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Massimo Fresta - One of the best experts on this subject based on the ideXlab platform.
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Novel PEG-coated Niosomes based on bola-surfactant as drug carriers for 5-fluorouracil
Biomedical Microdevices, 2009Co-Authors: Donato Cosco, D. Caponio, Rita Citraro, Nevio Picci, Donatella Paolino, Christian Celia, Rita Muzzalupo, Massimo FrestaAbstract:Innovative Niosomes made up of α,ω-hexadecyl-bis-(1-aza-18-crown-6) (bola), Span 80 and cholesterol (2:5:2 molar ratio) are proposed as suitable delivery systems for the administration of 5-fluorouracil (5-FU), an antitumoral compound largely used in the treatment of breast cancer. The bola-Niosomes, after sonication proce-dure, showed mean sizes of ~200 nm and a loading capacity of ~40% with respect to the amount of 5-FU added during the preparation. Similar findings wereachieved with PEG-coated bola-Niosomes (bola, Span 80, cholesterol, DSPE-mPEG2000, 2:5:2:0.1 molar ratio respectively). 5-FU-loaded PEG-coated and uncoated bola-Niosomes were tested on MCF-7 and T47D cells. Both bola-niosome formulations provided an increase in the cytotoxic effect with respect to the free drug. Confocal laser scanning microscopy studies were carried out to evaluate both the extent and the time-dependent bola-niosome-cell interaction. In vivo experiments on MCF-7 xenograft tumor SCID mice models showed a more effective antitumoral activity of the PEGylated niosomal 5-FU at a concentration ten times lower (8 mg/kg) than that of the free solution of the drug (80 mg/kg) after a treatment of 30 days.
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innovative bola surfactant Niosomes as topical delivery systems of 5 fluorouracil for the treatment of skin cancer
International Journal of Pharmaceutics, 2008Co-Authors: Donatella Paolino, Donato Cosco, Nevio Picci, Rita Muzzalupo, Elena Trapasso, Massimo FrestaAbstract:An innovative niosomal system made up of alpha,omega-hexadecyl-bis-(1-aza-18-crown-6) (Bola), Span 80 and cholesterol (2:5:2 molar ratio) was proposed as a topical delivery system for 5-fluorouracil (5-FU), largely used in the treatment of different forms of skin cancers. Bola-Niosomes showed a mean size of approximately 400 nm, which were reduced to approximately 200 nm by a sonication procedure with a polydispersion index value of 0.1. Bola-Niosomes showed a loading capacity of approximately 40% with respect to the amount of 5-FU added during the preparation. 5-FU-loaded bola-Niosomes were tested on SKMEL-28 (human melanoma) and HaCaT (non-melanoma skin cancer with a specific mutations in the p53 tumor suppressor gene) to assess the cytotoxic activity with respect to the free drug. 5-FU-loaded bola-Niosomes showed an improvement of the cytotoxic effect with respect to the free drug. Confocal laser scanning microscopy studies were carried out to evaluate both the extent and the time-dependent bola-niosome-cell interaction. The percutaneous permeation of 5-FU-loaded Niosomes was evaluated by using human stratum corneum and epidermis membranes. Bola-Niosomes provided an increase of the drug penetration of 8- and 4-folds with respect to a drug aqueous solution and to a mixture of empty bola-Niosomes with a drug aqueous solution.
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in vitro and in vivo evaluation of bola surfactant containing Niosomes for transdermal delivery
Biomedical Microdevices, 2007Co-Authors: Donatella Paolino, Antonio Ricciardi, Nevio Picci, Christian Celia, Rita Muzzalupo, Massimo FrestaAbstract:A novel niosome formulation is proposed for topical drug delivery of ammonium glycyrrhizinate, a natural compound with an efficacious anti-inflammatory activity. Niosomes were made up of a new non ionic surfactant, α,ω-hexadecyl-bis-(1-aza-18-crown-6) (Bola-surfactant)-Span 80-cholesterol (2:3:1 molar ratio). Niosome vesicles were prepared with the thin layer evaporation method and were physico-chemically characterized. The tolerability of Bola-surfactant both as free molecules or assembled ion niosome vesicles was evaluated in vitro on cultured of human keratinocyte cells (NCTC2544). Human tolerability was evaluated on volunteers. The ability of Bola-Niosomes to promote intracellular delivery was evaluated by confocal laser scanning microscopy (CLSM) studies. Human stratum corneum and epidermis (SCE) membranes were used in vitro to investigate the percutaneous permeation. The anti-inflammatory activity of ammonium glycyrrhizinate was evaluated in vivo on human volunteers with a chemically induced erythema. Experimental data show that Bola-Niosomes are characterized by a mean size of ∼400 nm and are able to provide an encapsulation efficiency of 40% with respect to the drug amount used during preparation. CLSM showed that Bola-Niosomes were able to promote the intracellular uptake of the delivered substances. Bola-Niosomes were also able to significantly improve (p <0.001) the percutaneous permeation of ammonium glycyrrhizinate with respect to both the aqueous drug solution and a physical mixture between unloaded Bola-Niosomes and the aqueous drug solution. Bola-Niosomes showed a suitable tolerability both in vitro and in vivo. Ammonium glycyrrhizinate-loaded Bola-Niosomes determined a significant (p <0.001) and noticeable improvement of the in vivo anti-inflammatory activity of the drug. An effective example of conjugating innovative colloidal carriers, coming from pharmaceutical nanotechnology, and therapeutically effective natural compounds, coming from traditional medicine, was reported.
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In vitro and in vivo evaluation of Bola-surfactant containing Niosomes for transdermal delivery
Biomedical Microdevices, 2007Co-Authors: Donatella Paolino, Antonio Ricciardi, Nevio Picci, Christian Celia, Rita Muzzalupo, Massimo FrestaAbstract:A novel niosome formulation is proposed for topical drug delivery of ammonium glycyrrhizinate, a natural compound with an efficacious anti-inflammatory activity. Niosomes were made up of a new non ionic surfactant, α,ω-hexadecyl-bis-(1-aza-18-crown-6) (Bolasurfactant)-Span 80-cholesterol (2:3:1 molar ratio). Niosome vesicles were prepared with the thin layer evaporation method and were physico-chemically characterized. The tolerability of Bola-surfactant both as free molecules or assembled ion niosome vesicles was evaluated in vitro on cultured of human keratinocyte cells (NCTC2544). Human tolerability was evaluated on volunteers. The ability of Bola-Niosomes to promote intracellular delivery was evaluated by confocal laser scanning microscopy (CLSM) studies. Human stratum corneum and epidermis (SCE) membranes were used in vitro to investigate the percutaneous permeation. The anti-inflammatory activity of ammonium glycyrrhizinate was evaluated in vivo on human volunteers with a chemically induced erythema. Experimental data show that Bola-Niosomes are characterized by amean size of ∼400 nm and are able to provide an encapsulation efficiency of 40% with respect to the drug amount used during preparation. CLSM showed that Bola-Niosomes were able to promote the intracellular uptake of the delivered substances. BolaNiosomes were also able to significantly improve (p
Donatella Paolino - One of the best experts on this subject based on the ideXlab platform.
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Novel PEG-coated Niosomes based on bola-surfactant as drug carriers for 5-fluorouracil
Biomedical Microdevices, 2009Co-Authors: Donato Cosco, D. Caponio, Rita Citraro, Nevio Picci, Donatella Paolino, Christian Celia, Rita Muzzalupo, Massimo FrestaAbstract:Innovative Niosomes made up of α,ω-hexadecyl-bis-(1-aza-18-crown-6) (bola), Span 80 and cholesterol (2:5:2 molar ratio) are proposed as suitable delivery systems for the administration of 5-fluorouracil (5-FU), an antitumoral compound largely used in the treatment of breast cancer. The bola-Niosomes, after sonication proce-dure, showed mean sizes of ~200 nm and a loading capacity of ~40% with respect to the amount of 5-FU added during the preparation. Similar findings wereachieved with PEG-coated bola-Niosomes (bola, Span 80, cholesterol, DSPE-mPEG2000, 2:5:2:0.1 molar ratio respectively). 5-FU-loaded PEG-coated and uncoated bola-Niosomes were tested on MCF-7 and T47D cells. Both bola-niosome formulations provided an increase in the cytotoxic effect with respect to the free drug. Confocal laser scanning microscopy studies were carried out to evaluate both the extent and the time-dependent bola-niosome-cell interaction. In vivo experiments on MCF-7 xenograft tumor SCID mice models showed a more effective antitumoral activity of the PEGylated niosomal 5-FU at a concentration ten times lower (8 mg/kg) than that of the free solution of the drug (80 mg/kg) after a treatment of 30 days.
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innovative bola surfactant Niosomes as topical delivery systems of 5 fluorouracil for the treatment of skin cancer
International Journal of Pharmaceutics, 2008Co-Authors: Donatella Paolino, Donato Cosco, Nevio Picci, Rita Muzzalupo, Elena Trapasso, Massimo FrestaAbstract:An innovative niosomal system made up of alpha,omega-hexadecyl-bis-(1-aza-18-crown-6) (Bola), Span 80 and cholesterol (2:5:2 molar ratio) was proposed as a topical delivery system for 5-fluorouracil (5-FU), largely used in the treatment of different forms of skin cancers. Bola-Niosomes showed a mean size of approximately 400 nm, which were reduced to approximately 200 nm by a sonication procedure with a polydispersion index value of 0.1. Bola-Niosomes showed a loading capacity of approximately 40% with respect to the amount of 5-FU added during the preparation. 5-FU-loaded bola-Niosomes were tested on SKMEL-28 (human melanoma) and HaCaT (non-melanoma skin cancer with a specific mutations in the p53 tumor suppressor gene) to assess the cytotoxic activity with respect to the free drug. 5-FU-loaded bola-Niosomes showed an improvement of the cytotoxic effect with respect to the free drug. Confocal laser scanning microscopy studies were carried out to evaluate both the extent and the time-dependent bola-niosome-cell interaction. The percutaneous permeation of 5-FU-loaded Niosomes was evaluated by using human stratum corneum and epidermis membranes. Bola-Niosomes provided an increase of the drug penetration of 8- and 4-folds with respect to a drug aqueous solution and to a mixture of empty bola-Niosomes with a drug aqueous solution.
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in vitro and in vivo evaluation of bola surfactant containing Niosomes for transdermal delivery
Biomedical Microdevices, 2007Co-Authors: Donatella Paolino, Antonio Ricciardi, Nevio Picci, Christian Celia, Rita Muzzalupo, Massimo FrestaAbstract:A novel niosome formulation is proposed for topical drug delivery of ammonium glycyrrhizinate, a natural compound with an efficacious anti-inflammatory activity. Niosomes were made up of a new non ionic surfactant, α,ω-hexadecyl-bis-(1-aza-18-crown-6) (Bola-surfactant)-Span 80-cholesterol (2:3:1 molar ratio). Niosome vesicles were prepared with the thin layer evaporation method and were physico-chemically characterized. The tolerability of Bola-surfactant both as free molecules or assembled ion niosome vesicles was evaluated in vitro on cultured of human keratinocyte cells (NCTC2544). Human tolerability was evaluated on volunteers. The ability of Bola-Niosomes to promote intracellular delivery was evaluated by confocal laser scanning microscopy (CLSM) studies. Human stratum corneum and epidermis (SCE) membranes were used in vitro to investigate the percutaneous permeation. The anti-inflammatory activity of ammonium glycyrrhizinate was evaluated in vivo on human volunteers with a chemically induced erythema. Experimental data show that Bola-Niosomes are characterized by a mean size of ∼400 nm and are able to provide an encapsulation efficiency of 40% with respect to the drug amount used during preparation. CLSM showed that Bola-Niosomes were able to promote the intracellular uptake of the delivered substances. Bola-Niosomes were also able to significantly improve (p <0.001) the percutaneous permeation of ammonium glycyrrhizinate with respect to both the aqueous drug solution and a physical mixture between unloaded Bola-Niosomes and the aqueous drug solution. Bola-Niosomes showed a suitable tolerability both in vitro and in vivo. Ammonium glycyrrhizinate-loaded Bola-Niosomes determined a significant (p <0.001) and noticeable improvement of the in vivo anti-inflammatory activity of the drug. An effective example of conjugating innovative colloidal carriers, coming from pharmaceutical nanotechnology, and therapeutically effective natural compounds, coming from traditional medicine, was reported.
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In vitro and in vivo evaluation of Bola-surfactant containing Niosomes for transdermal delivery
Biomedical Microdevices, 2007Co-Authors: Donatella Paolino, Antonio Ricciardi, Nevio Picci, Christian Celia, Rita Muzzalupo, Massimo FrestaAbstract:A novel niosome formulation is proposed for topical drug delivery of ammonium glycyrrhizinate, a natural compound with an efficacious anti-inflammatory activity. Niosomes were made up of a new non ionic surfactant, α,ω-hexadecyl-bis-(1-aza-18-crown-6) (Bolasurfactant)-Span 80-cholesterol (2:3:1 molar ratio). Niosome vesicles were prepared with the thin layer evaporation method and were physico-chemically characterized. The tolerability of Bola-surfactant both as free molecules or assembled ion niosome vesicles was evaluated in vitro on cultured of human keratinocyte cells (NCTC2544). Human tolerability was evaluated on volunteers. The ability of Bola-Niosomes to promote intracellular delivery was evaluated by confocal laser scanning microscopy (CLSM) studies. Human stratum corneum and epidermis (SCE) membranes were used in vitro to investigate the percutaneous permeation. The anti-inflammatory activity of ammonium glycyrrhizinate was evaluated in vivo on human volunteers with a chemically induced erythema. Experimental data show that Bola-Niosomes are characterized by amean size of ∼400 nm and are able to provide an encapsulation efficiency of 40% with respect to the drug amount used during preparation. CLSM showed that Bola-Niosomes were able to promote the intracellular uptake of the delivered substances. BolaNiosomes were also able to significantly improve (p
Jon Zarate - One of the best experts on this subject based on the ideXlab platform.
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polysorbate 20 non ionic surfactant enhances retinal gene delivery efficiency of cationic Niosomes after intravitreal and subretinal administration
International Journal of Pharmaceutics, 2018Co-Authors: Ilia Villatebeitia, Idoia Gallego, Gema Martineznavarrete, Jon Zarate, Tania Lopezmendez, Cristina SotosanchezAbstract:Abstract The success of non-viral vectors based on cationic Niosomes for retinal gene delivery applications depends on the ability to achieve persistent and high levels of transgene expression, ideally from a single administration. In this work, we studied the effect of the non-ionic surfactant component of Niosomes in their transfection efficiency in rat retina. For that purpose, three niosome formulations that only differed in the non-ionic tensioactives were elaborated. Niosomes contained: cationic lipid 1,2-di-O-octadecenyl-3-trimethylammonium propane (DOTMA), helper lipid squalene and polysorbate 20, polysorbate 80 or polysorbate 85. Niosomes and corresponding nioplexes were fully characterized in terms of size, polydispersity index, zeta potential, morphology and ability to protect and release DNA. In vitro experiments were carried out to evaluate transfection efficiency, cell viability and intracellular trafficking pathways of the formulations. Nioplexes based on polysorbate 20 Niosomes were the most efficient transfecting retinal cells in vitro . Moreover, subretinal and intravitreal administration of those nioplexes in vivo showed also high levels of transgene expression in rat retinas. Our results demonstrate that the incorporation of polysorbate 20 in cationic Niosomes enhances retinal gene delivery. Thus, this formulation emerges as a potential non-viral candidate to efficiently transfer specific therapeutic genes into the eye for biomedical purposes.
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the role of helper lipids in the intracellular disposition and transfection efficiency of niosome formulations for gene delivery to retinal pigment epithelial cells
International Journal of Pharmaceutics, 2016Co-Authors: Jon Zarate, Santiago Grijalvo, Edilberto Ojeda, Gustavo Puras, Mireia AgirreAbstract:In this work, we carried out a comparative study of four different niosome formulations based on the same cationic lipid and non-ionic tensoactive. The Niosomes prepared by oil-in-water emulsion technique (o/w) only differed in the helper lipid composition: squalene, cholesterol, squalane or no helper lipid. Niosomes and nioplexes elaborated upon the addition of pCMS-EGFP reporter plasmid were characterized in terms of size, zeta potential and polydispersity index. The capacity of the Niosomes to condense, release and protect the DNA against enzymatic degradation was evaluated by agarose gel electrophoresis. In vitro experiments were carried out to evaluate transfection efficiency and cell viability in retinal pigment epithelial cells. Moreover, uptake and intracellular trafficking studies were performed to further understand the role of the helper lipids in the transfection process. Interestingly, among all tested formulations, Niosomes elaborated with squalene as helper lipid were the most efficient transfecting cells. Such transfection efficiency could be attributed to their higher cellular uptake and the particular entry pathways used, where macropinocytosis pathway and lysosomal release played an important role. Therefore, these results suggest that helper lipid composition is a crucial step to be considered in the design of niosome formulation for retinal gene delivery applications since clearly modulates the cellular uptake, internalization mechanism and consequently, the final transfection efficiency.
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elaboration and physicochemical characterization of niosome based nioplexes for gene delivery purposes
Methods of Molecular Biology, 2016Co-Authors: Ilia Villatebeitia, Edilberto Ojeda, Gustavo Puras, Mireia Agirre, Mohamed Mashal, Jon ZarateAbstract:Niosome formulations for gene delivery purposes are based on nonionic surfactants, helper lipids, and cationic lipids that interact electrostatically with negatively charged DNA molecules to form the so-called nioplexes. Niosomes are elaborated by different techniques, such as solvent emulsion-evaporation, thin film hydration, hand-shaking, dissolvent injection, and microfluidization method, among many others. In this chapter, we have described some protocols for the elaboration of Niosomes and nioplexes and their physicochemical characterization that guarantees the quality criteria of the formulation in terms of size, morphology, ζ-potential, and stability.
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a novel cationic niosome formulation for gene delivery to the retina
Journal of Controlled Release, 2014Co-Authors: Jon Zarate, Edilberto Ojeda, Gustavo Puras, Mireia Agirre, Mohamed Mashal, Santiago GrijalvoAbstract:Abstract Niosomes represent a recent promising approach for gene delivery purposes. We elaborated on a novel niosome formulation based on the 2,3-di(tetradecyloxy)propan-1-amine cationic lipid, combined with squalene and polysorbate 80 to evaluate the transfection efficiency in rat retinas. Niosomes prepared by the solvent emulsification–evaporation technique were mixed with the pCMSEGFP plasmid to form lipoplexes which were characterized in terms of morphology, size, surface charge, and DNA condensation, protection and release. In vitro studies were conducted to evaluate transfection efficiency, viability and internalization mechanism in HEK-293 and ARPE-19 cells. The efficacy of the most promising formulation was evaluated in rat eyes by monitoring the expression of the EGFP after intravitreal and subretinal injections. Lipoplexes at 15/1 ratio were 200 nm in size, 25 mV in zeta potential and exhibited spherical morphology. At this ratio, Niosomes condensed and protected the DNA from enzymatic digestion. Lipoplexes successfully transfected HEK-293 and specially ARPE-19 cells, without affecting the viability. Whereas lipoplexes entered mainly retinal cells by clathrin-mediated endocytosis, HEK-293 cells showed a higher caveolae-dependent entry. After ocular administration, the expression of EGFP was detected in different cells of the retina depending on the administration route. This novel niosome formulation represents a promising approach to deliver genetic material into the retina to treat inherited retinal diseases.
Rita Muzzalupo - One of the best experts on this subject based on the ideXlab platform.
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Novel PEG-coated Niosomes based on bola-surfactant as drug carriers for 5-fluorouracil
Biomedical Microdevices, 2009Co-Authors: Donato Cosco, D. Caponio, Rita Citraro, Nevio Picci, Donatella Paolino, Christian Celia, Rita Muzzalupo, Massimo FrestaAbstract:Innovative Niosomes made up of α,ω-hexadecyl-bis-(1-aza-18-crown-6) (bola), Span 80 and cholesterol (2:5:2 molar ratio) are proposed as suitable delivery systems for the administration of 5-fluorouracil (5-FU), an antitumoral compound largely used in the treatment of breast cancer. The bola-Niosomes, after sonication proce-dure, showed mean sizes of ~200 nm and a loading capacity of ~40% with respect to the amount of 5-FU added during the preparation. Similar findings wereachieved with PEG-coated bola-Niosomes (bola, Span 80, cholesterol, DSPE-mPEG2000, 2:5:2:0.1 molar ratio respectively). 5-FU-loaded PEG-coated and uncoated bola-Niosomes were tested on MCF-7 and T47D cells. Both bola-niosome formulations provided an increase in the cytotoxic effect with respect to the free drug. Confocal laser scanning microscopy studies were carried out to evaluate both the extent and the time-dependent bola-niosome-cell interaction. In vivo experiments on MCF-7 xenograft tumor SCID mice models showed a more effective antitumoral activity of the PEGylated niosomal 5-FU at a concentration ten times lower (8 mg/kg) than that of the free solution of the drug (80 mg/kg) after a treatment of 30 days.
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innovative bola surfactant Niosomes as topical delivery systems of 5 fluorouracil for the treatment of skin cancer
International Journal of Pharmaceutics, 2008Co-Authors: Donatella Paolino, Donato Cosco, Nevio Picci, Rita Muzzalupo, Elena Trapasso, Massimo FrestaAbstract:An innovative niosomal system made up of alpha,omega-hexadecyl-bis-(1-aza-18-crown-6) (Bola), Span 80 and cholesterol (2:5:2 molar ratio) was proposed as a topical delivery system for 5-fluorouracil (5-FU), largely used in the treatment of different forms of skin cancers. Bola-Niosomes showed a mean size of approximately 400 nm, which were reduced to approximately 200 nm by a sonication procedure with a polydispersion index value of 0.1. Bola-Niosomes showed a loading capacity of approximately 40% with respect to the amount of 5-FU added during the preparation. 5-FU-loaded bola-Niosomes were tested on SKMEL-28 (human melanoma) and HaCaT (non-melanoma skin cancer with a specific mutations in the p53 tumor suppressor gene) to assess the cytotoxic activity with respect to the free drug. 5-FU-loaded bola-Niosomes showed an improvement of the cytotoxic effect with respect to the free drug. Confocal laser scanning microscopy studies were carried out to evaluate both the extent and the time-dependent bola-niosome-cell interaction. The percutaneous permeation of 5-FU-loaded Niosomes was evaluated by using human stratum corneum and epidermis membranes. Bola-Niosomes provided an increase of the drug penetration of 8- and 4-folds with respect to a drug aqueous solution and to a mixture of empty bola-Niosomes with a drug aqueous solution.
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in vitro and in vivo evaluation of bola surfactant containing Niosomes for transdermal delivery
Biomedical Microdevices, 2007Co-Authors: Donatella Paolino, Antonio Ricciardi, Nevio Picci, Christian Celia, Rita Muzzalupo, Massimo FrestaAbstract:A novel niosome formulation is proposed for topical drug delivery of ammonium glycyrrhizinate, a natural compound with an efficacious anti-inflammatory activity. Niosomes were made up of a new non ionic surfactant, α,ω-hexadecyl-bis-(1-aza-18-crown-6) (Bola-surfactant)-Span 80-cholesterol (2:3:1 molar ratio). Niosome vesicles were prepared with the thin layer evaporation method and were physico-chemically characterized. The tolerability of Bola-surfactant both as free molecules or assembled ion niosome vesicles was evaluated in vitro on cultured of human keratinocyte cells (NCTC2544). Human tolerability was evaluated on volunteers. The ability of Bola-Niosomes to promote intracellular delivery was evaluated by confocal laser scanning microscopy (CLSM) studies. Human stratum corneum and epidermis (SCE) membranes were used in vitro to investigate the percutaneous permeation. The anti-inflammatory activity of ammonium glycyrrhizinate was evaluated in vivo on human volunteers with a chemically induced erythema. Experimental data show that Bola-Niosomes are characterized by a mean size of ∼400 nm and are able to provide an encapsulation efficiency of 40% with respect to the drug amount used during preparation. CLSM showed that Bola-Niosomes were able to promote the intracellular uptake of the delivered substances. Bola-Niosomes were also able to significantly improve (p <0.001) the percutaneous permeation of ammonium glycyrrhizinate with respect to both the aqueous drug solution and a physical mixture between unloaded Bola-Niosomes and the aqueous drug solution. Bola-Niosomes showed a suitable tolerability both in vitro and in vivo. Ammonium glycyrrhizinate-loaded Bola-Niosomes determined a significant (p <0.001) and noticeable improvement of the in vivo anti-inflammatory activity of the drug. An effective example of conjugating innovative colloidal carriers, coming from pharmaceutical nanotechnology, and therapeutically effective natural compounds, coming from traditional medicine, was reported.
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In vitro and in vivo evaluation of Bola-surfactant containing Niosomes for transdermal delivery
Biomedical Microdevices, 2007Co-Authors: Donatella Paolino, Antonio Ricciardi, Nevio Picci, Christian Celia, Rita Muzzalupo, Massimo FrestaAbstract:A novel niosome formulation is proposed for topical drug delivery of ammonium glycyrrhizinate, a natural compound with an efficacious anti-inflammatory activity. Niosomes were made up of a new non ionic surfactant, α,ω-hexadecyl-bis-(1-aza-18-crown-6) (Bolasurfactant)-Span 80-cholesterol (2:3:1 molar ratio). Niosome vesicles were prepared with the thin layer evaporation method and were physico-chemically characterized. The tolerability of Bola-surfactant both as free molecules or assembled ion niosome vesicles was evaluated in vitro on cultured of human keratinocyte cells (NCTC2544). Human tolerability was evaluated on volunteers. The ability of Bola-Niosomes to promote intracellular delivery was evaluated by confocal laser scanning microscopy (CLSM) studies. Human stratum corneum and epidermis (SCE) membranes were used in vitro to investigate the percutaneous permeation. The anti-inflammatory activity of ammonium glycyrrhizinate was evaluated in vivo on human volunteers with a chemically induced erythema. Experimental data show that Bola-Niosomes are characterized by amean size of ∼400 nm and are able to provide an encapsulation efficiency of 40% with respect to the drug amount used during preparation. CLSM showed that Bola-Niosomes were able to promote the intracellular uptake of the delivered substances. BolaNiosomes were also able to significantly improve (p
Nevio Picci - One of the best experts on this subject based on the ideXlab platform.
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Novel PEG-coated Niosomes based on bola-surfactant as drug carriers for 5-fluorouracil
Biomedical Microdevices, 2009Co-Authors: Donato Cosco, D. Caponio, Rita Citraro, Nevio Picci, Donatella Paolino, Christian Celia, Rita Muzzalupo, Massimo FrestaAbstract:Innovative Niosomes made up of α,ω-hexadecyl-bis-(1-aza-18-crown-6) (bola), Span 80 and cholesterol (2:5:2 molar ratio) are proposed as suitable delivery systems for the administration of 5-fluorouracil (5-FU), an antitumoral compound largely used in the treatment of breast cancer. The bola-Niosomes, after sonication proce-dure, showed mean sizes of ~200 nm and a loading capacity of ~40% with respect to the amount of 5-FU added during the preparation. Similar findings wereachieved with PEG-coated bola-Niosomes (bola, Span 80, cholesterol, DSPE-mPEG2000, 2:5:2:0.1 molar ratio respectively). 5-FU-loaded PEG-coated and uncoated bola-Niosomes were tested on MCF-7 and T47D cells. Both bola-niosome formulations provided an increase in the cytotoxic effect with respect to the free drug. Confocal laser scanning microscopy studies were carried out to evaluate both the extent and the time-dependent bola-niosome-cell interaction. In vivo experiments on MCF-7 xenograft tumor SCID mice models showed a more effective antitumoral activity of the PEGylated niosomal 5-FU at a concentration ten times lower (8 mg/kg) than that of the free solution of the drug (80 mg/kg) after a treatment of 30 days.
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innovative bola surfactant Niosomes as topical delivery systems of 5 fluorouracil for the treatment of skin cancer
International Journal of Pharmaceutics, 2008Co-Authors: Donatella Paolino, Donato Cosco, Nevio Picci, Rita Muzzalupo, Elena Trapasso, Massimo FrestaAbstract:An innovative niosomal system made up of alpha,omega-hexadecyl-bis-(1-aza-18-crown-6) (Bola), Span 80 and cholesterol (2:5:2 molar ratio) was proposed as a topical delivery system for 5-fluorouracil (5-FU), largely used in the treatment of different forms of skin cancers. Bola-Niosomes showed a mean size of approximately 400 nm, which were reduced to approximately 200 nm by a sonication procedure with a polydispersion index value of 0.1. Bola-Niosomes showed a loading capacity of approximately 40% with respect to the amount of 5-FU added during the preparation. 5-FU-loaded bola-Niosomes were tested on SKMEL-28 (human melanoma) and HaCaT (non-melanoma skin cancer with a specific mutations in the p53 tumor suppressor gene) to assess the cytotoxic activity with respect to the free drug. 5-FU-loaded bola-Niosomes showed an improvement of the cytotoxic effect with respect to the free drug. Confocal laser scanning microscopy studies were carried out to evaluate both the extent and the time-dependent bola-niosome-cell interaction. The percutaneous permeation of 5-FU-loaded Niosomes was evaluated by using human stratum corneum and epidermis membranes. Bola-Niosomes provided an increase of the drug penetration of 8- and 4-folds with respect to a drug aqueous solution and to a mixture of empty bola-Niosomes with a drug aqueous solution.
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in vitro and in vivo evaluation of bola surfactant containing Niosomes for transdermal delivery
Biomedical Microdevices, 2007Co-Authors: Donatella Paolino, Antonio Ricciardi, Nevio Picci, Christian Celia, Rita Muzzalupo, Massimo FrestaAbstract:A novel niosome formulation is proposed for topical drug delivery of ammonium glycyrrhizinate, a natural compound with an efficacious anti-inflammatory activity. Niosomes were made up of a new non ionic surfactant, α,ω-hexadecyl-bis-(1-aza-18-crown-6) (Bola-surfactant)-Span 80-cholesterol (2:3:1 molar ratio). Niosome vesicles were prepared with the thin layer evaporation method and were physico-chemically characterized. The tolerability of Bola-surfactant both as free molecules or assembled ion niosome vesicles was evaluated in vitro on cultured of human keratinocyte cells (NCTC2544). Human tolerability was evaluated on volunteers. The ability of Bola-Niosomes to promote intracellular delivery was evaluated by confocal laser scanning microscopy (CLSM) studies. Human stratum corneum and epidermis (SCE) membranes were used in vitro to investigate the percutaneous permeation. The anti-inflammatory activity of ammonium glycyrrhizinate was evaluated in vivo on human volunteers with a chemically induced erythema. Experimental data show that Bola-Niosomes are characterized by a mean size of ∼400 nm and are able to provide an encapsulation efficiency of 40% with respect to the drug amount used during preparation. CLSM showed that Bola-Niosomes were able to promote the intracellular uptake of the delivered substances. Bola-Niosomes were also able to significantly improve (p <0.001) the percutaneous permeation of ammonium glycyrrhizinate with respect to both the aqueous drug solution and a physical mixture between unloaded Bola-Niosomes and the aqueous drug solution. Bola-Niosomes showed a suitable tolerability both in vitro and in vivo. Ammonium glycyrrhizinate-loaded Bola-Niosomes determined a significant (p <0.001) and noticeable improvement of the in vivo anti-inflammatory activity of the drug. An effective example of conjugating innovative colloidal carriers, coming from pharmaceutical nanotechnology, and therapeutically effective natural compounds, coming from traditional medicine, was reported.
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In vitro and in vivo evaluation of Bola-surfactant containing Niosomes for transdermal delivery
Biomedical Microdevices, 2007Co-Authors: Donatella Paolino, Antonio Ricciardi, Nevio Picci, Christian Celia, Rita Muzzalupo, Massimo FrestaAbstract:A novel niosome formulation is proposed for topical drug delivery of ammonium glycyrrhizinate, a natural compound with an efficacious anti-inflammatory activity. Niosomes were made up of a new non ionic surfactant, α,ω-hexadecyl-bis-(1-aza-18-crown-6) (Bolasurfactant)-Span 80-cholesterol (2:3:1 molar ratio). Niosome vesicles were prepared with the thin layer evaporation method and were physico-chemically characterized. The tolerability of Bola-surfactant both as free molecules or assembled ion niosome vesicles was evaluated in vitro on cultured of human keratinocyte cells (NCTC2544). Human tolerability was evaluated on volunteers. The ability of Bola-Niosomes to promote intracellular delivery was evaluated by confocal laser scanning microscopy (CLSM) studies. Human stratum corneum and epidermis (SCE) membranes were used in vitro to investigate the percutaneous permeation. The anti-inflammatory activity of ammonium glycyrrhizinate was evaluated in vivo on human volunteers with a chemically induced erythema. Experimental data show that Bola-Niosomes are characterized by amean size of ∼400 nm and are able to provide an encapsulation efficiency of 40% with respect to the drug amount used during preparation. CLSM showed that Bola-Niosomes were able to promote the intracellular uptake of the delivered substances. BolaNiosomes were also able to significantly improve (p