Particulate Delivery System of Chitosan - Diterpene Lactone Fraction of Sambiloto (Andrographis Paniculata Nees): Preparation, Characterization and in Vitro Drug Release

Abstract

Objective: This paper was aimed to study the effect of chitosan, sodium tripolyphosphate (TPP) as crosslinker, and diterpene lactone fraction of sambiloto (FDTL) from Andrographis paniculata Nees which contained 75.9% andrographolide on the characteristics of the FDTL-chitosan particulate system. Those characteristics were the physicochemical interaction, physical state, morphology, and drug entrapment efficiency. The in vitro drug release of the selected FDTL-chitosan particulate system was also evaluated. Methods:The particulate system of FDTL-chitosan was prepared by ionic gelation-spray drying method with the various amounts of TPP, chitosan, and FDTL. The physical characteristics were evaluated using Fourier transform infrared (FTIR), differential thermal analyzer (DTA), and X-ray diffraction, scanning electron microscope. In vitro drug release was performed in 0.1% sodium lauryl sulfate media at 37°C. Results:The results of FTIR and DTA analysis were in accordance with the results of morphology evaluation which indicated that chitosan-TPP ratio 10:8 could produce chitosan particles with a spherical and smooth surface. FDTL has been trapped in chitosan particulate systems, and the crystallinity of FDTL changed. Particulate systems with FDTL-chitosan-TPP ratio -4:10:8 showed better characteristics compared to others with entrapment efficiency of 33.82%. The dissolution efficiency at 360 minutes (ED 360 ) of particulate systems FDTL-chitosan was higher up to 1.5 times compared to FDTL. Conclusion:The difference in the ratio of chitosan and TPP affected the morphology of chitosan particles since the amount of drug loaded, and the amount of chitosan affected the drug entrapment. The ED 360 of FDTL of FDTL-chitosan-TPP increased up to 1.5 times compared to the FDTL.

The Effect of Chitosan Type and Concentration on Physical Characteristics and Drug Release Behavior of Andrographolide-Chitosan Microparticles Prepared by Ionic Gelation – Freeze Drying

“…The composition and preparation methods used in this study led to the drug entrapment efficiency (EE) of 77%, which was higher compared to the previous researches, were they were dried with spray drying methods and the EE was about 30% (Sari et al 2017). Freeze drying method could minimize drug loss during the drying process.…”

“…The diffractograms andrographolide-chitosan microparticle formulas, and the peak of Andografolid were still visible at an angle of 2θ 9.8°, 12°, 14.8°, 15.7° with small intensity. While its diffractogram did not show sharp diffraction peaks from andrographolide, which showed that andrographolide has undergone a change in crystalline structure due to the recrystallization barriers of crosslinked chitosan (Sari et al 2017).…”

“…The amount and molecular weight of chitosan was related to the availability of NH 3 + protonated from chitosan which interacted with -P 3 O 10 5of TPP to crosslink. This interaction affects the microparticles characteristics such as morphology, particle size, drug encapsulation which further affect the drug release, bioavailability and effectiveness (Sonia & Sharma, 2011;Kumar et al 2011;Sari et al 2017).…”

Screening of Critical Variables of Andrographis paniculata Extract Loaded onto Chitosan Microparticles

“…Encapsulation Efficiency is another important parameter to measure the amount of encapsulated active ingredient within the microparticles. The EE% is attributed to the concentration of the polymer in the system, where an increase in polymer concentration increases the density of the system and thus assist in the formation of crosslinks (Sari et al, 2016). Table 3 shows the EE% of all the formulations.…”