Thiolation of arabinoxylan and its application in the fabrication of controlled release mucoadhesive oral films

Abstract

BackgroundMucoadhesion is an important property that helps oral drug delivery system to remain attached with buccal mucosa and hence to improve the delivery of the drug. The current study was designed to achieve the thiol modification of Arabinoxylan (ARX) and to develop a mucoadhesive oral film for the improved delivery of tizanidine hydrochloride (TZN HCl).MethodSynthesis of thiolated arabinoxylan (TARX) was accomplished by esterification of ARX with thioglycolic acid (TGA). TARX was further used for the development of mucoadhesive oral films which were prepared by using a solvent casting technique. Formulation of the films was designed and optimized by using central composite design (CCRD), selecting TARX (X1) and glycerol (X2) as variables. Prepared film formulations were evaluated for mechanical strength, ex-vivo mucoadhesion, in-vitro drug release, ex-vivo drug permeation, surface morphology and drug contents.ResultsThiolation of ARX was confirmed by fourier transform infra-red spectroscopy (FTIR) as a peak related to thiol group appeared at 2516 cm−1. The claim of successful thiolation of ARX was strengthened by the presence of 2809.003 ± 1.03 μmoles of thiol contents per gram of the polymer, which was determined by Ellman’s reagent method. From the results, it was observed that the films were of satisfactory mechanical strength and mucoadhesiveness with folding endurance greater than 300 and mucoadhesive strength 11.53 ± 0.17 N, respectively. Reasonable drug retention was observed during in-vitro dissolution (85.03% cumulative drug release) and ex-vivo permeation (78.90% cumulative amount of permeated drug) studies conducted for 8 h. Effects of varying concentrations of both polymer and plasticizer on prepared mucoadhesive oral films were evaluated by ANOVA and it was observed that glycerol can enhanced the dissolution as well as permeation of the drug while TARX has opposite impact on these parameters.ConclusionIn nutshell, TARX in combination with glycerolwas found to be suitable for the development of controlled release mucoadhesive oral films of TZN HCl.Graphical AbstractSchematic diagram showing conversion of ARX to TARX, TARX to oral film and evaluation of fabricated oral film

Development of Tizanidine HCl-Meloxicam loaded mucoadhesive buccal films: In-vitro and in-vivo evaluation

“…Initially, SR layer containing TZN and IR layer of MLX were prepared and evaluated according to the method described by M Hanif and M Zaman in 2017, M Zaman, M Hanif and AA Qaiser in 2016[ 6 , 7 ]. Same method was followed for the formulation of bilayer films.…”

Application of quasi-emulsification and modified double emulsification techniques for formulation of tacrolimus microsponges

“…That is why an increase in the concentration of polymer causes a decrease in the release of drug from reservoir and vice versa. 22,23 Dissolution kinetics hold great potential in depicting how drug delivery systems show their viability by making drug available at biological sites for required actions. Globally, kinetic models are used in forecasting the release pattern of drug and the underlying mechanisms.…”

In vitro and ex vivo assessment of hydrophilic polymer‐ and plasticizer‐based thin buccal films designed by using central composite rotatable design for the delivery of meloxicam

“…The mathematical form of the MLRA model is given as [9,25,26] where, β 0 , the intercept (demonstrating the mathematical mean of all numerical outcomes of 13 trials), β 1 and β 2 were the coefficients (calculated from the observed experimental values of Y), and X 1 and X 2 were coded levels of the independent variable(s). Polynomial equation, including interaction and quadratic factors were studied for all the response variables using the multiple linear regression analysis (MLRA) approach.…”

“…It was measured by folding the film again and again at the same point until a crack appeared at that point, and the number of folds were counted and recorded. [26,43]…”