Colloids and Surfaces B: Biointerfaces 147 (2016) 258–264
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Colloids and Surfaces B: Biointerfaces
jo ur nal ho me p ag e: www.elsevier.com/locate/colsurfb
Antisolvent precipitation technique: A very promising approach to
crystallize curcumin in presence of polyvinyl pyrrolidon for solubility
and dissolution enhancement
Fatemeh Sadeghi
a,b
, Mohammad Ashofteh
b
, Alireza Homayouni
c
,
Mohammadreza Abbaspour
a,b
, Ali Nokhodchi
d,e,∗
, Hadi Afrasiabi Garekani
f,b,∗∗
a
Targeted Drug Delivery Research Center, Mashhad University of Medical Sciences, Mashhad, Iran
b
Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
c
School of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran
d
Pharmaceutics Research Laboratory, Arundel Building, School of Life Sciences, University of Sussex, Brighton, BN1 9QJ, UK
e
Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
f
Pharmaceutical research center, Mashhad University of Medical Sciences, Mashhad, Iran
a r t i c l e i n f o
Article history:
Received 23 May 2016
Received in revised form 1 August 2016
Accepted 3 August 2016
Available online 6 August 2016
Keywords:
Curcumin
Antisolvent crystallization
PVP
Dissolution
Solubility
Amorphous
a b s t r a c t
Curcumin with a vast number of pharmacological activities is a poorly water soluble drug which its
oral bioavailability is profoundly limited by its dissolution or solubility in GI tract. Curcumin could be
a good anticancer drug if its solubility could be increased. Therefore, the aim of the present study was
to increase the dissolution rate of curcumin by employing antisolvent crystallization technique and to
investigate the effect of polyvinyl pyrrolidone K30 (PVP) as colloidal particles in crystallization medium on
resultant particles. Curcumin was crystalized in the presence of different amounts of PVP by antisolvent
crystallization method and their physical mixtures were prepared for comparison purposes. The samples
were characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-
ray powder diffraction (XRPD) and Fourier transform infrared spectroscopy (FT-IR). The solubility and
dissolution of the treated and untreated curcumin were also determined. Antisolvent crystallization
of curcumin led to the formation of particles with no definite geometric shape. It was interesting to
note that the DSC and XRPD studies indicated the formation of a new polymorph and less crystallinity
for particles crystallized in the absence of PVP. However, the crystallized curcumin in the presence of
PVP was completely amorphous. All crystalized curcumin samples showed much higher dissolution rate
compared to untreated curcumin. The amount of curcumin dissolved within 10 for treated curcumin in the
presence of PVP (1:1 curcumin:PVP) was 7 times higher than untreated curcumin and this enhancement
in the dissolution for curcumin samples crystallized in the absence of PVP was around 5 times. Overall‘
the results of this study showed that antisolvent crystallization method in the absence or presence of
small amounts of PVP is very efficient in increasing the dissolution rate of curcumin to achieve better
efficiency for curcumin.
© 2016 Elsevier B.V. All rights reserved.
∗
Corresponding authors at: Pharmaceutics Research Laboratory, Arundel Build-
ing, School of Life Sciences, University of Sussex, Brighton, BN1 9QJ, UK.
Tel.: +44 1273 872811.
∗ ∗
Corresponding author at: Pharmaceutical research center, Mashhad University
of Medical Sciences, Mashhad, Iran
E-mail addresses: a.nokhodchi@sussex.ac.uk (A. Nokhodchi),
afrasiabih@mums.ac.ir (H.A. Garekani).
1. Introduction
There are lots of techniques that have been used to enhance
the dissolution rate or solubility of poorly water-soluble drugs [1].
Crystal engineering or crystal manipulation has been the focus of
many research activities to achieve this goal during the past few
years. Crystal manipulation has been performed by either top-
down or bottom-up techniques [2,3,4].
Top-down procedures involve the breaking of drug particles by
milling and/or homogenization while bottom-up methods involve
the building up particles from drug molecules via precipitation
http://dx.doi.org/10.1016/j.colsurfb.2016.08.004
0927-7765/© 2016 Elsevier B.V. All rights reserved.