development of new polymeric nanoparticles containing

DEVELOPMENT OF NEW POLYMERIC NANOPARTICLES CONTAINING
SHEA BUTTER FOR DRUG DELIVERY
SILVEIRA, F.1; BONINI, M.B.1; SAURIN, S.2; JORNADA, D.S.3.; POHLMANN, A.R.3,4; GUTERRES, S.S.3;
CRUZ, L5; SCHAFFAZICK, S. R5*.
1
Curso de Farmácia, UFSM, Santa Maria, RS, Brazil – [email protected]; 2PPG Ciências
Farmacêuticas, UFSM, Santa Maria, RS, Brazil; 3Faculdade de Farmácia, UFRGS, Porto Alegre-RS, Brazil.;4
Instituto de Química, UFRGS, Porto Alegre-RS, Brazil; 5Departamento de Farmácia Industrial, Centro de Ciências
da Saúde, Universidade Federal de Santa Maria, Santa Maria-RS, Brazil – [email protected].
Keywords: polymeric nanoparticles, lipid nanoparticles, shea butter, drug delivery, idebenone.
1. Introduction
The interest in nanoparticulate systems (polymeric or
lipid) for controlling release of drug has been
growing in pharmaceutical fiel. Polymeric
nanoparticles including nanocapsules (oil core
surrounded by a polymeric wall) and nanospheres
(polymeric matrix). Lipid nanoparticles are solid lipid
matrices. Cacao1 and cupuaçu2 butters have been
employed to prepare solid lipid nanoparticles.
In this way, the present study reports the
development of a new drug delivery system based on
both
polymer
(Eudragit
RS
100
or
polycaprolactone) and solid lipid (shea butter)
components. The ability of theses systems to
encapsulate a lipophilic drug was also evaluated,
employing idebenone as model.
2. Methods
The nanoparticle suspensions were prepared by
Interfacial deposition of preformed polymer
method[3], using Eudragit RS100 [RS: poly (ethyl
acrylate-co-methyl
methacrylate-co-methacrylate
chloride
trimetilamonioetila)
1:2:0,1]
or
polycaprolactone (PCL) as polymer, shea butter (SB)
as lipid (instead of oil), sorbitan monooleate and
polysorbate 80 as surfactants. Suspensions containing
1 mg/mL of idebenone as also prepared. The mean
particle sizes, polydispersity index (PDI) and zeta
potentials (ZP; 10 mM NaCl) were measured using
Zetasizer Nano Series (Malvern). Idebenone was
assayed by HPLC[4] and its encapsulation efficiency
was calculated from the difference between the total
and free drug concentrations, using ultrafiltrationcentrifugation (Amicon, Millipore, 2.200 x g/10 min).
3. Results
All
formulations
presented
macroscopic
homogeneous aspect, colloidal sizes and low PDI
(Table 1). The nanoparticles prepared only with shea
butter (SB) presented lower size than formulations
containing also PCL (PCL/SB) and similar negative
zeta potential values. On the other hands, the
nanoparticles prepared with Eudragit RS (cationic
polymer) and shea butter (RS-SB) presented positive
zeta potential values and lower size than SB
formulations. These results show that probably shea
butter is contained in the core of Eudragit RS
nanoparticles.
Table 1. Physicochemical characteristics of
nanoparticle suspensions (n=2).
pH
RSSB 6,61±1,28
PCLSB 6,24±0,09
SB 6,22±0,22
Size (nm)
PDI
ZP (mV)
156 ± 12
0,15 ± 0,01
+8 ± 0,2
267 ± 76
182 ± 1
0,22 ± 0,06
0,12 ± 0,02
-11 ± 1,4
-11 ± 1,0
After, idebenone was incorporated in the new
systems developed. Hence, it is possible to prepare
idebenone-loaded PCL nanoparticles containing shea
butter (size= 253 nm; PDI = 0,244; ZP= -13 mV;
drug content= 0,97 mg/mL) with encapsulation
efficiency close to 100 %. Besides, idebenone-loaded
Eudragit® RS nanoparticle containing shea butter
(size= 181 nm; PDI = 0,19; ZP= +7 mV) also
presented high encapsulation efficiency (97,3 %), but
low total content (0,83 mg/mL) in comparison to the
theoretical value (1,0 mg/mL).
4. Conclusion
It was possible to prepare innovative nanoparticles
containing a polymer (Eudragit RS100 or
polycaprolactone)
and
shea
butter.
The
polycaprolactone/shea butter nanoparticles were able
to efficiently encapsulate a model drug (idebenone)
and
presented
suitable
physicochemical
characteristics. Further studies will be necessary to
confirm if the butter is at the core of the polymeric
nanoparticles.
Acknowledgments
We thank financial support received from FIPE –
Enxoval/UFSM, Programa FIT/UFSM and Programa
FIPE Júnior/UFSM.
References
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