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.
Highlights
Gellan gum (GG) and pectin (P) are widespread available, low-cost, nontoxic, stable, biocompatible polysaccharides which exhibit gelling properties and have several structures able to be chemically and/or physically modified, providing promising characteristics for the design of drug delivery systems in the pharmaceutical field [1,2]
We showed that crosslinked mucoadhesive gellan gum:pectin (GG):P beads are a rational strategy to protect RES from the harsh environment of the stomach and modulate its release rates and biological interactions, and is an efficient and safe system for the targeted colonic delivery of this promising drug by the oral route
RES was successfully encapsulated in mucoadhesive beads of GG:P ionically crosslinked with Al3+ ions, achieving a high %EE
Summary
Gellan gum (GG) and pectin (P) are widespread available, low-cost, nontoxic, stable, biocompatible polysaccharides which exhibit gelling properties and have several structures able to be chemically and/or physically modified, providing promising characteristics for the design of drug delivery systems in the pharmaceutical field [1,2]. Mucoadhesion is a complex phenomenon and mucoadhesive ability can be related to the presence of reactive functional groups in the polymer chain capable of interacting with mucin present in the mucus [9]. Both GG and P are anionic polysaccharides with well-known mucoadhesiveness, related mainly to their numerous carboxyl groups that can interact through hydrogen bonds with mucin oligosaccharide chains [1,10,11,12,13,14,15,16]
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