Preparation and Characterization of PEG4000 Palmitate/PEG8000 Palmitate-Solid Dispersion Containing the Poorly Water-Soluble Drug Andrographolide

Abstract

Solid dispersion (SD) is the effective approach to improve the dissolution rate and bioavailability of class II drugs with low water solubility and high tissue permeability in the Biopharmaceutics Classification System. is study investigated the effects of polyethylene glycol (PEG) molecular weight in carrier material PEG palmitate on the properties of andrographolide (AG)-SD. We prepared SDs containing the poorly water-soluble drug AG by the freeze-drying method. e SDs were manufactured from two different polymers, PEG4000 palmitate and PEG8000 palmitate. e physicochemical properties of the AG-SDs were characterized by Fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, dissolution testing, and so on. We found that AG-PEG4000 palmitate-SD and AG-PEG8000 palmitate-SD were similar in the surface morphology, specific surface area, and pore volume. Compared with the AG-PEG4000 palmitate-SD, the intermolecular interaction between PEG8000 palmitate and AG was stronger, and the thermal stability of AG-PEG8000 palmitate-SD was better. In the meanwhile, the AG relative crystallinity was lower and the AG dissolution rate was faster in AG-PEG8000 palmitate-SD. e results demonstrate that the increasing PEG molecular weight in the PEG palmitate can improve the compatibility between the poorly water-soluble drug and carrier material, which is beneficial to improve the SD thermal stability and increases the dissolution rate of poorly water-soluble drug in the SD.

Characterization of Novel Solid Dispersions of Moringa oleifera Leaf Powder Using Thermo-Analytical Techniques

“…Similar results were reported by [20]. Zeng et al [54] also reported a similar finding that PEG increased the thermal stability of Palmitate in solid dispersion.…”

Cellulose Acetate-Based Electrospun Materials with a Variety of Biological Potentials: Antibacterial, Antifungal and Anticancer

“…PEG is a water-soluble polymer with low toxicity, thus making it suitable for contact with living organisms. Moreover, PEG improves the solubilization of poor water-soluble drugs and could assist in their release [ 3 ]. Some of us have studied the effect of PEG incorporation on the release of 5-nitro-8-hydroxyquinoline (5N8Q) from the electrospun PLA/PEG fibers.…”

Polymer Matrix and Manufacturing Methods in Solid Dispersion System for Enhancing Andrographolide Solubility and Absorption: A Systematic Review

“…Eleven in vitro studies [5,6,10,15,17,18,[20][21][22][23][24] were conducted to assess the SD of ADG aqueous solubility. They could be classified according to polymer matrices into eight groups, namely polyethylene glycol (PEG), the polyvinyl carprolactam-polyvinyl acetatepolyethylene glycol graft copolymer (PCL-PVAc-PEG; Soluplus), polyvinylpyrrolidone (PVP), PVP with vinyl acetate (PVP-VA), hydroxypropyl methylcellulose (Hypromellose; HPMC), silicon dioxide, chitosan and Poloxamer 188.…”

“…Andrographolide (ADG), a diterpene lactone with pharmacological effects such as anti-inflammatory, antiviral, antibacterial, antioxidant and immune-boosting properties, serves as a marker to control the specification of Andrographis paniculata extract and its products [3,4]. However, it exhibits poor aqueous solubility (3.29 ± 0.73 µg/mL at 25 • C) with a log p value of 2.632 ± 0.135, and its crystalline form has a melting point at 243 • C. The molecular weight of ADG is 350.45 g•mol −1 [5,6]. Ye et al reported low oral absorption of ADG (dose 120 mg/kg) with a C max of 0.23 ± 0.05 µg/mL in rats [7].…”