Planta Med 2017; 83(05): 420-425
DOI: 10.1055/s-0042-103161
Formulation and Delivery Systems of Natural Products
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

New Dendrimer-Based Nanoparticles Enhance Curcumin Solubility

Maria Cristina Falconieri
1   Dipartimento di Chimica, Università degli Studi di Firenze, Sesto Fiorentino, Italy
,
Mauro Adamo
2   Department of Pharmaceutical and Medicinal Chemistry, Royal College of Surgeons in Ireland, Dublin, Ireland
,
Claudio Monasterolo
2   Department of Pharmaceutical and Medicinal Chemistry, Royal College of Surgeons in Ireland, Dublin, Ireland
,
Maria Camilla Bergonzi
1   Dipartimento di Chimica, Università degli Studi di Firenze, Sesto Fiorentino, Italy
,
Marcella Coronnello
3   Dipartimento di Scienze della Salute, Sezione di Farmacologia Clinica e Oncologia, Università degli Studi di Firenze, Firenze, Italy
,
Anna Rita Bilia
1   Dipartimento di Chimica, Università degli Studi di Firenze, Sesto Fiorentino, Italy
› Author Affiliations
Further Information

Publication History

received 04 December 2015
revised 29 January 2016

accepted 04 February 2016

Publication Date:
22 March 2016 (online)

Abstract

Curcumin, the main curcuminoid of the popular Indian spice turmeric, is a potent chemopreventive agent and useful in many different diseases. A major limitation of applicability of curcumin as a health promoting and medicinal agent is its extremely low bioavailability due to efficient first pass metabolism, poor gastrointestinal absorption, rapid elimination, and poor aqueous solubility. In the present study, nanotechnology was selected as a choice approach to enhance the bioavailability of the curcuminis. A new polyamidoamine dendrimer (G0.5) was synthesized, characterized, and tested for cytotoxicity in human breast cancer cells (MCF-7). No cytotoxicity of G0.5 was found in the range between 10−3 and 3 × 10−8 M. Consequently, G0.5 was used to prepare spherical nanoparticles of ca. 150 nm, which were loaded with curcumin [molar ratio G0.5/curcumin 1 : 1 (formulation 1) and 1 : 0.5 (formulation 2)]. Remarkably, the occurrence of a single population of nanoparticles having an excellent polydispersity index (< 0.20) was found in both formulations. Formulation 1 was selected to test in vitro drug release because it was superior in terms of encapsulation efficiency (62 %) and loading capacity (32 %). The solubility of curcumin was increased ca. 415 and 150 times with respect to the unformulated drug, respectively, for formulation 1 and formulation 2. The release of curcumin from the nanoparticles showed an interesting prolonged and sustained release profile.

 
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