Synthesis and Evaluation of Rutin–Hydroxypropyl β-Cyclodextrin Inclusion Complexes Embedded in Xanthan Gum-Based (HPMC-g-AMPS) Hydrogels for Oral Controlled Drug Delivery

Abstract

Oxidants play a significant role in causing oxidative stress in the body, which contributes to the development of diseases. Rutin—a powerful antioxidant—may be useful in the prevention and treatment of various diseases by scavenging oxidants and reducing oxidative stress. However, low solubility and oral bioavailability have restricted its use. Due to the hydrophobic nature of rutin, it cannot be easily loaded inside hydrogels. Therefore, first rutin inclusion complexes (RIC) with hydroxypropyl-β-cyclodextrin (HP-βCD) were prepared to improve its solubility, followed by incorporation into xanthan gum-based (hydroxypropyl methylcellulose-grafted-2-acrylamido -2-methyl-1-propane sulfonic acid) hydrogels for controlled drug release in order to improve the bioavailability. Rutin inclusion complexes and hydrogels were validated by FTIR, XRD, SEM, TGA, and DSC. The highest swelling ratio and drug release occurred at pH 1.2 (28% swelling ratio and 70% drug release) versus pH 7.4 (22% swelling ratio, 65% drug release) after 48 h. Hydrogels showed high porosity (94%) and biodegradation (9% in 1 week in phosphate buffer saline). Moreover, in vitro antioxidative and antibacterial studies (Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli) confirmed the antioxidative and antibacterial potential of the developed hydrogels.

Enhanced Cellular Delivery of Tildipirosin by Xanthan Gum–Gelatin Composite Nanogels

“…Gelatin, which is the hydrolysate of collagen, expands in an aqueous solution because it contains a lot of hydrophilic groups, like amino and hydroxyl ones . The capacity of xanthan gum to boost the hydrogel’s swelling degree may be attributed to its hydrophilicity and the presence of o-acetyl and pyruvyl residues . Similar results have also been observed in other investigations .…”

“…31 The capacity of xanthan gum to boost the hydrogel's swelling degree may be attributed to its hydrophilicity and the presence of o-acetyl and pyruvyl residues. 33 Similar results have also been observed in other investigations. 37 According to the literature, xanthan gum and gelatin interact by forming many bridges to which water molecules can adhere within the matrix, hence increasing the water contact surface.…”

“…At 13.7°, tildipirosin showed a peak, confirming that the drug is crystalline in nature; after tildipirosin was loaded into the nanogels, the nanogels came to be more amorphous. It is hypothesized that the observed decrease in crystallinity was caused by changes in the supramolecular structure of nanogels produced by the development of intermolecular hydrogen bonds between the drug and the polymer, interfering with its purity and lowering its crystal lattice properties . Drug amorphization can be attributed to the presence of potent interactions between the drug and the carrier, which is known to result in amorphous dispersions when amorphous polymers are utilized as drug carriers …”

In‐vitro evaluation of antimicrobial and anti‐inflammatory efficacy of the gelatin‐β‐cyclodextrin hydrogels as biodegradable carriers for rutin

“…Obviously, the swelling of Gel‐ βCD 2‐R and Gel‐ βCD 4‐R hydrogels was slowed and dependent on the hydrophobicity of rutin compared to the unloaded Gel‐ βCD 2 and Gel‐ βCD 4 hydrogels [29] . The porosity of hydrogels plays an important effect on the swelling and the drug release that in turn their surfaces affected by the received media [30] . The water uptake is dependent on the cross‐linking density, porosity, hydrophilicity, and wall thickness of polymer network [31] and the interaction between the polymer network and the swelling medium [21,32] …”

“…[29] The porosity of hydrogels plays an important effect on the swelling and the drug release that in turn their surfaces affected by the received media. [30] The water uptake is dependent on the cross-linking density, porosity, hydrophilicity, and wall thickness of polymer network [31] and the interaction between the polymer network and the swelling medium. [21,32]…”