Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of Phoenix dactylifera L. of 5-Fluorouracil for Colon-Specific Drug Delivery

Abstract

In this study, 5-fluorouracil (5-FU)-loaded pollens of Phoenix dactylifera and their coating with ERS was done and evaluated for the colon-targeted delivery of 5-FU to treat colon cancer. Sporopollenin exine microcapsules (SEMC) from the pollens of Phoenix dactylifera were extracted by the reflux method and 5-FU into SEMC was encapsulated by the vacuum-assisted loading method. 5-FU loaded SEMC was coated with Eudragit® RS-100 (ERS) by the organic solvent-evaporation technique under vacuum to avoid the discharge of 5-FU in the stomach and small intestine. Morphological and physicochemical characterization of drug-loaded SEMC (coated/uncoated) was performed by scanning electron microscopy (SEM), FTIR, XRD, and DSC. The encapsulation and drug loading were determined by the direct method, and an in vitro release study was performed in simulated gastric and intestinal fluids (SGF/SIF). The colon-specific delivery of 5-FU from the SEMC was assessed in terms of pharmacokinetics and gastrointestinal tract distribution after oral administration in rats. The successful encapsulation and loading of 5-FU into SEMC by a vacuum-assisted loading technique and its coating with ERS by a solvent-evaporation technique were achieved. SEM images of uncoated SEMC have shown porous structures, and coating with ERS reserved their morphology with a smooth surface and discrete microstructures and the 5% w/v ERS acetone solution. ERS-coated SEMC sustained the release of 5-FU until 24 h in SIF, while it was up to 12 h only from uncoated SEMC. The maximum plasma concentration (Cmax) of 5-FU from uncoated SEMC was 102.82 μg/mL after 1 h, indicating a rapid release of 5-FU in the upper gastrointestinal tract. This concentration decreased quickly with a half-life of 4 h, AUC0-t was 264.1 μg/mL.h, and MRT0-inf was 5.2 h. The Cmax of 5-FU from ERS-coated SEMC was 19.47 μg/mL at 16 h. The Cmax of 5-FU in small intestines was 406.2 μg/g at 1 h from uncoated SEMC and 1271.5 μg/g at 12 h from coated SEMC. Conclusively, a 249.9-fold higher relative bioavailability of 5-FU was achieved with the ERS-coated SEMC in colon tissues than that from uncoated SEMC.

Multiparticulate Systems of Meloxicam for Colonic Administration in Cancer or Autoimmune Diseases

“…In previous works [ 13 , 14 ] some pH-dependent formulations were prepared with polymers, such as cellulose acetate phthalate (CAP), hydroxypropyl methyl cellulose phthalates (HPMCP) 50 and 55, and copolymers of methacrylic acid and methyl-methacrylate (for example, Eudragit ® S100, Eudragit ® L, Eudragit ® FS and Eudragit ® P4135F). Eudragit ® polymers are the most widely used synthetic products in the design of colonic release formulations because they offer mucoadhesiveness and pH-dependent release [ 15 , 16 , 17 , 18 ]. The ideal polymer should be able to withstand the low pH of the stomach (pH 1–3) and proximal small intestine (pH 4.5–6.0) but dissolve at the pH of the terminal ileum and colon (pH 6.5–7.5) (see Figure 1 ).…”

Dual-Responsive Microsphere Based on Natural Sunflower Pollen for Hemostasis and Repair in Inflammatory Bowel Disease

“…To prepare the AP@PS­(t+Dex) coated with Eudragit L100-55 (EL), the coating solution was prepared by dissolving EL in acetone . For the coating process, 100 mg of AP@PS­(t+Dex) was added to the 5 mL of 2.5% (w/v) EL solution.…”

“…To prepare the AP@PS(t+Dex) coated with Eudragit L100-55 (EL), the coating solution was prepared by dissolving EL in acetone. 44 For the coating process, 100 mg of AP@PS(t+Dex) was added to the 5 mL of 2.5% (w/v) EL solution. The dried EL/AP@PS(t+Dex) was obtained by evaporating acetone under vacuum at room temperature for 2 h. 4.4.…”

Utility of CT in detecting and monitoring subphrenic jujube pits: a retrospective cross-sectional study of clinical cases and ex vivo experiments

“…After analyzing the initial data ( Figure S2 and Table S3 ), only jujube pits longer than 2.5 cm were chosen for further mimic phantom study, including 20 raw and 20 boiled jujube pits together. They were then equally divided into five groups and soaked in five different solutions: double distilled water, saline, commercially available simulated gastric fluid, commercially available simulated intestinal fluid, and mixed solution ( 30 ). Double distilled water was used as a control, while the other four solutions simulated the liquid conditions of the gastrointestinal tract and extracellular fluid.…”