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Molecules 2018, 23(4), 739; https://doi.org/10.3390/molecules23040739

Encapsulation of Curcumin-Loaded Liposomes for Colonic Drug Delivery in a pH-Responsive Polymer Cluster Using a pH-Driven and Organic Solvent-Free Process

1
Department of Chemistry, University of Bari, Via Orabona 4, 70126 Bari, Italy
2
CNR-IPCF Institute for Physical and Chemical Processes, Bari unit, Via Orabona 4, 70126 Bari, Italy
3
Department of Biological and Environmental Sciences and Technologies, University of Salento, SP Lecce-Monteroni, I-73100 Lecce, Italy
4
CNR-ICCOM Institute of chemistry of organometallic compounds, Bari unit, Via E. Orabona, 4, 70126 Bari, Italy
5
CNR-ISPA Institute of Sciences of Food Production, Via G. Amendola 122/O, 70125 Bari, Italy
*
Authors to whom correspondence should be addressed.
Received: 6 February 2018 / Revised: 9 March 2018 / Accepted: 21 March 2018 / Published: 23 March 2018
(This article belongs to the Special Issue Chemical Transformation of Renewable Material for Green Chemistry)
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Abstract

The present study aimed to develop and optimize liposome formulation for the colonic delivery of biologically active compounds. A strategy to facilitate such targeting is to formulate liposomes 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 coated with the pH-responsive polymer Eudragit S100 were prepared and characterized. Curcumin was encapsulated 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 Eudragit S100 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 antioxidant activity. In particular, curcumin-loaded liposomes displayed size lower than 100 nm, encapsulation efficiency of 98%, high stability at both 4 °C and 25 °C, high in vitro antioxidant activity, and a cumulative release that was completed within 200 min. A good Eudragit S100 coating which did not alter the properties of the curcumin-loaded liposomes was obtained. The present work therefore provides a fast and solvent-free method to prepare pH-responsive polymer-coated liposomes for the colonic delivery of biologically active compounds. View Full-Text
Keywords: curcumin; nanoliposomes; Eudragit S100; colonic drug delivery; TEAC; pH jump method curcumin; nanoliposomes; Eudragit S100; colonic drug delivery; TEAC; pH jump method
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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De Leo, V.; Milano, F.; Mancini, E.; Comparelli, R.; Giotta, L.; Nacci, A.; Longobardi, F.; Garbetta, A.; Agostiano, A.; Catucci, L. Encapsulation of Curcumin-Loaded Liposomes for Colonic Drug Delivery in a pH-Responsive Polymer Cluster Using a pH-Driven and Organic Solvent-Free Process. Molecules 2018, 23, 739.

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