Abstract
Objective: Hot Melt Extrusion (HME) is one of the techniques for preparing a solid dispersion hydrophilic excipient known as a no solvents practical method to increase the solubility of drugs. Apigenin (APG) has properties that thermal stable with melting point 345-350 °C but very low solubility in the water around 1,35 µg/ml. The polymer is stable in the HME method are Soluplus and Kollidon VA 64. The study aims to optimize the kind of polymer in HME formulae to improve the solubility and dissolution rate of apigenin by solid dispersion using hot-melt extrusion.
 Methods: Apigenin 10–50% w/w and Kollidon®VA 64 or Soluplus® and combination of Kollidon®VA 64 and Soluplus® were mixed, and the resulting blends extruded using a twin-screw extruder (Teach-Line ZK25T). Characterization of apigenin extrudates conducted using scanning electron microscopy, thermogravimetric analysis, differential scanning calorimetry, Fourier transform infrared spectroscopy, powder X-ray diffractometry, and dissolution.
 Results: Solubility studies presented enhancement in apigenin of 10%/Soluplus®90%; 10% w/w apigenin/Kollidon®VA 64 (90%); and 33,3% w/w apigenin/Kollidon®VA 64 33,3% mix Soluplus® 33,3% increased more than 18,25; 16,18-and 8,52-fold in water, respectively. Furthermore dissolution studies showed enhancement in apigenin percent release of 10%/Soluplus®90%; 10% w/w apigenin/Kollidon®VA 64 90%; and 33,3% w/w apigenin/Kollidon®VA 64 33,3% mix Soluplus® 33,3% tablet apigenin HME up to 34,29%; 69,75% and 30,69%, respectively.
 Conclusion: The formulation of 10% w/w Apigenin and 90% Soluplus® using hot-melt extrusion able to increase water solubility approximately 18,25-fold than raw material apigenin.
Highlights
Apigenin is a phytochemical compound that contained in some fruits, herbs, and vegetables
APG has much practical use, it faces an obstacle in the formulation because of limited solubility, especially when it is used for oral administration
Limited studies concerning the application of these techniques apigenin for examples apigenin nanocrystals using supercritical antisolvent process [8], inclusion complex of apigenin-hydroxypropyl-β-cyclodextrin by using supercritical antisolvent process [9], cocrystal of apigenin [10], apigenin in binary {Transcutol® + water} mixtures [11], Formulation and characterization of an apigenin-phospholipid phytosomes (APLC) [12], design and evaluation of a self-micro emulsifying drug delivery system for apigenin [13], improved solubility and oral bioavailability of apigenin via soluplus/pluronic f127 binary mixed micelles system [14], preparation and in vitro evaluation of apigenin loaded lipid nanocapsules [15]
Summary
Hot Melt Extrusion Apigenin 10–50% w/w and Soluplus®, Kollidon® VA 64 (table 1) mix using a mixer (IKA EUROSTAR) for 10 min. 1. XRD data showed pure apigenin, the physical mixture is crystalline, but with HME change crystallin form to amorf so that solubility can increase, all the extrudates showed in fig. The hot-melt extrusion process carried out using a twin-screw extruder (Teach-Line ZK25T) standard screw configuration used in this study, which consists of five conveying zones and two mixing zones Scanning electron microscopy images showed the absence of crystals in 10% w/w apigenin/Soluplus and kollidon indicating that apigenin was dispersed in the Soluplus and in the kollidon polymer carrier as an amorphous, but when apigenin, soluplus mixed by kollidon with the same comparison still have image crystallin. Dissolution studies demonstrated enhancement in apigenin percent release of 10%/Soluplus®90%; 10% w/w apigenin/Kollidon®VA 64 90%; and 33,3% w/w apigenin/Kollidon®VA 64 33,3% mix Soluplus® 33,3% tablet apigenin HME up to 34,29%; 69,75% and 30,69%, respectively Dissolution studies demonstrated enhancement in apigenin percent release of 10%/Soluplus®90%; 10% w/w apigenin/Kollidon®VA 64 90%; and 33,3% w/w apigenin/Kollidon®VA 64 33,3% mix Soluplus® 33,3% tablet apigenin HME up to 34,29%; 69,75% and 30,69%, respectively (fig. 9)
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
