Orodispersible Films: A Delivery Platform for Solid Lipid Nanoparticles?

To overcome the poor bioavailability observed for many newly developed active pharmaceutical ingredients (APIs), an appropriate formulation strategy is necessary. One approach is the formulation of these substances in solid lipid nanoparticles and their further processing into solid dosage forms. A promising and innovative oral delivery platform could be orodispersible films (ODFs). ODFs were already investigated more closely, e.g., for the administration of API nanoparticles, and proved their suitability for this formulation approach. The current study was aimed at investigating if the HPMC (hydroxypropyl methyl cellulose) film matrix is also suitable to serve as an appropriate delivery platform for solid lipid nanoparticles. Dependent on the type of triglyceride nanoparticles embedded in the film matrix and the formulation of the lipid particles, lipid contents of up to 54 wt.% could be realized in the film matrix without the loss of the nanoparticulate state. Good mechanical properties were confirmed for these films by determining the tensile strength as well as the elongation before breakage. Interestingly, processing of a lipid suspension into this solid dosage form led to a significantly reduced transformation of the lipid particles from the metastable α- into the stable β-polymorph. This could prove very beneficial when the lipid particles are loaded with APIs.

Characterization of Hydrophilic Polymers as a Syringe Extrusion 3D Printing Material for Orodispersible Film

The application of hydrophilic polymers in designing and three-dimensional (3D) printing of pharmaceutical products in various dosage forms has recently been paid much attention. Use of hydrophilic polymers and syringe extrusion 3D printing technology in the fabrication of orodispersible films (ODFs) might hold great potential in rapid drug delivery, personalized medicine, and manufacturing time savings. In this study, the feasibility of 3D-printed ODFs fabrication through a syringe extrusion 3D printing technique and using five different hydrophilic polymers (e.g., hydroxypropyl methylcellulose E15, hydroxypropyl methylcellulose E50, high methoxyl pectin, sodium carboxymethylcellulose, and hydroxyethylcellulose) as film-forming polymers and printing materials has been investigated. Rheology properties and printability of printing gels and physicochemical and mechanical properties of 3D-printed ODFs were evaluated. Amongst the investigated hydrophilic polymers, sodium carboxymethylcellulose at a concentration of 5% w/v (SCMC-5) showed promising results with a good printing resolution and accurate dimensions of the 3D-printed ODFs. In addition, SCMC-5 3D-printed ODFs exhibited the fastest disintegration time within 3 s due to high wettability, roughness and porosity on the surface. However, the results of the mechanical properties study showed that SCMC-5 3D printed ODFs were rigid and brittle, thus requiring special packaging to prevent them from any damage before practical use.

Preparation and Characterization of Orodispersible Films Loaded Diclofenac Sodium/β-Cyclodextrin Inclusion Complexes

Orodispersible films (ODFs) is orally pharmaceutical dosage form that rapidly disintegrates and instantly releases the drug when placed on the tongue. This study was firstly aimed to investigate physicomechanical properties of ODFs containing diclofenac sodium/β-cyclodextrin (DS/βCD) inclusion complexes prepared by solvent casting method. The influence of plasticizer, βCD and DS on hydroxypropyl metlhycellulose (HPMC) film was studied. Increasing of plasticizer concentration (e.g. PEG400 amd glycerol) resulted in decrement of disintegration time, strength and elasticity of HPMC films. When βCD was incorporated, opaque films were observed. Presence of βCD resulted in degrading of physicomechanical properties, except percentage of elongation representing the film’s elasticity. βCD films containing DS (DS/βCD films) were more brittle and transparent than blank βCD films. Amount of incorporated DS influenced on disintegration time and strength of obtained films. Cross-section scanning electron microscope (SEM) photomicrographs showed spherical particles scattered on DS/βCD films illustrating the occurrence of DS/βCD inclusion complexes during casting process. The DS/βCD inclusion complexes were then confirmed in both solid and solution. Furthermore, DS/βCD ODFs were prepared by incorporation of artificial sweeteners in DS/βCD films. It was found that DS/βCD ODFs containing xylitol were more brittle and their disintegration times were faster then those containing sucralose. Dissolution profiles were investigated then reported that release kinetic of DS/βCD films and ODFs were fitted to Higuchi model. In summary, the βCD-based ODFs containing DS were successfully developed.

Resveratrol Nanocrystal Loaded Orodispersible Films: Formulation Development and In Vitro Characterization

Nanocrystals are a feasible system to improve the aqueous solubility of poorly soluble compounds. Orodispersible films (ODFs) offer a rapid release of the drug in the mouth and are preferred for patients with dysphagia or paediatrics. The objective of the current study was to develop resveratrol (RES) nanocrystal-loaded ODFs. RES nanocrystals were prepared by antisolvent precipitation in the existence of Poloxamer 188 as a polymeric stabilizer. Polyvinyl alcohol was used for the preparation of the ODFs by using the solvent casting method. Then, RES nanocrystals were incorporated into the films. Particle size (PS), polydispersity index (PDI), and zeta potential (ZP) values were measured for nanocrystals. ODFs were characterized, and bioadhesion, disintegration, and in vitro release studies were performed. RES nanocrystals were obtained with 631 nm PS, 0.314 PDI and − 14.3 ZP values. Over 90% of RES nanocrystals were loaded in ODFs, which were approximately 75 µm in thickness. The thermal and crystal properties of nanocrystals in ODFs were preserved regarding DSC and FTIR analyses. Homogenous distribution in smooth films was observed on SEM. Mechanical properties and bioadhesion forces were found to be appropriate for ODFs. The disintegration time was found below 30 seconds for nanocrystal loaded films. RES nanocrystal loaded film formulations showed > 85% release in 5 minutes, significantly higher (p < 0.05) than those prepared with coarse RES. Novel RES nanocrystal-loaded ODFs can be a promising delivery system for use as an antioxidant with improved patient compliance by increasing solubility and physical stability of RES.

“Success Depends on Your Backbone”—About the Use of Polymers as Essential Materials Forming Orodispersible Films

Polymers constitute a group of materials having a wide-ranging impact on modern pharmaceutical technology. Polymeric components provide the foundation for the advancement of novel drug delivery platforms, inter alia orodispersible films. Orodispersible films are thin, polymeric scraps intended to dissolve quickly when put on the tongue, allowing them to be easily swallowed without the necessity of drinking water, thus eliminating the risk of choking, which is of great importance in the case of pediatric and geriatric patients. Polymers are essential excipients in designing orodispersible films, as they constitute the backbone of these drug dosage form. The type of polymer is of significant importance in obtaining the formulation of the desired quality. The polymers employed to produce orodispersible films must meet particular requirements due to their oral administration and have to provide adequate surface texture, film thickness, mechanical attributes, tensile and folding strength as well as relevant disintegration time and drug release to obtain the final product characterized by optimal pharmaceutical features. A variety of natural and synthetic polymers currently utilized in manufacturing of orodispersible films might be used alone or in a blend. The goal of the present manuscript was to present a review about polymers utilized in designing oral-dissolving films.