Polymeric Micelles Enhance Mucosal Contact Time and Deposition of Fluocinolone Acetonide

Abstract

This study used polymeric micelles to improve quality by increasing drug solubility, extending mucosal drug retention time, enhancing mucoadhesiveness, and promoting drug permeation and deposition. Fluocinolone acetonide (FA) was loaded into polymeric micelles (FPM), which were composed of poloxamer 407 (P407), sodium polyacrylate (SPA), and polyethylene glycol 400, and their physicochemical properties were examined. Small-angle X-ray scattering (SAXS) revealed a hexagonal micellar structure at all temperatures, and the concentrations of P407 and SPA were shown to significantly affect the solubility, mucoadhesion, release, and permeation of FPMs. The characteristics of FPM7 and FPM8 revealed crystalline states inside the micelles, which was consistent with the morphology and nano-hexagonal structure. The results of ex vivo experiments using focal plane array (FPA)-based Fourier transform infrared (FTIR) imaging showed that FPM7 penetrated quickly through the epithelium, lamina propria, and submucosa, and remained in all layers from 5–30 min following administration. In contrast, FPM8 penetrated and passed through all layers. FPMs with extended mucoadhesion, improved drug–mucosal retention time, and increased FA permeation and deposition were successfully developed, and could be a promising innovation for increasing the efficiency of mouth rinses, as well as other topical pharmaceutical and dental applications.

In Vitro and Ex Vivo Evaluation of Fluocinolone Acetonide–Acitretin-Coloaded Nanostructured Lipid Carriers for Topical Treatment of Psoriasis

“…Similarly, a principal peak at 21° was observed in the diffractogram of the stearic acid [ 37 ]. Moreover, the FLU executed sharp characteristic crystalline peaks at 15°, 19°, 22°, 24° and 25° [ 38 ], whereas such peaks disappeared in the case of the NLCs, which may be due to the conversion of the stearic acid, ACT and FLU from a crystalline form to an amorphous form, and the successful incorporation of both ACT and FLU into the NLCs ( Figure 4 ).…”

Preparation, Properties and Therapeutic Effect of a TPL Nanoparticle Thermosensitive Gel for Intra-Articular Injection

“…The ultrasonic velocity, dynamic scattering, light scattering, small-angle X-ray diffraction, small-angle neutron scattering, rheology and electrolyte behavior of the P407 aqueous solution were studied [ 26 , 27 , 28 , 29 ]. It was found that the gelation process was the result of micellar properties (aggregation number and micellar symmetry, etc.)…”

New Technological Approaches for Dental Caries Treatment: From Liquid Crystalline Systems to Nanocarriers

“…The most commonly used polymers are poloxamers (amphiphilic block copolymers) and polyethylene glycol (PEG). Some advantages of micelles are the ability to improve the solubility and stability of poorly water-soluble drugs, promote a sustained drug release, improve permeability, and biocompatibility, in addition to improved drug biodistribution, that can be achieved by surface modifications (i.e., acrylate groups, which increases the mucoadhesion), as well as reduced side effects [ 108 , 109 ]. Common uses of PMs in dentistry include their use for the protection of dental structures, in combination with antimicrobial drugs for the inhibition of demineralization ( Table 3 ) [ 110 ].…”