Electrospun nanofibers of polyCD/PMAA polymers and their potential
application as drug delivery system
Michele F. Oliveira
a
, Diego Suarez
a
, Júlio Cézar Barbosa Rocha
b
, Alvaro Vianna Novaes de Carvalho Teixeira
b
,
Maria E. Cortés
c
, Frederico B. De Sousa
d,
⁎, Rubén D. Sinisterra
a
a
Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Minas Gerais (UFMG), Belo Horizonte, 31270-901 MG, Brazil
b
Departamento de Física, Centro de Ciências Exatas e Tecnológicas, Universidade Federal de Viçosa (UFV), Viçosa, 36570-000 MG, Brazil
c
Departamento de Odontologia Restauradora, Faculdade de Odontologia, Universidade Federal de Minas Gerais (UFMG), Belo Horizonte, 31270-901 MG, Brazil
d
Instituto de Física e Química, Universidade Federal de Itajubá (UNIFEI), Itajubá, 37500-903 MG, Brazil
abstract article info
Article history:
Received 18 December 2014
Accepted 21 April 2015
Available online xxxx
Keywords:
Electrospinning
Polymeric nanofibers
Poly-cyclodextrin
Drug delivery system
Propranolol
Herein, we used an electrospinning process to develop highly efficacious and hydrophobic coaxial nanofibers
based on poly-cyclodextrin (polyCD) associated with poly(methacrylic acid) (PMAA) that combines polymeric
and supramolecular features for modulating the release of the hydrophilic drug, propranolol hydrochloride
(PROP). For this purpose, polyCD was synthesized and characterized, and its biocompatibility was assessed
using fibroblast cytotoxicity tests. Moreover, the interactions between the guest PROP molecule and both polyCD
and βCD were found to be spontaneous. Subsequently, PROP was encapsulated in uniaxial and coaxial polyCD/
PMAA nanofibers. A lower PROP burst effect (reduction of approximately 50%) and higher modulation were ob-
served from the coaxial than from the uniaxial fibers. Thus, the coaxial nanofibers could potentially be a useful
strategy for developing a controlled release system for hydrophilic molecules.
© 2015 Elsevier B.V. All rights reserved.
1. Introduction
Technologies associated with the development of drug delivery sys-
tems (DDS) have significantly increased in recent decades [1,2]. DDS
based on polymers have been widely used due to their considerable
therapeutic efficacy and low side effects [3]. The fusion between
polymer science and innovative processing techniques has led to new
architectures with desired hierarchical structures and multiple func-
tionalities for biomedical applications [4,5]. In this sense, polymer fibers
have attracted great interest, including for use as DDS, due to their typ-
ical properties, e.g. , large surface area-to-volume ratio and possible sur-
face modifications [6–8]. Moreover, drugs loaded in polymeric fibers
can provide systemic and locoregional therapies compared with other
DDS, such as nanoparticles, nanocapsules or micellar systems, which
have intrinsic fluidity and are difficult to keep localized in a specific
area of the body [9,10].
Electrospinning is a simple and versatile technique that is capable of
manufacturing continuous fibers with diameters ranging from micro-
meters down to several nanometers by applying strong electric fields,
and this technique can be a useful alternative for pharmaceutical appli-
cations in which drugs incorporated in a polymeric solution or melt are
used [11–13]. Fibers produced by electrospinning can combine different
natural and synthetic polymers, thereby exhibiting distinct and comple-
mentary functions [9,14,15]. Indeed, biocompatible polymers have been
used by the pharmaceutical industry and have been approved by the
FDA, such as polymethacrylates, which are widely applied as film-
coating agents, as well as transdermal films, buccal patches and other
devices [16]. This might be an interesting strategy for producing
electrospun fibers for use as drug delivery systems.
Hence, we are comparing the release of the hydrophilic drug, pro-
pranolol hydrochloride (PROP), using two strategies: using uniaxial fi-
bers and using coaxial fibers which combine poly(methacrylic acid)
(PMMA) and poly-cyclodextrin (polyCD). The latter provides the
host:guest properties, thereby providing many cavities for drug inclu-
sion and polymeric features (high molecular weight) through chemical-
ly linked cyclodextrins (CDs, Fig. 1). Furthermore, CDs have been used to
enhance pharmaceutical properties, leading to a modified solubility, sta-
bility, greater bioavailability and reduction in side effects; therefore, CDs
are promising molecules for constructing advanced delivery systems
[17–19]. Another important role is that the CDs presented in the polymer
main chain can play in this system and this is the potential of CDs
allowing it to be used as a crosslinking agent to improve the hydropho-
bicity of acrylic polymers, according to data reported in the literature [20].
PROP is a nonselective beta-blocker that is primarily used in the
treatment of angina pectoris, cardiac arrhythmias, hypertension and
many other cardiovascular disorders. PROP is well absorbed in the gas-
trointestinal tract, but it has a relatively low oral bioavailability
(15–23%) because of extensive hepatic first-pass metabolism. In
Materials Science and Engineering C xxx (2015) xxx–xxx
⁎ Corresponding author at: Instituto de Física e Química, Universidade Federal de
Itajubá (UNIFEI), Itajubá, 37500-903 MG, Brazil.
E-mail addresses: fredbsousa@gmail.com, fredbsousa@unifei.edu.br (F.B. De Sousa).
MSC-05429; No of Pages 10
http://dx.doi.org/10.1016/j.msec.2015.04.042
0928-4931/© 2015 Elsevier B.V. All rights reserved.
Contents lists available at ScienceDirect
Materials Science and Engineering C
journal homepage: www.elsevier.com/locate/msec
Please cite this article as: M.F. Oliveira, et al., Electrospun nanofibers of polyCD/PMAA polymers and their potential application as drug delivery
system, Mater. Sci. Eng., C (2015), http://dx.doi.org/10.1016/j.msec.2015.04.042