Publicação
The use of nanoparticles as drug delivery systems for topical administration in the eye
| Resumo: | Ceftazidime is a broad spectrum third generation cephalosporin antibiotic which is effective against pathogens that are usually responsible for ophthalmological infections. Ceftazidime offers a good coverage against Pseudomonas aeruginosa as well as resistance to several types of beta lactamases. As a result it is commonly used for the treatment of ophthalmological infections particularly caused by P. aeruginosa. Even so, ceftazidime undergoes rapid degradation in aqueous solutions, thus eye drops containing ceftazidime in aqueous solutions are not commercially available. On the other hand, the entry of eye drops in the ocular globe is hampered by the barriers protecting the eye. The aim of the present work was to prepare a mucoadhesive nanoparticle eye drop formulation containing ceftazidime to treat eye infections. Our objective was to develop an eye drop with mucoadhesive polymers which prolongs the retention of drugs in the ocular surface and in consequence its bioavailability. These solutions were characterized in terms of pH, osmolality, viscosity and zeta potential. To overcome the instability problem of ceftazidime in aqueous solutions and contributing to increase the bioavailability, Chitosan/TPP-Hyaluronic Acid nanoparticles were developed to encapsulate ceftazidime. In order to optimize a nanoparticulate system for a potential eye drop formulation the nanoparticles were characterized for their size, zeta potential and the ceftazidime encapsulation efficiency. In addition, the in vitro release and permeation studies were performed and the results suggest a prolonged drug release from the nanoparticles. The results of nanoparticles interaction with mucin highlight their mucoadhesivity and ability to interact with the ocular surface thus increasing the drug residence time in the eye. The prepared nanoparticles were subjected to stability and microbiological studies with satisfactory results. In conclusion, Chitosan/TPP-Hyaluronic Acid nanoparticles proved to be a promising platform for ceftazidime delivery in the eye. |
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| Autores principais: | Silva, Mariana Monteiro da |
| Assunto: | Ceftazidime Eye drop solution Mucoadhesive polymers Nanoparticles Mestrado Integrado - 2016 |
| Ano: | 2016 |
| País: | Portugal |
| Tipo de documento: | dissertação de mestrado |
| Tipo de acesso: | acesso restrito |
| Instituição associada: | Universidade de Lisboa |
| Idioma: | inglês |
| Origem: | Repositório da Universidade de Lisboa |
| Resumo: | Ceftazidime is a broad spectrum third generation cephalosporin antibiotic which is effective against pathogens that are usually responsible for ophthalmological infections. Ceftazidime offers a good coverage against Pseudomonas aeruginosa as well as resistance to several types of beta lactamases. As a result it is commonly used for the treatment of ophthalmological infections particularly caused by P. aeruginosa. Even so, ceftazidime undergoes rapid degradation in aqueous solutions, thus eye drops containing ceftazidime in aqueous solutions are not commercially available. On the other hand, the entry of eye drops in the ocular globe is hampered by the barriers protecting the eye. The aim of the present work was to prepare a mucoadhesive nanoparticle eye drop formulation containing ceftazidime to treat eye infections. Our objective was to develop an eye drop with mucoadhesive polymers which prolongs the retention of drugs in the ocular surface and in consequence its bioavailability. These solutions were characterized in terms of pH, osmolality, viscosity and zeta potential. To overcome the instability problem of ceftazidime in aqueous solutions and contributing to increase the bioavailability, Chitosan/TPP-Hyaluronic Acid nanoparticles were developed to encapsulate ceftazidime. In order to optimize a nanoparticulate system for a potential eye drop formulation the nanoparticles were characterized for their size, zeta potential and the ceftazidime encapsulation efficiency. In addition, the in vitro release and permeation studies were performed and the results suggest a prolonged drug release from the nanoparticles. The results of nanoparticles interaction with mucin highlight their mucoadhesivity and ability to interact with the ocular surface thus increasing the drug residence time in the eye. The prepared nanoparticles were subjected to stability and microbiological studies with satisfactory results. In conclusion, Chitosan/TPP-Hyaluronic Acid nanoparticles proved to be a promising platform for ceftazidime delivery in the eye. |
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