Abstract

The present study aimed to develop and optimize liposome formulation for the colonicdelivery of biologically active compounds. A strategy to facilitate such targeting is to formulateliposomes with a polymer coating sensitive to the pH shifts in the gastrointestinal tract. To this end,liposomes encapsulating curcumin--chosen as the biologically active compound model--and coatedwith the pH-responsive polymer Eudragit S100 were prepared and characterized. Curcumin wasencapsulated into small unilamellar vesicles (SUVs) by the micelle-to-vesicle transition method (MVT)in a simple and organic solvent-free way. Curcumin-loaded liposomes were coated with EudragitS100 by a fast and easily scalable pH-driven method. The prepared liposomes were evaluated for size,surface morphology, entrapment efficiency, stability, in vitro drug release, and curcumin antioxidantactivity. In particular, curcumin-loaded liposomes displayed size lower than 100 nm, encapsulationefficiency of 98%, high stability at both 4 oC and 25 oC, high in vitro antioxidant activity, and acumulative release that was completed within 200 min. A good Eudragit S100 coating which didnot alter the properties of the curcumin-loaded liposomes was obtained. The present work thereforeprovides a fast and solvent-free method to prepare pH-responsive polymer-coated liposomes for thecolonic delivery of biologically active compounds.

Autore Pugliese

• Milano Francesco , Comparelli Roberto

Tutti gli autori

• De Leo V.; Milano F.; Mancini E.; Comparelli R.; Giotta L.; Nacci A.; Longobardi F.; Garbetta A.; Agostiano A.; Catucci L.

Titolo volume/Rivista

Molecules

Anno di pubblicazione

2018

ISSN

1420-3049

ISBN

Non Disponibile

Numero di citazioni Wos

Nessuna citazione

Ultimo Aggiornamento Citazioni

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Numero di citazioni Scopus

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Ultimo Aggiornamento Citazioni

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Settori ERC

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Codici ASJC

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