A Micellar-Hydrogel Nanogrid from a UV Crosslinked Inulin Derivative for the Simultaneous Delivery of Hydrophobic and Hydrophilic Drugs.

Delia Mandracchia,Cinzia Di Franco,Maria Torre,Enrica Calleri,Sara Perteghella,Adriana Trapani,Giuseppe Tripodo

doi:10.3390/pharmaceutics10030097

Abstract

Hydrogels are among the most common materials used in drug delivery, as polymeric micelles are too. They, preferentially, load hydrophilic and hydrophobic drugs, respectively. In this paper, we thought to combine the favorable behaviors of both hydrogels and polymeric micelles with the specific aim of delivering hydrophilic and hydrophobic drugs for dual delivery in combination therapy, in particular for colon drug delivery. Thus, we developed a hydrogel by UV crosslinking of a methacrylated (MA) amphiphilic derivative from inulin (INU) (as known INU is specifically degraded into the colon) and vitamin E (VITE), called INVITEMA. The methacrylated micelles were physicochemically characterized and subjected to UV irradiation to form what we called the “nanogrids”. The INVITEMA nanogrids were characterized by DSC, SEM, TEM, water uptake and beclomethasone dipropionate (BDP) release. In particular, the release of the hydrophobic drug was specifically assessed to verify that it can spread along the hydrophilic portions and, therefore, effectively released. These systems can open new pharmaceutical applications for known hydrogels or micelle systems, considering that in literature only few examples are present.

Highlights

Hydrogels are tridimensional networks formed by interconnected polymer chains to form an insoluble network
The first step allowed the formation of the ester group between vitamin E (VITE) and INU to provide the hydrophilic polymer with hydrophobic moieties leading to an amphiphilic derivative self-assembling in nanomicelles as previously described [17,19,20]
INVITEMA derivatives were obtained with three different DD% based on the applied reaction conditions

Summary

Introduction

Hydrogels are tridimensional networks formed by interconnected polymer chains to form an insoluble network They absorb large amounts of water while still maintaining the 3D structure and the original shape while changing their volume [1]. From a pharmaceutical point of view, the polysaccharides can be considered as a gold standard in the delivery of water soluble molecules including macromolecules such as proteins and other biomolecules such as peptides or DNA/RNA fragments [12]. These kinds of molecules are mostly excluded from being delivered by other drug delivery systems (DDSs) such as those with hydrophobic groups providing a good environment for non-water-soluble molecules. Other commonly used DDSs are undoubtedly liposomes and solid dispersions [14,15]

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Conclusion