Planta Med 2013; 79(06): 447-451
DOI: 10.1055/s-0032-1328363
Biological and Pharmacological Activity
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Antitumor Activity of PEGylated Nanoliposomes Containing Crocin in Mice Bearing C26 Colon Carcinoma

Marziyeh Rastgoo
1  Biotechnology Research Center, Nanotechnology Research Center, School of Pharmacy, Mashhad University of Medical Science, Mashhad, Iran
,
Hossein Hosseinzadeh
2  Pharmaceutical Research Center, School of Pharmacy, Mashhad University of Medical Science, Mashhad, Iran
,
Hoda Alavizadeh
1  Biotechnology Research Center, Nanotechnology Research Center, School of Pharmacy, Mashhad University of Medical Science, Mashhad, Iran
,
Azam Abbasi
1  Biotechnology Research Center, Nanotechnology Research Center, School of Pharmacy, Mashhad University of Medical Science, Mashhad, Iran
,
Zahra Ayati
1  Biotechnology Research Center, Nanotechnology Research Center, School of Pharmacy, Mashhad University of Medical Science, Mashhad, Iran
,
Mahmoud R. Jaafari
1  Biotechnology Research Center, Nanotechnology Research Center, School of Pharmacy, Mashhad University of Medical Science, Mashhad, Iran
› Author Affiliations
Further Information

Publication History

received 23 July 2012
revised 02 February 2013

accepted 21 February 2013

Publication Date:
28 March 2013 (online)

Abstract

Crocin is a pharmacologically active component of Crocus sativus. It is an unusual water-soluble carotenoid responsible for the red color of saffron. In various studies, the anticancer effect of saffron and its constituents has been established. Polyethylene glycolated nanoliposomes with a size range up to 200 nm are suitable for encapsulation of cytotoxic drugs and can target tumors passively through the enhanced permeation and retention effect. The aim of this study was to develop a nanoliposomal formulation containing crocin with a higher therapeutic index for the treatment of cancer. Four formulations of polyethylene glycolated nanoliposomes containing 25 mg/ml crocin were prepared with hydrogenated soy phosphatidylcholine, cholesterol, and methoxy-polyethylene glycol (MW 2000)-distearoylphosphatidylcholine at different molar ratios by a solvent evaporation method plus extrusion. Then the liposomes were characterized for their size, zeta potential, crocin encapsulation, release properties, and in vitro cytotoxicity against C26 colon carcinoma cells. Based on in vitro results, the best formulation was selected for an in vivo study, and its antitumor activity was evaluated in BALB/c mice bearing C26 colon carcinoma. The IC50 of crocin itself against C26 colon carcinoma was 0.73 mM. The characterization of the best formulation was as follow: Z-average size: 127.6 ± 1.5 nm; polydispersity index: 0.087 ± 0.018; zeta potential: − 21.7 mV ± 6.7; % encapsulation: 84.62 ± 0.59; % release after 168 hours in RPMI 1640 containing 30 % FBS: 16.26 ± 0.01 %. Liposomal crocin at doses of 50 and 100 mg/kg significantly decreased tumor size and increased survival rate compared with PBS and crocin in buffer (100 mg/kg) groups. The results of this study indicated that liposomal encapsulation of crocin could increase its antitumorigenic activity. Thus, to obtain an optimal dose for use in humans, the formulation merits further investigation.

Supporting Information