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.

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About the article: Steiner, D.; Emmendörffer, J.F.; Bunjes, H. Orodispersible Films: A Delivery Platform for Solid Lipid Nanoparticles? Pharmaceutics 2021, 13, 2162. https://doi.org/10.3390/pharmaceutics13122162

Materials
The three different triglycerides tristearin (Dynasan® 118), tripalmitin (Dynasan® 116) and trimyristin (Dynasan® 112) were used in this study. All were from Hüls AG/Cremer Oleo (Witten, Germany) and kind gifts from the manufacturer. For lipid particle stabilization the following stabilizers were investigated: hydroxypropyl methyl cellulose Pharmacoat 606 (HPMC; Shin-Etsu Chemical Eo., Tokyo, Japan; kind gift from Harke Pharma, Mühlheim, Germany), polyvinylpyrrolidone Kollidon® 30 (PVP; BASF, Ludwigshafen, Germany), vinylpyrrolidone-vinyl acetate copolymers Kollidon®VA 64 (KVA 64; BASF, Ludwigshafen, Germany), polyvinyl alcohol Mowiol 3-83 (PVA, Kuraray Europe GmbH, Hattersheim, Germany; kind gift from the manufacturer), poloxamer 188 (P188, BASF, Ludwigshafen, Germany; kind gift from the manufacturer), polysorbate 80 (Tween80, Caesar & Loretz GmbH, Hilden, Germany) and sodium dodecyl sulphate (SDS, Roth, Karlsruhe, Germany). For the preparation of ODFs, the film-forming polymer HPMC and the plasticizer glycerol (Roth, Karlsruhe, Germany) were used. All formulations were prepared with distilled water.