Development of Gastroretentive Carriers for Curcumin-Loaded Solid Dispersion Based on Expandable Starch/Chitosan Films

Abstract

Curcumin, a polyphenolic extract from the rhizomes of turmeric, exhibits antioxidant, anti-inflammatory, and anticancer activities, which are beneficial for the treatment of gastric diseases. However, curcumin’s therapeutic usefulness is restricted by its low aqueous solubility and short gastric residence time. In this study, curcumin-loaded solid dispersion (ratio 1:5) was prepared using Eudragit® EPO (Cur EPO-SD), resulting in an approximately 12,000-fold increase in solubility to 6.38 mg/mL. Expandable films incorporating Cur EPO-SD were subsequently prepared by solvent casting using different types of starch (banana, corn, pregelatinized, and mung bean starch) in combination with chitosan. Films produced from banana, corn, pregelatinized and mung bean starch unfolded and expanded upon exposure to simulated gastric medium, resulting in sustained release of 80% of the curcumin content within 8 h, whereas films based on pregelatinized starch showed immediate release characteristics. Curcumin-loaded expandable films based on different types of starch exhibited similar cytotoxic effects toward AGS cells and more activity than unformulated curcumin. Furthermore, the films resulted in increased anti-inflammatory activity against RAW 264.7 macrophage cells compared with the NSAID, indomethacin. These findings demonstrate the potential of expandable curcumin-loaded films as gastroretentive dosage forms for the treatment of gastric diseases and to improve oral bioavailability.

Development of raft-forming liquid formulations loaded with ginger extract-solid dispersion for treatment of gastric ulceration

“…The results were also confirmed by FT-IR spectra and the improvement of 6-gingerol solubility. Similar results have been reported for atorvastatin-PVP K30 [ 32 ], quercetin-PVP K30 [ 16 ], and curcumin-Eudragit® EPO solid dispersions [ 19 ].

Fig.

…”

“…Solid dispersion techniques have been used extensively to increase the solubility and bioavailability of hydrophobic drug compounds [ [16] , [17] , [18] , [19] , [20] , 25 , 31 , 32 ]. The 6-gingerol component of ginger extract was previously reported to be poorly soluble, with values lower than 1 mg/mL [ 25 ].…”

“…Solid-dispersion (SD) technology offers a mean of enhancing the solubility of 6-gingerol by dispersion in a hydrophilic carrier matrix [ 15 ]. Polymers are typically used as the carrier, including polyvinylpyrrolidone (PVP) [ 16 ], polyethylene glycol (PEG) [ 17 ], Eudragit® EPO [ 18 , 19 ] and hydroxypropyl methylcellulose (HPMC) [ 20 ].…”

Mucoadhesive buccal tablets incorporating curcumin solid dispersion as a potential approach for enhancing curcumin therapeutic efficacy in oral inflammatory disorders

“…This results in a significantly increased solubility of the drug compared to its crystalline form (20) . Several amorphous cur formulations with improved cur solubility have been created as amorphous solid dispersions (21)(22)(23) , co-amorphous systems (24,25) , and amorphous nanoparticles (26,27) . Amidst these various amorphous pharmacological formulations, the amorphous cur solid dispersion (Cur SD) is noteworthy for its notably uncomplicated technique of manufacture.…”