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Barbara Vigani, Caterina Valentino, Giuseppina Sandri, Carla Marcella Caramella, Franca Ferrari, Silvia Rossi Department of Drug Sciences, University of Pavia, Pavia, ItalyCorrespondence: Silvia Rossi, Department of Drug Sciences, University of Pavia, Viale Taramelli 12, Pavia, 27100, Italy, Tel +39 0382987357, Fax +39 0382422975, Email silvia.rossi@unipv.itPurpose: Aim of the work was to develop a potential neural scaffold, endowed with neuroprotective and neuroregenerative potential, to be applied at the site of nervous tissue injuries: nanofibers, consisting of gellan gum (GG), spermidine (SP) and gelatin (GL), were prepared via electrospinning. SP was selected for its neuroprotective activity and cationic nature that makes it an ideal GG cross-linking agent. GL was added to improve the scaffold bioactivity.Methods: Mixtures, containing 1.5% w/w GG and increasing SP concentrations (0– 0.125% w/w), were prepared to investigate GG/SP interaction and, thus, to find the best mixture to be electrospun. Mixture rheological and mechanical properties were assessed. The addition of 0.1% w/w GL was also investigated. The most promising GG/SP/GL mixtures were added with poly(ethylene oxide) (PEO) and poloxamer (P407) and, then, electrospun. The resulting fibers were characterized in terms of size and mechanical properties and fiber morphology was observed after soaking in water for 24 hours. Nanofiber biocompatibility was assessed on Schwann cells.Results: More and more structured GG/SP mixtures were obtained by increasing SP concentration, proving its cross-linking potential. After blending with PEO and P407, the mixture consisting of 1.5% w/w GG, 0.05% w/w SP and 0.1% w/w GL was electrospun. The resulting nanofibers appeared homogenous and characterized by a plastic behavior, suggesting a good mechanical resistance when applied at the injury site. Nanofibers were insoluble in aqueous media and able to form a thin gel layer after hydration. GG/SP/GL nanofibers sh

Recently nanoparticle-based vaginal drug delivery formulations have been acquiring great attention for the administration of peptide based-vaccines or microbicides to prevent or treat sexually transmitted diseases. In this work, a straightforward and efficient strategy for the vaginal application and release of peptideloaded mucoadhesive nanoparticles was developed. This essentially consists of chitosan nanoparticles encapsulated in suitable hydrophilic freeze-dried cylinders. Chitosan nanoparticles are responsible for carrying the peptide drug and allowing adhesion to the vaginal mucosal epithelium. Hydrophilic freezedried cylinders facilitate the application and quick release of the nanoparticles to the vaginal zone. Upon contact with the aqueous vaginal medium, the excipients constituting these sponge-like systems are quickly dissolved enabling the release of their content. In vitro release studies showed the ability of the sponge-like systems and chitosan nanoparticles to deliver the mucoadhesive nanoparticles and peptide respectively. CLSM micrographs proved the nanoparticles ability promoting the peptide penetration inside the vaginal mucosa., Instituto de Salud Carlos III, Xunta de Galicia, Depto. de Química en Ciencias Farmacéuticas, Fac. de Farmacia, TRUE, pub

Recently nanoparticle-based vaginal drug delivery formulations have been acquiring great attention for the administration of peptide based-vaccines or microbicides to prevent or treat sexually transmitted diseases. In this work, a straightforward and efficient strategy for the vaginal application and release of peptideloaded mucoadhesive nanoparticles was developed. This essentially consists of chitosan nanoparticles encapsulated in suitable hydrophilic freeze-dried cylinders. Chitosan nanoparticles are responsible for carrying the peptide drug and allowing adhesion to the vaginal mucosal epithelium. Hydrophilic freezedried cylinders facilitate the application and quick release of the nanoparticles to the vaginal zone. Upon contact with the aqueous vaginal medium, the excipients constituting these sponge-like systems are quickly dissolved enabling the release of their content. In vitro release studies showed the ability of the sponge-like systems and chitosan nanoparticles to deliver the mucoadhesive nanoparticles and peptide respectively. CLSM micrographs proved the nanoparticles ability promoting the peptide penetration inside the vaginal mucosa., Instituto de Salud Carlos III, Xunta de Galicia, Depto. de Química en Ciencias Farmacéuticas, Fac. de Farmacia, TRUE, pub

The present review is aimed at elucidating relatively new aspects of mucoadhesion/mucus interaction and related phenomena that emerged from a Mucoadhesion workshop held in Munster on 2-3 September 2015 as a satellite event of the ICCC 13th-EUCHIS 12th. After a brief outline of the new issues, the focus is on mucus description, purification, and mucus/mucin characterization, all steps that are pivotal to the understanding of mucus related phenomena and the choice of the correct mucosal model for in vitro and ex vivo experiments, alternative bio/mucomimetic materials are also presented. Then a selection of preparative techniques and testing methods are described (at molecular as well as micro and macroscale) that may support the pharmaceutical development of mucus interactive systems and assist formulators in the scale-up and industrialization steps. Recent applications of mucoadhesive systems (including medical devices) intended for different routes of administration (oral, gastrointestinal, vaginal, nasal, ocular, and intravesical) and for the treatment of difficult to treat pathologies or the alleviation of symptoms are described.

The present review is aimed at elucidating relatively new aspects of mucoadhesion/mucus interaction and related phenomena that emerged from a Mucoadhesion workshop held in Munster on 2–3 September 2015 as a satellite event of the ICCC 13th—EUCHIS 12th. After a brief outline of the new issues, the focus is on mucus description, purification, and mucus/mucin characterization, all steps that are pivotal to the understanding of mucus related phenomena and the choice of the correct mucosal model for in vitro and ex vivo experiments, alternative bio/mucomimetic materials are also presented. Then a selection of preparative techniques and testing methods are described (at molecular as well as micro and macroscale) that may support the pharmaceutical development of mucus interactive systems and assist formulators in the scale-up and industrialization steps. Recent applications of mucoadhesive systems (including medical devices) intended for different routes of administration (oral, gastrointestinal, vaginal, nasal, ocular, and intravesical) and for the treatment of difficult to treat pathologies or the alleviation of symptoms are described.

Luiza A Frank,1 Giuseppina Sandri,2 Francesca D´Autilia,2 Renata V Contri,1 Maria Cristina Bonferoni,2 Carla Caramella,2 Alejandro G Frank,3 Adriana R Pohlmann,1 Silvia S Guterres11Pharmaceutical Science Graduate Program, Federal University of Rio Grande do Sul, Porto Alegre, RS, Brazil; 2Department of Drug Sciences, University of Pavia, Pavia, PV, Italy; 3Department of Industrial Engineering, Federal University of Rio Grande do Sul, Porto Alegre, RS, BrazilAbstract: The vaginal route of administration is an alternative for several treatments for either local or systemic pharmacological effects. However, the permanence of a drug in this route represents a challenge for formulation development that can be overcome by using nanoencapsulation and chitosan gel. Thus, this work aimed to evaluate the performance of chitosan hydrogels containing cationic and anionic acrylic-based nanocapsules (Eudragit® RS 100 and Eudragit® S 100, respectively) with Nile red as a model of lipophilic substance in the vaginal route of administration, as measured by increases in the residence time and the penetration of these formulations. Several formulations were prepared with increasing chitosan concentrations, and were analyzed in terms of pH and rheological behavior so that the most suitable formulation could be selected. The enhancement of the adhesion (tensile stress test and washability profile) and penetration (confocal laser scanning microscopy and extraction followed by quantification) properties of the formulations, when applied to porcine vaginal mucosa, were evaluated. The nanocapsule suspensions produced presented adequate properties: size of approximately 200 nm (polydispersity index of ≤0.2); zeta potential around +10 mV for the cationic formulation and -10 mV for the anionic formulation; and pH values of 6.1±0.1 (Eudragit RS 100), 5.3±0.2&am

Luiza A Frank,1 Giuseppina Sandri,2 Francesca D´Autilia,2 Renata V Contri,1 Maria Cristina Bonferoni,2 Carla Caramella,2 Alejandro G Frank,3 Adriana R Pohlmann,1 Silvia S Guterres11Pharmaceutical Science Graduate Program, Federal University of Rio Grande do Sul, Porto Alegre, RS, Brazil; 2Department of Drug Sciences, University of Pavia, Pavia, PV, Italy; 3Department of Industrial Engineering, Federal University of Rio Grande do Sul, Porto Alegre, RS, BrazilAbstract: The vaginal route of administration is an alternative for several treatments for either local or systemic pharmacological effects. However, the permanence of a drug in this route represents a challenge for formulation development that can be overcome by using nanoencapsulation and chitosan gel. Thus, this work aimed to evaluate the performance of chitosan hydrogels containing cationic and anionic acrylic-based nanocapsules (Eudragit® RS 100 and Eudragit® S 100, respectively) with Nile red as a model of lipophilic substance in the vaginal route of administration, as measured by increases in the residence time and the penetration of these formulations. Several formulations were prepared with increasing chitosan concentrations, and were analyzed in terms of pH and rheological behavior so that the most suitable formulation could be selected. The enhancement of the adhesion (tensile stress test and washability profile) and penetration (confocal laser scanning microscopy and extraction followed by quantification) properties of the formulations, when applied to porcine vaginal mucosa, were evaluated. The nanocapsule suspensions produced presented adequate properties: size of approximately 200 nm (polydispersity index of ≤0.2); zeta potential around +10 mV for the cationic formulation and -10 mV for the anionic formulation; and pH values of 6.1±0.1 (Eudragit RS 100), 5.3±0.2&am

Luiz Cláudio da Silva,1 Thiago Garcia,1 Michela Mori,2 Giuseppina Sandri,2 Maria Cristina Bonferoni,2 Priscila V Finotelli,1 Leonardo P Cinelli,1 Carla Caramella,2 Lúcio M Cabral11Drug Department, Rio de Janeiro Federal University, Rio de Janeiro, Brazil; 2Department of Drug Sciences, University of Pavia, Pavia, ItalyAbstract: The aim of this study was to produce and characterize nanoparticles (NPs), combining chondroitin sulfate (CS) and fucoidan (FC) with chitosan for therapeutic purposes. These NPs were characterized by dynamic light scattering, zeta potential determination, and transmission electronic microscopy. The anticoagulant activity was determined for FC NPs and compared with FC solution at the same concentration. FC NPs showed regular shapes and better anticoagulant activity than free polysaccharide solution. FC solution did not affect coagulation compared to FC NPs, which increased up to two-fold, even at a lower concentration. Cytotoxicity and permeability tests were conducted using Caco-2 cell monolayer, exhibiting no toxic effect in this cell line and higher permeability for NP2 samples than FC solution at the same concentration.Keywords: nanoparticles, chitosan, chondroitin sulfate, fucoidan, aPTT, Caco-2

Luiz Cláudio da Silva,1 Thiago Garcia,1 Michela Mori,2 Giuseppina Sandri,2 Maria Cristina Bonferoni,2 Priscila V Finotelli,1 Leonardo P Cinelli,1 Carla Caramella,2 Lúcio M Cabral11Drug Department, Rio de Janeiro Federal University, Rio de Janeiro, Brazil; 2Department of Drug Sciences, University of Pavia, Pavia, ItalyAbstract: The aim of this study was to produce and characterize nanoparticles (NPs), combining chondroitin sulfate (CS) and fucoidan (FC) with chitosan for therapeutic purposes. These NPs were characterized by dynamic light scattering, zeta potential determination, and transmission electronic microscopy. The anticoagulant activity was determined for FC NPs and compared with FC solution at the same concentration. FC NPs showed regular shapes and better anticoagulant activity than free polysaccharide solution. FC solution did not affect coagulation compared to FC NPs, which increased up to two-fold, even at a lower concentration. Cytotoxicity and permeability tests were conducted using Caco-2 cell monolayer, exhibiting no toxic effect in this cell line and higher permeability for NP2 samples than FC solution at the same concentration.Keywords: nanoparticles, chitosan, chondroitin sulfate, fucoidan, aPTT, Caco-2