k-Carrageenan/sericin-based multiparticulate systems: A novel gastro-resistant polymer matrix for indomethacin delivery

Int J Biol Macromol. 2023 Mar 31:232:123381. doi: 10.1016/j.ijbiomac.2023.123381. Epub 2023 Jan 31.

Abstract

This study aimed to develop a natural and multiparticulate carrier of k-carrageenan (k-Car) and sericin (Ser) for encapsulation of indomethacin (IND) in order to minimize gastrointestinal effects caused by immediate-release. Increasing the amount of IND in the formulations subtly reduced the entrapment efficiency (EE) and drug loading (DL) due to matrix saturation. Sericin was essential to improve EE and DL when compared to pure k-Car (EE > 90 % and DL > 47 %) with suitable particle sizes (1.3461 ± 0.1891-1.7213 ± 0.1586 mm). The incorporation and integrity of IND in the particles were confirmed by analytical techniques of HPLC, XRD, FTIR, and SEM. Additionally, the k-Car/Ser matrix was pH-responsive with low IND release at pH 1.2 and extended-release at pH 6.8. The Weibull model had an adequate fit to the experimental data with R2aju 0.950.99 and AIC 82.4-24.9, with curves in parabolic profile (b < 1) and indicative of a controlled drug-release mechanism by diffusion. Besides, k-Car/Ser/IND and placebo were not cytotoxic (cell viability > 85 % at 150-600 μM) for the Caco-2 cell line. Therefore, the polymeric matrix is gastro-resistant, stable, and biocompatible to carry indomethacin and deliver it to the intestinal environment.

Keywords: Anti-inflammatory; Drug delivery; Natural polymer; Polysaccharide; Protein.

MeSH terms

  • Caco-2 Cells
  • Carrageenan
  • Drug Delivery Systems
  • Humans
  • Indomethacin* / pharmacology
  • Polymers
  • Sericins*

Substances

  • Indomethacin
  • Sericins
  • Carrageenan
  • Polymers