J Therm Anal Calorim (2016) 123:2283–2290
DOI 10.1007/s10973-015-4935-z
The effect of Pluronic F127 on the physicochemical properties
and dissolution profile of lovastatin solid dispersions
Bo_zena Karolewicz1 • Maciej Gajda1 • Janusz Pluta1 • Agata Górniak2
Received: 28 April 2015 / Accepted: 16 July 2015 / Published online: 26 July 2015
 Akadémiai Kiadó, Budapest, Hungary 2015
Abstract Lovastatin (LOV) is a BCS class II drug and
hence has poor water solubility, due to which its rate of
solubilization is low. The objective of this study was to
improve the dissolution rate of LOV by preparing, using the
kneading method, solid dispersions with Pluronic F127
(PLU) as a carrier. LOV/PLU solid dispersions were char-
acterized by means of differential scanning calorimetry
(DSC), Fourier transform infrared spectroscopy (FTIR),
X-ray powder diffractometry (XRPD), and in vitro dissolu-
tion tests. The DSC investigation revealed that LOV and
PLU form a simple eutectic system containing 6.0 % w/w of
LOV at the eutectic point. FTIR spectroscopy and XRPD
studies indicated no interaction between LOV and PLU in
the solid state. The intrinsic dissolution rate and in vitro
release into a hard gelatin capsule of LOV from solid dis-
persions was compared to pure LOV. The dissolution rate of
LOV reached within 24 h was improved among all solid
dispersions with PLU. The intrinsic dissolution rate in pH 7.0
phosphate buffer with 0.5 % sodium lauryl sulfate of LOV in
solid dispersion containing the substance by mass percentage
of 60, 70 and 80 % w/w increased more than 30-fold. While
within 24 h 16.53 % of the pure drug was dissolved, 100 %
of the drug was dissolved with the formulations containing
50–80 % w/w of LOV within 240 min. The dissolution rate
of LOV from solid dispersions 50/50 LOV/PLU, 60/40 LOV/
PLU, 70/30 LOV/PLU and 80/20 LOV/PLU percent,
& Bo_zena Karolewicz
bozena.karolewicz@umed.wroc.pl
1 the substance is still poorly wetted [6]. Solid dispersions
Department of Drug Form Technology, Wroclaw Medical
University, Borowska 211A, 50-556 Wroclaw, Poland
2 (within the solid solution) with maximizing the surface area of
Laboratory of Elemental Analysis and Structural Research,
Wroclaw Medical University, Borowska 211A,
50-556 Wroclaw, Poland
respectively, into a hard gelatin capsule was higher (100.0,
83.37, 98.95 and 87.50 %, respectively) than that of pure
LOV (71.15 %) within 30 min.
Keywords Lovastatin
Pluronic F127
Solid dispersion

DSC
Phase diagram
Intrinsic dissolution rate
Introduction
Several reports in the literature indicate the importance of the
substance dissolution process for its absorption from the
gastrointestinal tract and its later therapeutic efficiency. The
low aqueous solubility of LOV (4 9 10-4 mg mL-1), in
addition to its first pass metabolism, results in a low oral
bioavailability (less than 5 %) [1]. Achieving the high disso-
lution rate of lipophilic drugs such as LOV is a key aim in the
development of formulations with rapid dissolution and
improved bioavailability, as they will simultaneously improve
patient compliance and ultimately reduce the total therapeutic
dose of the drug. Various techniques have been applied when
attempting to improve LOV dissolution rate [2], including
obtaining solid lipid nanoparticles [3], liquisolid systems [4],
self-microemulsifying drug delivery systems [1, 5], the for-
mation of water soluble complexes and other methods by the
use of superdisintegrants [6], solid dispersions [7, 8], surfac-
tants [9] and particle size reduction [10]. The release of LOV
from solid dosage forms can be enhanced by the addition of
suitable super disintegrants; however, this does not improve
its solubility and does not decrease the size of the particles, so
combine the benefits of a local increase in the solubility
the compound that comes into contact with the dissolution
medium as the carrier dissolves [6].
123
2284
There are a number of carriers used in the preparation of
LOV solid dispersions like as polymers such as Poloxamer
F-68 [11], polyethylene glycol 4000 and 6000 (PEG 4000,
PEG 6000), polyvinylpyrrolidone K30 (PVP K30) [7], sodium
starch glycolate, croscarmellose sodium, crospovidone
[6, 12], surfactants, or others, e.g., water/tertiary butyl alcohol
(TBA) with mannitol [13].
The in vitro LOV release from tablets containing solid
dispersion prepared by solvent evaporation method using
Poloxamer F-68 showed a faster release of the substance in
comparison to tablets with pure drug and marketed formu-
lations [11]. Patel et al. used a modified locust bean gum to
prepare LOV solid dispersions and achieved an enhance-
ment in the dissolution rate of substance. An in vivo study of
the inhibition activity of 3-hydroxy-3-methyl-glutaryl-
coenzyme A reductase showed a significant reduction in its
activity in the case of solid dispersions of LOV [8]. Solid
dispersions were also prepared by using PEG 4000 and PVP
K30 through a fusion-cooling and solvent evaporation
technique. Tablets containing these solid dispersions showed
a significant improvement in the release profile of LOV
compared with tablets containing LOV without polymers
[7]. Raja Rajeswari et al., using the hot melt extrusion
technique, prepared LOV solid dispersions with Soluplus
(polyvinyl caprolactam-polyvinyl acetate-polyethylene gly-
col graft copolymer) where the drug was in an amorphous
state in the molten polymer. All the formulations showed a
marked increase in the drug release when there was an
increase in the concentration of Soluplus [9]. In studies by
Verma et al. [13], an increase in the solubility and dissolu-
tion rate was obtained for solid dispersion (7:5 ratio of TBA/
water) prepared by freeze–dried method due to the conver-
sion of the crystalline nature of the drug an amorphous one,
as well as a decrease in the particle size of the drug.
Pluronic F127, also known as Poloxamer 407, belongs to
the category of nonionic surface-active triblock copolymer
consisting of a central hydrophobic block of polypropylene
glycol flanked by two hydrophilic blocks of polyethylene
glycol. This polymer is exploited in drug form technology
as emulsifier, solubilizer and wetting agent for poor water-
soluble drugs. Drugs from II BSC class may be solubilized
with a core of micelle or conjugated to the micelle-forming
polymers which lead to an increase in dissolution of these
substances [14].
The present study examines LOV–PLU solid dispersions
prepared in 10/90, 20/80, 30/70, 40/60, 50/50, 60/40, 70/30,
80/20 and 90/10 mass ratios by kneading method. To
investigate the properties of the obtained series of solid
dispersions of LOV–PLU, differential scanning calorimetry
(DSC), X-ray powder diffraction (XRD) and Fourier trans-
form infrared spectroscopy (FTIR) methods were employed.
Intrinsic dissolution studies of LOV from obtained solid
dispersions and the release substance from solid dispersions
123
B. Karolewicz et al.
in hard gelatin capsule were performed in pH 7.0 phosphate
buffer with 0.5 % SLS and compared with pure LOV.
Experimental
Materials
Samples of LOV (99 % purity) was obtained as a gift from
Polpharma S.A. (Poland). PLU was supplied from Sigma-
Aldrich (USA). Sodium lauryl sulfate (SLS) was purchased
from P.P.H. ‘‘Stanlab’’ (Poland). Ethanol and acetonitrile
HPLC grade were obtained from Fluka Biochemica (Ger-
many). Phosphoric acid was purchased from Fluka Bio-
chemica (Germany). Sodium hydrogen phosphate,
potassium dihydrogen phosphate, and phosphoric acid
were purchased from Chempur (Poland).
Preparation of solid dispersion
Accurately weighed amounts of LOV were mixed with
different concentrations of in agate mortar, while a suffi-
cient volume of ethanol was added to achieve a consistency
like slurry. The solvent was then completely evaporated at
40–45 C while being continuously stirred to obtain a dry
mass. The obtained solid dispersions were pulverized
powders, sieved using a 315-lm sieve and then stored in a
desiccator at room temperature until use. The mass ratios
of the LOV/PLU mixtures were 90/10, 80/20, 70/30, 60/30,
50/50, 40/60, 30/70, 20/80 and 10/90 percent, respectively.
Drug content
The equivalent mass of solid dispersions containing 10 mg
of LOV was weighed accurately and dissolved in 10 mL of
acetonitrile. The solution was filtered, and LOV content
was analyzed by HPLC.
Differential scanning calorimetry (DSC)
The DSC curves of each mixture were obtained using a
differential scanning calorimeter (Mettler Toledo DSC 25)
equipped with a heat flow sensor and joined via an inter-
face TA Controller TC 15 to a computer. Measurements
were recorded by STARe software. Samples for DSC
measurements were sealed in 40 lL standard aluminum
crucibles with a single hole punched in the lid. An empty
pan of the same type was employed as a reference. The
DSC instrument was calibrated using the melting point of
indium (156.6 ± 0.3 C) as a standard. DSC scans of each
mixture were performed at a heating rate of 5 C min-1 at
a temperature range of 25 to 190 C. The DSC cell was
purged with a stream of dry argon at a rate of
The effect of Pluronic F127 on the physicochemical properties and dissolution profile of… 2285

50 mL min-1. Experiments were performed in triplicate,
and the mean values were calculated.
Powder X-ray diffraction analysis (XRPD)
Powder X-ray diffraction patterns were recorded on a
powder diffractometer (D2 Phaser, Bruker) with CuKa
radiation with LYNXEYE detector. The degree of
diffractions was measured at 15 min-1 between 5 and
40 (2h) with an accuracy of 0.02 throughout the mea-
surement range, at 0.5 s/step.
performed using an HPLC system (System GOLD 126,
Beckman Coulter) with a UV–VIS detector. The analysis
was carried out with the use of Zorbax SB-C8
(250 9 4.6 mm, 5 lm, Agilent). An HPLC analysis was
performed by gradient elution with a flow rate of
1.5 mL min-1. The mobile phase composition was ace-
tonitrile–water with 0.1 % phosphoric acid [15]. Substances
eluted from the column were identified by a UV visible
detector at 238 nm. External standards of LOV were used to
obtain calibration curves. The linear correlation coefficient
(r2) was greater than 0.99 in the range of 5–285 lg mL-1.

Fourier transform infrared spectroscopy (FTIR) In vitro of LOV dissolving into hard gelatin capsule

FTIR spectra were registered by using a Spectrum Two
spectrophotometer (PerkinElmer) with a UATR accessory
attached. The scanning range was 4000–450 cm-1. The
spectral resolution for all step-scan FTIR measurements
was 4 cm-1.
Dissolution studies
Release studies were carried out in triplicate in USP
Apparatus 2 (Basket type). Solid dispersions equivalent to
40 mg of drug in gelatin capsules were added to 500 mL of
pH 7.0 phosphate buffer with 0.5 % SLS stirred at 75 rpm.
Aliquots of 3 mL were withdrawn at specified time inter-
vals and analyzed by HPLC at 238 nm.

Intrinsic dissolution (IDR) studies Results and discussion

The dissolution test was conducted under sink conditions in Drug content
1000 mL of pH 7.0 phosphate buffer with 0.5 % SLS at
37 ± 0.5 C and rotational speeds of 50 rpm. The disso- The LOV content of the formulations was found to be in
lution system was fitted with SR8-PLUS (Hanson) and a the range of 99.21 % to 102.55 % of the declared amount.
7-channel peristaltic pump. LOV (100.0 mg) or an equiv-
alent amount of solid dispersion disks was prepared by Differential scanning calorimetry study
compressing powder in hydraulic press (Specac, Mettler
Toledo) for 1 min under a 1t compression force, using a The DSC curves of pure components, obtained at a heating
8-mm punch. Samples were withdrawn at appropriate time rate of 5 C min-1 in the temperature range from 25 to
intervals. The quantitative determination for LOV was 190 C, are presented in Fig. 1. The DSC curve of pure
Fig. 1 DSC curves of pure
LOV and PLU ^Exo

LOVASTATIN
Integral –512.94 mJ
Normalized –104.68 Jg^–1
Peak 171.75 °C

20 PLURONIC F127
mW
Integral –1606.00 mJ
Normalized –176.29 Jg^–1
Peak 53.42 °C

40 60 80 100 120 140 160 180 °C

0 2 4 6 8 10 12 14 16 18 20 22 24 26 28 30 min

123
2286 B. Karolewicz et al.

LOV shows only one endothermic peak corresponding to
the melting of the drug at 171.8 C, which corresponds
with the data presented by Yoshida et al. [16]. Similarly,
the DSC curve of PLU, presented in the same figure, shows
one endothermic effect, associated with its melting at
53.4 C. This confirms that under these conditions both
components are stable and do not decompose.
Figure 2 shows the phase diagram of the examined
system constructed on the basis of the DSC results. The
DSC curves of obtained dispersions (Fig. 3) clearly indi-
cate that the investigated compounds formed a simple
binary eutectic system—only two kinds of thermal effects
are shown for the whole range of compositions. The onset
of the first peak consistently appeared near 48.0 C
(Fig. 3), indicating a eutectic reaction: solid lovastatin
(LOV) ? solid Pluronic F127 (PLU) = liquid (L). The
second peak (the temperature of liquid) was generally
wider, indicating that the complete melting took place over
a temperature range. Terminal solid solutions were not
observed at either sides of the phase diagram. The melting
points of the pure components (LOV: 171.8 C, PLU:
53.4 C) were depressed due to the existence of the other
component in the mixture as shown in the phase diagram in
Fig. 2. The values of the eutectic melting enthalpy DH for a
given dispersion, determined by integration of the eutectic
peak area on DSC curves, are plotted in Fig. 4 versus mass
fraction of LOV (Tamman’s triangle construction [17]).
The thermal effect of the eutectic transition goes to zero for
a composition corresponding to pure LOV. This confirms
that there is no mutual miscibility in the solid state and no
formation of a terminal solid solution. The values of the

200.0

180.0
200.0
160.0
180.0
L 140.0
160.0
120.0
ΔT/J g–1

140.0
100.0
120.0
T/°C

80.0
L + LOV
100.0 60.0
80.0 40.0

60.0 20.0

40.0 0.0
0.00 10.00 20.00 30.00 40.00 50.00 60.00 70.00 80.00 90.00 100.00
20.0 PLU + L PLU + LOV LOV/mass%

0.0 10.0 20.0 30.0 40.0 50.0 60.0 70.0 80.0 90.0 100.0 Fig. 4 Determination of the eutectic composition in the LOV–PLU
PLU LOV/mass% LOV system by Tamman’s triangle construction for the eutectic melting
enthalpy DH at 48.0 C (filled triangles a) and by plotting noneutectic
Fig. 2 Phase diagram of the LOV–PLU system melting enthalpy versus mass ratio of LOV (filled circles)

Fig. 3 DSC curves of obtained

LOV/PLU solid dispersions 10/90 %w/w LOV/PLU
20/80 %w/w LOV/PLU
30/70 %w/w LOV/PLU
40/60 %w/w LOV/PLU
50/50 %w/w LOV/PLU
60/40 %w/w LOV/PLU
70/30 %w/w LOV/PLU
80/20 %w/w LOV/PLU
90/10 %w/w LOV/PLU
2
–1
Wg^

^Exo 40 60 80 100 120 140 160 180 °C

123
The effect of Pluronic F127 on the physicochemical properties and dissolution profile of… 2287

eutectic melting enthalpy DH (Fig. 4, filled triangles) • Eutectic composition: mass fraction of LOV 6.0 %,
increase linearly with the content of PLU. Near the eutectic mass fraction of PLU 94.0 %;
point, the DSC scans showed a characteristic overlap of • Eutectic temperature: 48.0 C.
two endotherms (eutectic and liquid events) into a single
peak. Because of this, the eutectic composition was
X-ray diffraction
determined by plotting the non-eutectic melting enthalpy
(after the eutectic melting) of LOV as a function of the
The X-ray diffraction patterns of pure LOV, PLU and solid
mass percentage of the drug and extrapolating the fitted
dispersions are presented in Fig. 5. The XRD patterns of
line to zero enthalpy (Fig. 4, filled circles). Finally, the
pure LOV showed a series of peaks, which are character-
parameters of the eutectic point (E) have been established
istic of a crystalline compound at diffraction angles (2h) at
as follows:
6.80, 8.19, 8.86, 9.75, 14.06, 14.38, 14.83, 15.43,
16.28, 16.69, 17.76, 18.87, 20.86, 21.20, 21.87,
23.10 and 26.95. The X-ray diffractograms of pure PLU
show distinct peaks at 18.87 band 23.10. Drug crys-
(k)
tallinity peaks were also detectable in obtained solid dis-
(j)
persions. The diffraction patterns of solid dispersions
(i)
showed the presence of characteristic diffraction peaks of
(h)
Intensity/a.u.

both the drug and polymer, indicating that LOV was pre-
(g)
(f)
sent as a crystalline material and suggesting that these are
(e)
simple mixtures of drug and carrier without any chemical
(d) interaction between the components.
(c)
(b)
(a) Fourier transform infrared spectroscopy
5 10 15 20 25 30 35 40
2θ /° Figure 6 shows FTIR spectra of PLU, LOV and its solid
dispersions. The spectra of the pure drug presented, simi-
Fig. 5 XRPD patterns of: LOV (a), 90/10 % w/w LOV/PLU (b), larly to that found in works [1, 18], characteristic peaks at
80/20 % w/w LOV/PLU (c), 70/30 % w/w LOV/PLU (d), 60/40 % 3539 cm-1 (alcohol OH stretching vibration), at
w/w LOV/PLU (e), 50/50 % w/w LOV/PLU (f), 40/60 % w/w LOV/
PLU (g), 30/70 % w/w LOV/PLU (h), 20/80 % w/w LOV/PLU (i), 3016 cm-1 (olefinic CH stretching vibration), at
10/90 % w/w LOV/PLU (j), PLU (k) 2965 cm-1 (methyl C–H asymmetric stretching), at

Fig. 6 FTIR spectra of: LOV

(a), 90/10 % w/w LOV/PLU (k)
(b), 80/20 % w/w LOV/PLU
(j)
(c), 70/30 % w/w LOV/PLU
(d), 60/40 % w/w LOV/PLU (i)
(e), 50/50 % w/w LOV/PLU (f),
40/60 % w/w LOV/PLU (g), (h)
30/70 % w/w LOV/PLU (h),
(g)
20/80 % w/w LOV/PLU (i),
10/90 % w/w LOV/PLU (j), (f)
PLU (k)
(e)

(d)

(c)

(b)

(a)

4000 3700 3400 3100 2800 2500 2200 1900 1600 1300 1000 700 400
Wavenumber/cm–1

123
2288 B. Karolewicz et al.

2929 cm-1 (methylene C–H asymmetric stretching), at Dissolution studies

2865 cm-1 (methyl and methylene CH asymmetric
stretching vibration), at 1724, 1710 and 1698 cm-1 (lac- The maximum concentration of dissolved LOV reached
tone and ester carbonyl stretch) and at 871 cm-1 (trisub- within 24 h was enhanced for solid dispersions containing
stituted olefinic CH). The FTIR spectrum of PLU is 80/20, 70/30, 60/40, 50/50, 40/60, 30/70 and 20/80 % w/w.
characterized by principal absorption peaks at 2882 cm-1 However, the initial release rate is enhanced for all solid
(C–H stretch aliphatic), 1342 cm-1 (in-plane O–H bend), dispersions, and the saturation level was reached within
1279 cm-1 (CH2 bending) and 1100 cm-1 (C–O stretch), 240 min of the dissolution process for solid dispersions
which were consistent in all binary systems with the drug. 60/40, 70/30 and 80/20 % w/w (see Figs. 7, 8). In Table 1,
This indicates the absence of drug–polymer interactions, as the intrinsic dissolution rate (IDR) of the pure drug and
all the specific peaks of drug were present in the solid solid dispersions LOV/PLU in pH 7.0 phosphate buffer with
dispersion. 0.5 % SLS were collected. Kaplan [19] noted that com-
pounds with an IDR below 0.1 mg cm-2 min-1 usually
exhibited a dissolution rate-limited absorption. The IDR of
pure LOV of 0.023 mg cm-2 min-1 falls into this category.
The intrinsic dissolution rate of LOV in a solid dispersion
110
containing the substance by mass percentage of 60, 70 and
100 80 % w/w increased more than 30-fold. After 240 min of
90 the test, more than 99 % of LOV was released from the
80 10/90LOV/PLU solid dispersion containing 60–80 % w/w of LOV, when at
Drug dissolved/%

20/80LOV/PLU
70 30/70LOV/PLU this time only 1.40 % of pure LOV had been dissolved.
60 40/60LOV/PLU
50/50LOV/PLU
In vitro results of LOV dissolving into a hard gelatin
50 60/40LOV/PLU capsule in pH 7.0 phosphate buffer with 0.5 % SLS are
40 70/30LOV/PLU
80/20LOV/PLU reported in Table 2. The graphical presentation of the
30 90/10LOV/PLU
dissolution profile into hard gelatin capsules of pure LOV,
20 LOV

10
and LOV/PLU solid dispersions over a period of 120 min
0 is shown in Fig. 9. The dissolution rate of LOV from solid
0 2 4 6 8 10 12 14 16 18 20 22 24 dispersions 50/50 LOV/PLU, 60/40 LOV/PLU, 70/30
t /h LOV/PLU and 80/20 LOV/PLU was higher (100.0, 83.37,
Fig. 7 Dissolution profiles of LOV and its solid dispersions with
98.95 and 87.50 %, respectively) than that of pure LOV
PLU within 24 h of dissolution process (71.15 %) within 30 min.

Fig. 8 Dissolved amount of

LOV from solid dispersions 210
Dissolved amount of LOV/mg 0.5 cm–2

180

10/90LOV/PLU
150 20/80LOV/PLU
30/70LOV/PLU
40/60LOV/PLU
120
50/50LOV/PLU
60/40LOV/PLU
90 70/30LOV/PLU
80/20LOV/PLU
90/10LOV/PLU
60
LOV

30

0
0 120 240 360 480 600 720 840 960 1080 1200 1320 1440
t /min

123
The effect of Pluronic F127 on the physicochemical properties and dissolution profile of… 2289

Table 1 Intrinsic dissolution rate (IDR) of pure LOV and prepared solid dispersions and corresponding ratios. Data are expressed as
mean ± SD (n = 3)
Dispersion code IDR/mg cm-2 min-1 r2 IDR ratio SDs/LOV

10/90 LOV/PLU 0.069 ± 0.0012 0.9989 2.97

20/80 LOV/PLU 0.162 ± 0.0014 0.9974 6.98
30/70 LOV/PLU 0.245 ± 0.0061 0.9988 10.56
40/60 LOV/PLU 0.284 ± 0.0002 0.9881 12.28
50/50 LOV/PLU 0.547 ± 0.0061 0.9996 23.63
60/40 LOV/PLU 0.824 ± 0.0265 0.9977 35.58
70/30 LOV/PLU 0.836 ± 0.0049 0.9917 36.12
80/20 LOV/PLU 0.853 ± 0.0022 0.9633 36.82
90/10 LOV/PLU 0.111 ± 0.0161 0.8147 4.80
Pure LOV 0.023 ± 0.0004 0.9995 –

Table 2 Percentage of lovastatin dissolved within 60 min

Dispersion code Q5min Q30min Q60min

10/90 LOV/PLU 0.71 ± 0.26 1.30 ± 1.99 11.75 ± 5.39

20/80 LOV/PLU 0.04 ± 0.02 2.15 ± 0.53 21.75 ± 3.82
30/70 LOV/PLU 2.47 ± 1.70 79.64 ± 6.30 99.36 ± 3.19
40/60 LOV/PLU 0.77 ± 0.71 10.13 ± 9.15 90.63 ± 8.26
50/50 LOV/PLU 25.42 ± 9.96 100.32 ± 7.12 100.57 ± 0.46
60/40 LOV/PLU 0.25 ± 0.07 83.37 ± 15.94 100.75 ± 5.49
70/30 LOV/PLU 16.67 ± 9.32 98.95 ± 7.46 100.08 ± 5.515
80/20 LOV/PLU 1.127 ± 0.17 87.50 ± 0.60 97.20 ± 1.25
90/10 LOV/PLU 0.63 ± 0.53 70.95 ± 5.34 96.66 ± 0.38
Pure LOV 2.22 4 ± 0.39 71.15 ± 7.30 96.51 ± 2.11
Q5min, Q30min and Q60min values (percent drug dissolved within 5, 30 and 60 min, respectively). Mean ± SD, n = 3

110 Conclusions
100
90 The presented DSC studies demonstrate that LOV and PLU
Cululative drug release/%

10/90LOV/PLU
80 20/80LOV/PLU formed a simple eutectic phase diagram. The FTIR spec-
70 30/70LOV/PLU
40/60LOV/PLU
troscopy and XRPD studies of the obtained dispersions
60
50/50LOV/PLU showed no interaction between the components in the solid
50
60/40LOV/PLU state and confirmed the absence of terminal solid solutions.
40 70/30LOV/PLU
30
Our study demonstrates the successful application of
80/20LOV/PLU

20 90/10LOV/PLU
PLU for the dissolution enhancement of the poorly water-
10 LOV soluble drug LOV. The dissolution rate of LOV was
0 enhanced for all investigated dispersions. It was shown that
0 20 40 60 80 100 120
the release profile of the solid dispersions is strongly
t /min dependent on the content of the polymeric carrier. How-
Fig. 9 Lovastatin dissolving from solid dispersions contained into ever, the initial release rate from solid dispersions con-
hard gelatin capsules within 120 min taining 50–80 % w/w LOV was drastically increased due to

123
2290
a large dissolution rate in these formulations. The results of
this work suggest that the use of PLU as a polymer carrier
for LOV in solid dispersions, as in the case of simvastatin
[20], could be a promising approach to improve its release
from oral form and hence may affect its absorption rate.
Acknowledgements The authors would like to thank Polpharma S.
A. for providing lovastatin.
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