Technology of Orodispersible Polymer Films with Micronized Loratadine—Influence of Different Drug Loadings on Film Properties

Abstract

The production of orodispersible films (ODFs) with suspended insoluble drug substances is still a challenge, mainly due to the difficulty associated with achieving a proper homogeneity and mechanical properties of the films. Hypromellose (HPMC) and a mixture of polyvinyl alcohol (AP) and povidone (PVP) were compared in terms of their suitability for ODFs incorporating suspended micronized loratadine (LO) in a concentration range of 10%–40%. In a planetary mixer (Thinky), a uniform dispersion of LO in an aqueous viscous casting solution was obtained. The suspended LO particles caused dose-dependent changes in the viscosity of the casting mass and affected the mechanical quality of ODFs. Drug concentrations higher than 30% reduced the film flexibility and tear resistance, depending on the polymer type. LO films with a thickness of 100 µm disintegrated within 60-100 s, with no significant influence of the LO content in the range 10%–30%. HPMC films, regardless of the drug concentration, met the pharmacopoeial requirements regarding the uniformity of the drug content. AP/PVP films were too elastic, and the drug content uniformity was not achieved. The conclusion is that, using an HPMC matrix, it is possible to obtain a high load of a poorly water-soluble drug (30% of dry film mass corresponds to a dose of 5 mg per 1.5 cm2) in ODFs characterized by proper physical characteristics.

Hydroxypropyl Methylcellulose E15: A Hydrophilic Polymer for Fabrication of Orodispersible Film Using Syringe Extrusion 3D Printer

“…This may be due to the disruption of the polymeric matrix continuity when drug particles were incorporated. This result was consistent with the previous studies showing that the addition of the drug to the formulations significantly influenced the mechanical properties of the film by decreasing the tensile strength and increasing the film’s brittleness [ 22 , 23 , 24 ].…”

Bilayer Mucoadhesive Buccal Film for Mucosal Ulcers Treatment: Development, Characterization, and Single Study Case

“…The viscosity results of the polymeric gel-like solution are shown in Table 3 . The polymeric gel-like blend was prepared to bring together the best properties of each of the polymers as well as to provide synergistic actions among them, ensuring adequate flow behavior for the formation of the film [ 27 ].…”

“…The viscosity results of the polymeric gel-like solution are shown in Table 3. The polymeric gel-like blend was prepared to bring together the best properties of each of the polymers as well as to provide synergistic actions among them, ensuring adequate flow behavior for the formation of the film [27]. The high viscosity and film-forming ability of polymers without drugs (P-film monolayer and P-film bilayer) is a result of the interactions between the polymer chains, decreasing the intermolecular spaces and increasing the entanglement.…”

Production of Itraconazole Nanocrystal-Based Polymeric Film Formulations for Immediate Drug Release

“…For the selection of the nanosuspension concentration in the film casting mixture, it was noticed that higher drug loadings generally required longer dissolution times for total drug release and, if the amount of the drug particles in the film was above 30% ( w/w ), the film tended to be brittle [ 5 , 12 , 25 ]. Poloxamers’ impact on the HPMC film structure was assumed to be a result of HPMC–poloxamer interaction, which results in a higher resistance in the gel, retards the erosion, and improves the film-forming ability [ 26 ].…”

“…The formulated films disintegrated within 30 s and the dissolution was fast [ 11 ]. However, the production of film formulations with (nano)particle dispersions is challenging, due to the difficulty in reaching high homogeneity and because of the mechanical properties of the films [ 12 ].…”