Abstract
Chitosan-alginate microparticles loaded with hydrophobic mangostins present in the mangosteen rind extract have been formulated and optimized for colon-targeted bioactive drug delivery systems. The chitosan–mangostin microparticles were prepared using the ionotropic gelation method with sodium tripolyphosphate as the cross-linking agent of chitosan. The chitosan–mangostin microparticles were then encapsulated in alginate with calcium chloride as the linking agent. The mangostin release profile was optimized using the Box–Behnken design for response surface methodology with three independent variables: (A) chitosan–mangostin microparticle size, (B) alginate:chitosan mass ratio, and (C) concentration of calcium chloride. The following representative equation was obtained: percent cumulative release of mangostins (10 h) = 59.51 − 5.16A + 20.00B − 1.27C − 1.70AB − 5.43AC − 5.04BC + 0.0579A2 + 10.25B2 + 1.10C2. Cumulative release of 97% was obtained under the following optimum condition for microparticle preparation: chitosan–mangosteen particle size < 100 µm, alginate:chitosan mass ratio of 0.5, and calcium chloride concentration of 4% w/v. The alginate to chitosan mass ratio is the statistically significant variable in the optimization of sequential release profile of mangostins in simulated gastrointestinal fluids. Furthermore, a sufficient amount of alginate is necessary to modify the chitosan microparticles and to achieve a complete release of mangostins. The results of this work indicate that the complete release of mangostins to the colon area can be achieved using the chitosan–alginate microparticles as the bioactive delivery system.
Highlights
The colon is one of the most important organs in the human digestive tract
This study aims to optimize the formulation of chitosan–alginate microparticles as a carrier to deliver mangostin to the colon area such that minimum release is achieved in the stomach but a high and constant release rate is achieved in the colon
The use of UV-vis spectrophotometry to quantify total mangostins in the mangosteen rind extract has been validated against the use of a high-performance liquid chromatography (HPLC) apparatus
Summary
It is desirable to formulate a colon-targeted drug delivery system to treat various colon diseases such as ulcerative colitis, Crohn’s disease, and colon cancer [1,2]. Patients prefer the oral administration of drugs for the treatment of colonic diseases; several factors must be considered first. Inappropriate formulations in combining several polymers as carriers can cause drugs to degrade and fail to cure the disease because they do not reach the location in the colon. Mangostins from mangosteen peel extract are hydrophobic phenolic compounds that have been identified as strong anti-proliferative agents against human DLD-1 colon cancer cells [3]. Mangostins are reported to show potential as chemopreventive agents for cancer without causing side-effects [4]. The encapsulation of mangostins in chitosan has been reported to increase their bioavailability and mucoadhesivity [9,10]
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