Formulation, Characterization, and In Vitro Evaluation of Bioadhesive Gels Containing 5-Fluorouracil

Abstract

The objective of this study was to prepare and evaluate in vitro the bioadhesive gels of 5-Fluorouracil (FU) for the treatment of oropharyngeal cancer. In preformulation study, the physicochemical interactions between FU and polymers were investigated by X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectrophotometry, and differential scanning calorimetry (DSC). According to FTIR, XRD, and DSC studies, the drug did not show any evidence of an interaction with the polymers used and was present in an unchanged state. The gel formulations containing FU were prepared by using Poloxamer 407, HPMC K 15 M, and Gantrez ® S-97 (polymethylvinylether-co-maleic anhydride). The formulations contained Poloxamer 407 (16-18% w/w) either alone or in combination with HPMC K 15 M and Gantrez ® S-97. The bioadhesiveness of the gels was found to increase with increasing proportion of HPMC K 15 M and Gantrez ® S-97. In vitro release studies indicated that release could be sustained up to 8 hr. The permeability coefficients (Kp) of gel across cellulose membrane and buccal mucosal membrane were 1.06 × 10 -4 cm/s and 3.94 × 10 -5 cm/s, respectively, and differed significantly ( p < 0.05). Increasing temperature increased the drug release by increasing drug diffusion despite increase in viscosity. The pH of the release medium showed a very slight effect on the release of FU. Mathematical modeling of in vitro dissolution data indicated the best fitting with Korsemeyer-Peppas model and the drug release kinetics primarily as non-Fickian diffusion.

Transbuccal Delivery of 5-Fluorouracil: Permeation Enhancement and Pharmacokinetic Study

“…The bioadhesive strength and viscosity of the optimized formulation were 12.8 (±1.4)×10 3 dyne/cm 2 and 544.49 (± 5.9) cps, respectively (29). No interactions were found between formulation ingredients and FU (29). Table II depicts results of stability study of FU bioadhesive gels.…”

“…These gels were evaluated for compatibility between drug and polymers, assay, pH, bioadhesion, viscosity, in vitro release across cellulosic membrane, and in vitro diffusion across buccal mucosa. The details of formulation and characterization of buccal bioadhesive gels containing FU are reported in our earlier work (29).…”

Modified drug release of poloxamer matrix by including water-soluble and water-insoluble polymer

“…Reversible gels refer to those that have the capacity to make, break, and modify the bonds responsible for holding the network together. Poloxamer is a thermoreversible gel; this property has been studied in the delivery of topical, intraocular, intranasal, and implantable dosage forms [7][8][9][10][11] . In ocular drug delivery, the increase in viscosity of poloxamer 407 at body temperature increases the residence time of the drug in the eyes 12 .…”

Preparation and Evaluation of Tubular Micelles of Pluronic Lecithin Organogel for Transdermal Delivery of Sumatriptan

“…Further, the strategies for vectorization of drug across the skin have been extended to polymeric gels like pluronic lecithin organogels (45), bioadhesive gels, etc. (46).…”