Gellan Gum/Pectin Beads Are Safe and Efficient for the Targeted Colonic Delivery of Resveratrol

Abstract

This work addresses the establishment and characterization of gellan gum:pectin (GG:P) biodegradable mucoadhesive beads intended for the colon-targeted delivery of resveratrol (RES). The impact of the polymer carrier system on the cytotoxicity and permeability of RES was evaluated. Beads of circular shape (circularity index of 0.81) with an average diameter of 914 µm, Span index of 0.29, and RES entrapment efficiency of 76% were developed. In vitro drug release demonstrated that beads were able to reduce release rates in gastric media and control release for up to 48 h at an intestinal pH of 6.8. Weibull's model correlated better with release data and b parameter (0.79) indicated that the release process was driven by a combination of Fickian diffusion and Case II transport, indicating that both diffusion and swelling/polymer chains relaxation are processes that contribute equally to control drug release rates. Beads and isolated polymers were observed to be safe for Caco-2 and HT29-MTX intestinal cell lines. RES encapsulation into the beads allowed for an expressive reduction of drug permeation in an in vitro triple intestinal model. This feature, associated with low RES release rates in acidic media, can favor targeted drug delivery from the beads in the colon, a promising behavior to improve the local activity of RES.

Encapsulation and Enhanced Release of Resveratrol from Mesoporous Silica Nanoparticles for Melanoma Therapy

“…The Weibull model better described the release kinetics data than the NWF equation (higher R 2 and lower χ 2 values), with a coefficient of determination (R 2 ) in the range of 0.960–0.990 ( Table 2 ). The Weibull model is a general empirical equation that has been successfully applied to several drug release systems, including to RES release from lipid and polymer-based carriers [ 76 , 77 , 78 , 79 ]. Because this is an empiric model, not deducted from any kinetic fundament, the model does not provide information about the mechanism of release [ 69 ].…”

Exploiting supramolecular interactions to produce bevacizumab-loaded nanoparticles for potential mucosal delivery

“…Generally, different materials and systems are able to establish supramolecular interactions with mucosal components, such as mucin chains, because of the presence of reactive functional groups at the polymer chains, which facilitate adhesion to the mucus. On the other hand, to design mucus penetrating systems, the opposite logic must be used in order to open paths, facilitating system permeation [19,[25][26][27].…”

Carbohydrate‐based nanomaterials for biomedical applications

“…Additionally, oxygen‐producing biomaterials were developed based on gellan gum (Newland, Baeger, Eigel, Newland, & Werner, ). Chitosan‐gellan gum systems (S. Kumar, Kaur, Bernela, Rani, & Thakur, ), and pectin‐gellan gum systems (Bera, Kumar, & Maiti, ; Fernandes, Fortes, da Cruz Fonseca, Breitkreutz, & Ferraz, ; Prezotti et al, ) are popular choices for smart drug delivery systems. Xanthan gum is a microbial polysaccharide produced by Xanthomonas bacteria; it is negatively charged and widely used for tissue engineering (A. Kumar, Rao, & Han, ) and drug delivery (Salamanca, Yarce, Moreno, Prieto, & Recalde, ).…”