Ketorolac is an NSAID (Non-Steroidal Anti-Inflammatory Drug) used in the treatment of post-quirurgical pain and inflammation in cataract removal. The actual eyedrops have a short time of action and low levels of drug in the affected zone. The drug formulations destinated to ocular delivery are a challenge due to the difficulty of the drugs to reach the posterior segment of the eye and the requirements for been administrated to the eye. These polymers interact with the mucine therefore increasing the mucoadhesivity of the nanoparticles. Using nanoparticles formed by mucoadhesives polymers could improve the terapeutical effect of ketorolac. Due to their low stability, is proper to make a drying to eliminate the solvent of the nanoparticles. In this work a preparation of λ-carrageenan and poly-L-lysine is proposed. As a method to increased the long-term stability of these nanoparticles, three lyophilization cicles were realised according to the freezing speed of the nanoparticles. Nanoparticles with a ketorolac’s concentration of 0,4 mg/ml and 1 mg/mL were prepared with the λ-carrageenan and poly-L-lysine, and then freeze dried with low freezing and fast freezing (with líquid nitrogen). Particle size and polidispersion were observed before and after the lyophilization.
In questo lavoro sperimentale viene proposto l’utilizzo di nanoparticelle costituite da polimeri mucoadesivi (carragenina e polilisina) come possibile miglioramento dell'effetto terapeutico del ketorolac. Per aumentare la stabilità a lungo termine delle nanoparticelle sintetizzate è poi doveroso procedere all’essiccamento per eliminare il solvente dai campioni e a tal fine si sono sperimentati 3 protocolli di liofilizzazione: congelamento lento a temperatura ambiente, congelamento lento a -40°C e congelamento rapido con azoto liquido. Le nanoparticelle sono state sintetizzate a concentrazioni di 0,4 mg/mL e 1 mg/mL e sono state poi ricoperte con TMC, in diverse proporzioni. Si è sempre tenuto sotto controllo la stabilità di tali particelle analizzandone il size ad intervalli di tempo regolari (ogni 14 giorni). Il diametro e l’indice di polidispersione sono stati verificati attraverso l’utilizzo della tecnica DLS e AFM.
SVILUPPO DI NANOPARTICELLE MUCOADESIVE DI KETOROLAC PER LA SOMMINISTRAZIONE OFTALMICA
BOTTA CHINNICI, FEDERICA
2014/2015
Abstract
Ketorolac is an NSAID (Non-Steroidal Anti-Inflammatory Drug) used in the treatment of post-quirurgical pain and inflammation in cataract removal. The actual eyedrops have a short time of action and low levels of drug in the affected zone. The drug formulations destinated to ocular delivery are a challenge due to the difficulty of the drugs to reach the posterior segment of the eye and the requirements for been administrated to the eye. These polymers interact with the mucine therefore increasing the mucoadhesivity of the nanoparticles. Using nanoparticles formed by mucoadhesives polymers could improve the terapeutical effect of ketorolac. Due to their low stability, is proper to make a drying to eliminate the solvent of the nanoparticles. In this work a preparation of λ-carrageenan and poly-L-lysine is proposed. As a method to increased the long-term stability of these nanoparticles, three lyophilization cicles were realised according to the freezing speed of the nanoparticles. Nanoparticles with a ketorolac’s concentration of 0,4 mg/ml and 1 mg/mL were prepared with the λ-carrageenan and poly-L-lysine, and then freeze dried with low freezing and fast freezing (with líquid nitrogen). Particle size and polidispersion were observed before and after the lyophilization.È consentito all'utente scaricare e condividere i documenti disponibili a testo pieno in UNITESI UNIPV nel rispetto della licenza Creative Commons del tipo CC BY NC ND.
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https://hdl.handle.net/20.500.14239/20240