Mechanical, optical, and physicochemical properties of HPMC-based doxazosin mesylate orodispersible films

Abstract

In this study, orodispersible films formed from hydroxypropyl methylcellulose (HPMC) E6 (2, 2.5, and 3%) and plasticizers ((glycerin (Gly), propylene glycol (PP), or polyethylene glycol (PEG)), containing doxazosin mesylate, were prepared by the solvent casting method and characterized. Design of experiments (DoE) was used as a statistical tool to facilitate the interpretation of the experimental data and allow the identification of optimal levels of factors for maximum formulation performance. Differential scanning calorimetry (DSC) curves and X-ray powder diffraction (XRPD) diffractograms showed doxazosin mesylate amorphization, probably due to complexation with the polymer (HPMC E6), and the glass transition temperature of the polymer was reduced by adding a plasticizer. Fourier transformed infrared (FTIR) spectroscopy results showed that the chemical structure of doxazosin mesylate was preserved when introduced into the polymer matrix, and the plasticizers, glycerin and PEG, affected the polymer matrix with high intensity. The addition of plasticizers increased the elongation at break and adhesiveness (Gly > PEG > PP), confirming the greater plasticizer effect of Gly observed in DSC and FTIR studies. Greater transparency was observed for the orodispersible films prepared using PP. The addition of citric acid as a pH modifier was fundamental for the release of doxazosin mesylate, and the desirability formulation had a release profile similar to that of the reference product.

A comparison between solvent casting and electrospinning methods for the fabrication of HPMC fast-dissolving films: investigation of the physicochemical, mechanical and drug release characteristics

“…The FTIR spectrum of bisoprolol fumarate shows O-H stretching vibration in the range of 3300-2200 cm −1 , C=C aromatic skeletal vibration at 1610 and 1512 cm −1 , CH 2 vibration at 1462 cm −1 , C-O(H) stretching at 1248 cm −1 , C-O-C stretching vibration at 1045 cm −1 and = CH out of plain CH vibration of 1,4-disubstituted aromatic ring at 814 cm −1 [27]. For the HPMC spectrum, broad bands centered at 3451, and 2880 cm −1 indicate -OH vibrational stretching and a band between 1000-1100 cm −1 centered at 1064 cm −1 represent the stretching vibration of C-O-C groups [28]. In the case of PEG, the spectra had intense peaks at 3421 cm −1 and 1112 cm −1 due to the hydroxyl group and etheric link (C-O-C), respectively [29].…”