU in microcarriers were confirmed by FTIR analysis, the presence of an amorphous dispersion of 5-FU in prepared microparticles was also confirmed by DSC. Finally, shell-core enteric coated microcarriers encapsulating 5-fluorouracil were used to prepare tablets, which can be potentially used as oral administration dosage systems for their 5-fluorouracil slower release. |
2012
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Cascone, Sara; Lamberti, Gaetano; Titomanlio, Giuseppe; Barba, Anna Angela; D'Amore, Matteo Microencapsulation effectiveness of small active molecules in biopolymer by ultrasonic atomization technique Journal Article Drug Development and Industrial Pharmacy, 38 (12), pp. 1486–1493, 2012, ISSN: 0363-9045. Links | BibTeX | Tags: Micro and Nano Vectors @article{Cascone2012,
title = {Microencapsulation effectiveness of small active molecules in biopolymer by ultrasonic atomization technique},
author = { Sara Cascone and Gaetano Lamberti and Giuseppe Titomanlio and Anna Angela Barba and Matteo D'Amore},
url = {http://www.tandfonline.com/doi/full/10.3109/03639045.2011.653814},
doi = {10.3109/03639045.2011.653814},
issn = {0363-9045},
year = {2012},
date = {2012-12-01},
journal = {Drug Development and Industrial Pharmacy},
volume = {38},
number = {12},
pages = {1486--1493},
keywords = {Micro and Nano Vectors},
pubstate = {published},
tppubtype = {article}
}
|
2009
|
Barba, Anna Angela; D'Amore, Matteo; Cascone, Sara; Lamberti, Gaetano; Titomanlio, Giuseppe Intensification of biopolymeric microparticles production by ultrasonic assisted atomization Journal Article Chemical Engineering and Processing: Process Intensification, 48 (10), pp. 1477–1483, 2009, ISSN: 02552701. Abstract | Links | BibTeX | Tags: Biopolymer, Intensified ultrasonic atomization, Micro and Nano Vectors, Microparticles @article{Barba2009g,
title = {Intensification of biopolymeric microparticles production by ultrasonic assisted atomization},
author = { Anna Angela Barba and Matteo D'Amore and Sara Cascone and Gaetano Lamberti and Giuseppe Titomanlio},
url = {http://www.sciencedirect.com/science/article/pii/S0255270109001524},
doi = {10.1016/j.cep.2009.08.004},
issn = {02552701},
year = {2009},
date = {2009-01-01},
journal = {Chemical Engineering and Processing: Process Intensification},
volume = {48},
number = {10},
pages = {1477--1483},
abstract = {In this work ultrasonic atomization process is applied to produce biopolymer microparticles with potential applications in pharmaceutical and nutraceutical fields. Natural polymer (alginate)/water solution is atomized by ultrasonic assisted process and the droplets spray is reticulated using a solution of copper sulfate, where the Cu2+ ions cause the formation of a network structure (hard porous gel). Several operating parameters (solution concentration, flow rate, atomization power) are changed to study their effects on the produced microparticles. Literature correlations able to predict the features of the droplets as functions of process parameters are optimized using a statistical approach. Furthermore, the energy requirement for the drops production is compared with the energy required by traditional techniques to evaluate the intensification effect of the ultrasonic on the atomization process.},
keywords = {Biopolymer, Intensified ultrasonic atomization, Micro and Nano Vectors, Microparticles},
pubstate = {published},
tppubtype = {article}
}
In this work ultrasonic atomization process is applied to produce biopolymer microparticles with potential applications in pharmaceutical and nutraceutical fields. Natural polymer (alginate)/water solution is atomized by ultrasonic assisted process and the droplets spray is reticulated using a solution of copper sulfate, where the Cu2+ ions cause the formation of a network structure (hard porous gel). Several operating parameters (solution concentration, flow rate, atomization power) are changed to study their effects on the produced microparticles. Literature correlations able to predict the features of the droplets as functions of process parameters are optimized using a statistical approach. Furthermore, the energy requirement for the drops production is compared with the energy required by traditional techniques to evaluate the intensification effect of the ultrasonic on the atomization process. |