Thermoreversible mucoadhesive polymer-drug dispersion for sustained local delivery of budesonide to treat inflammatory disorders of the GI tract

Santos

Materials Science and Engineering: C

et al. 2021

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Section: Transmission Electron Microscopy (Tem)supporting

confidence: 89%

Interaction between mucoadhesive cellulose derivatives and Pluronic F127: Investigation on the micelle structure and mucoadhesive performance

Santos

Materials Science and Engineering: C

et al. 2021

Beilstein J. Nanotechnol.

“…0.2 mL of the nanostructured material was diluted in a 10 mL volumetric flask and placed on a formvar/Carbon 200 mesh, copper grid (Ted Tella, Redding, CA, USA). This set was negatively stained with 2% (w/v) uranyl acetate solution for observation [57,95–96]. The samples were prepared at 37 °C.…”

Section: Methodsmentioning

confidence: 99%

Design of a nanostructured mucoadhesive system containing curcumin for buccal application: from physicochemical to biological aspects

Ferreira¹,

Braga²,

Oliveira³

et al. 2019

Mucoadhesive nanostructured systems comprising poloxamer 407 and Carbopol 974P® have already demonstrated good mucoadhesion, as well as improved mechanical and rheological properties. Curcumin displays excellent biological activity, mainly in oral squamous cancer; however, its physicochemical characteristics hinder its application. Therefore, the aim of this study was to develop nanostructured formulations containing curcumin for oral cancer therapy. The photophysical interactions between curcumin and the formulations were elucidated by incorporation kinetics and location studies. They revealed that the drug was quickly incorporated and located in the hydrophobic portion of nanometer-sized polymeric micelles. Moreover, the systems displayed plastic behavior with rheopexy characteristics at 37 °C, viscoelastic properties and a gelation temperature of 36 °C, which ensures increased retention after application in the oral cavity. The mucoadhesion results confirmed the previous findings with the nanostructured systems showing a residence time of 20 min in porcine oral mucosa under flow system conditions. Curcumin was released after 8 h and could permeate through the porcine oral mucosa. Cytotoxicity testing revealed that the formulations were selective to cancer cells over healthy cells. Therefore, these systems could improve the physicochemical characteristics of curcumin by providing improved release and permeation, while selectivity targeting cancer cells.

“…Antonino et al [ 86 ] developed an in situ gelling formulation using poloxamer P127, as thermo-reversible polymer, and entrapping budesonide (BUD), a potent corticosteroid used for the treatment of gastrointestinal inflammatory diseases. In vivo studies performed in a murine model of intestinal mucositis proved that the formulation was effective in the treatment of inflammatory injuries of the intestinal mucosa.…”

Section: Gastrointestinal Routementioning

confidence: 99%

Recent Advances in the Development of In Situ Gelling Drug Delivery Systems for Non-Parenteral Administration Routes

et al. 2020

In situ gelling drug delivery systems have gained enormous attention over the last decade. They are in a sol-state before administration, and they are capable of forming gels in response to different endogenous stimuli, such as temperature increase, pH change and the presence of ions. Such systems can be administered through different routes, to achieve local or systemic drug delivery and can also be successfully used as vehicles for drug-loaded nano- and microparticles. Natural, synthetic and/or semi-synthetic polymers with in situ gelling behavior can be used alone, or in combination, for the preparation of such systems; the association with mucoadhesive polymers is highly desirable in order to further prolong the residence time at the site of action/absorption. In situ gelling systems include also solid polymeric formulations, generally obtained by freeze-drying, which, after contact with biological fluids, undergo a fast hydration with the formation of a gel able to release the drug loaded in a controlled manner. This review provides an overview of the in situ gelling drug delivery systems developed in the last 10 years for non-parenteral administration routes, such as ocular, nasal, buccal, gastrointestinal, vaginal and intravesical ones, with a special focus on formulation composition, polymer gelation mechanism and in vitro release studies.