Cyanine derivative as a suitable marker for thermosensitive in situ gelling delivery systems: In vitro and in vivo validation of a sustained buccal drug delivery

Abstract

Buccal administration route is a promising way for a large number of drugs exhibiting a low oral bioavailability. The present work describes the formulation and evaluation of a mucoadhesive and thermosensitive in situ gelling delivery system based on poloxamer 407, poloxamer 188 and xanthan gum for buccal drug delivery. First, the mucoadhesion properties were evaluated using a tensile test. The effect of xanthan gum on the mucoadhesion force was demonstrated. Then, to assess the buccal residence time which reflects the mucoadhesion properties, the validation of a fluorescence probe for in vivo optical imaging experiment was conducted. Methyl-Cyanine 5 derivative (Me-Cy5) was used to label the hydrogels, dissolution tests and permeation studies through buccal epithelium cells showed that Me-Cy5 release from hydrogels was mainly due to an erosion mechanism and presented a limited penetration across epithelium cells. These results suggest that, Me-Cy5 is a suitable marker for thermosensitive in situ gelling delivery systems as the probe mostly stays entrapped in the hydrogel and do not cross the epithelial barrier. Buccal residence performance of the hydrogel was evaluated for the first time by non-invasive optical imaging after administration to mice. This technique is an interesting alternative compared to visual observations and sacrifice involved experiments, which could also be exploited to various administration routes.

Hydrogels in Burn Wound Management—A Review

“…Hydrogel properties led to the development of systems with controlled drug release, high drug concentration in the tumor site, prolonged topical residence time, sustained drug release, and reduced systemic side effects because of minimal invasiveness. To date, thermogel delivery systems were used in transdermal [ 81 , 82 , 83 ], ocular [ 84 , 85 , 86 ], nasal [ 87 , 88 , 89 ], buccal [ 90 , 91 ] drug delivery systems, as well as anti-tumor [ 92 , 93 , 94 ] drug delivery systems in cancer and chronic diseases treatment.…”

An Updated Overview of the Emerging Role of Patch and Film-Based Buccal Delivery Systems

“…Nanocarriers loaded into hydrogels are used for buccal delivery to improve the residence time, bioavailability as well as to protect the drug degradation. It was reported that salbutamol induced buccal epithelial changes were effectively counteracted by including a combination of bioadhesive poloxamer and xanthan gum in the buccal film formulation [ 142 ]. The cell viability enhancement evaluated using TR146 human buccal epithelial cell line indicates the applicability of these hydrogels for buccal delivery of diverse drugs.…”

<p>Bucco-Adhesive Film as a Pediatric Proper Dosage Form for Systemic Delivery of Propranolol Hydrochloride: In-vitro and in-vivo Evaluation</p>

“…This entire unit was shacked at 50 rpm in a water-bath kept at 37± 0.1ºC. 26,27 The 2 mL samples were removed at appropriate times and replaced with fresh phosphate buffer solution. The samples were assayed spectrophotometrically at 290 nm 28 using a UV-VIS spectrophotometer (Spectronic, Genesys 2PC, NJ, USA) to determine the amount of drug released.…”