Tablet Formulation Containing Chitosan-Alginate Microparticles: Characterization and Release Profile of Xanthones
Corresponding email: elsakm@che.ui.ac.id
Published at : 27 Nov 2020
Volume : IJtech
Vol 11, No 5 (2020)
DOI : https://doi.org/10.14716/ijtech.v11i5.4338
Krisanti, E.A., Lazuardi, D., Kiresya, K.K., Mulia, K., 2020. Tablet Formulation Containing Chitosan-Alginate Microparticles: Characterization and Release Profile of Xanthones. International Journal of Technology. Volume 11(5), pp. 900-909
| Elsa Anisa Krisanti | Chemical Engineering Department, Faculty of Engineering, Universitas Indonesia, Depok 16424, Indonesia |
| David Lazuardi | Chemical Engineering Department, Faculty of Engineering, Universitas Indonesia, Depok 16424, Indonesia |
| Kianti Kasya Kiresya | Chemical Engineering Department, Faculty of Engineering, Universitas Indonesia, Depok 16424, Indonesia |
| Kamarza Mulia | Chemical Engineering Department, Faculty of Engineering, Universitas Indonesia, Depok 16424, Indonesia |
Mangosteen pericarp extract contains a high amount of
xanthones, which are secondary plant metabolites that exhibit high antioxidant
activities as well as beneficial pharmacological properties, but low
bioavailabilities. In this study, xanthones extracted from the
pericarp of soursop fruit were encapsulated in chitosan-alginate microparticles
by ionic gelation, and the
microparticles were subsequently formulated into
antioxidant supplement tablets by direct compression. One of
the tablet formulations satisfied the requirements for weight and size
uniformity as well as friability, but not hardness. Dissolution test results
revealed similar release profiles characterized by a burst release that occurs
in the first 60 min of immersion in simulated gastrointestinal fluids and a
complete release of xanthones in 120 min. The results obtained herein
demonstrated the potential of the tested tablet formulations for the delivery
of xanthones into the gastrointestinal tract. If a targeted release to a
specific area in the gastrointestinal tract is desirable, the composition of
the excipients in the present formulation should be modified.
Alginate; Chitosan; Mangosteen; Mangostin; Xanthone
od
supplements are food products intended to complement a diet with vitamins,
minerals, or other substances in concentrated amounts that exert physiological
effects (Nicoletti, 2012). Antioxidant compounds present in food
supplements reduce the incidence of chronic diseases caused by free radicals in
the body, such as cancer, brain dysfunction and heart disease. Although
the body can produce antioxidants from cell metabolism, the additional intake
of antioxidants is required as the number of free radicals increases.
Meanwhile, the pericarp of mangosteen fruit (Garcinia
mangostana L.) contains bioactive compounds known as xanthones, which
exhibit high antioxidant activities (Jung et al.,
2006; Palakawong et al., 2010; Chaovanalikit et al., 2012), and ?-mangostin
and ?-mangostin are the main derivatives of xanthones (Al-Massarni
et al., 2013; Mulia et al., 2015). Figure 1 shows their molecular
structures. Mangostins have been reported to exhibit cytotoxic effects,
with the ability to induce the apoptosis of cancer cells and to selectively
kill cancer cells (Pedraza-Chaverri et al., 2008;
Genoux-Bastide et al., 2011).
Owing to its biodegradable, non-toxic and mucoadhesive properties, chitosan is an extensively investigated biopolymer for drug delivery. It has been used in controlled-release oral formulations to increase the bioavailability of easily degraded drugs and bioactive compounds such as antibiotics, anticancer agents, proteins, peptides and vaccines (Sinha et al., 2004).
?-mangostin | ?-mangostin |
Figure
1 Molecular
structures of ?-mangostin and ?-mangostin
Alginate is another biodegradable and non-toxic polymer typically used
in drug formulations and as a food additive (Tonnesen
and Karlsen, 2002). In contrast to chitosan, alginate exhibits
stable properties under an acidic pH in the stomach, while it undergoes
swelling and dissolution at a more neutral pH in the intestine (Kumar et al., 2005). A tablet is the most
commonly used oral formulation for the delivery of drugs into the
gastrointestinal tract, comprising active substances and excipients such as
diluents, binders, lubricants, crushing agents, coatings, flavoring ingredients
and other additives (Ansel et al., 1999).
Direct compression is employed to manufacture tablets via the direct
compression of a mixture of active substances and dry excipients without prior
treatment.
Xanthones, often
reported as a-mangostin,
have been encapsulated in various chitosan-alginate formulations including
powder in a capsule (Peerapattana et al., 2013),
microparticles (Krisanti et al., 2017; Mulia et
al., 2020), effervescent tablets (Widowati
et al., 2013), dispersion in a microgel (Ahmad
et al., 2012), tablets (Tamat et al., 2014),
hydrogel films (Wathoni et al., 2019) and
freeze-dried matrices (Mulia et al., 2019). Recently, the optimization of chitosan-alginate
microparticles by using the Box–Behnken experimental design confirmed that
alginate is a suitable biopolymer to complement chitosan for the delivery of
mangostin to the colon area (Mulia et al., 2020).
For further investigation, tablet formulations of microparticles as an
antioxidant supplement were prepared and tested. In this study, physicochemical
characteristics of tablet formulations of xanthone-loaded chitosan-alginate
microparticles (including dissolution, hardness and friability tests), as well
as the release profile of xanthones in simulated gastrointestinal fluids, were
investigated.
|
|
Xanthone-loaded
chitosan-alginate microparticles in a tablet formulation were evaluated in
terms of their physicochemical characteristics and release profiles in
simulated gastrointestinal fluids. The two tablet formulations satisfied the
requirements for weight and size uniformity, but not for hardness; only one
formula satisfied the friability requirement. The dissolution test using three
simulated gastrointestinal fluids revealed similar pH-independent cumulative
release profiles of mangostin. All simulated gastrointestinal fluids exhibited
burst releases in the first 60 min of the immersion time. The results obtained
herein demonstrated the potential of the tested tablet formulations for the
delivery of xanthones into the gastrointestinal tract. To achieve the release
to a targeted area in the digestive tract, the excipient composition of the
tablet should be modified.
The research activity was part of the LPDP Rispro Invitasi 2019 UI
SK KEP-52/LPDP/2019 .
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