A novel orodispersible film load with dual-coated sustained-release microparticles for pediatric drug delivery

Abstract

Orodispersible films (ODFs), easy to administer, flexible in dosage, and free of choking and aspiration risks, have drawn widespread attention as pediatric formulations. However, it is a great challenge to endow ODFs with sustained release due to their fast disintegration. Herein, we designed a novel orodispersible film load with dual-coated sustained-release microparticles (SRMPs) for children using topiramate as a model drug.

Highlights

• SRMPs are fabricated with a pellet core, a drug layer, and a coating layer.
• The release mechanism of SRMPs is elucidated.
• SRODFs exhibit good formability, mechanical properties, and palatability.
• The factors influencing release of SRODFs are explored.
• A strong in vivo-in vitro correlation of the SRODFs is established.

SRMPs with a particle size of 98.32 ± 0.22 µm, fabricated with a pellet core, a drug layer, and a coating layer, were prepared by two microparticle coating steps. The sustained-release orodispersible films (SRODFs) with uniform distribution of SRMPs and favorable disintegration time showed good formability, mechanical properties, and palatability. The factors affecting drug release of the SRMPs and the SRODFs were further explored.

More importantly, pharmacokinetics study in human demonstrated that, although the SRODFs had a longer mean retention time, they were bioequivalence compared with the commercially available extended-release products (Qudexy® XR). A strong in vivo-in vitro correlation of the SRODFs was established. Notably, the SRODFs can be loaded with other drugs other than topiramate, offering a promising formulation option for pediatric patients with different diseases.

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Materials

Microcrystalline cellulose pellet core (MCCPC) was a gift from Changsha Jingyi Pharmaceutical Technology Co., LTD. (Changsha, China). Hydroxypropyl methylcellulose (HPMC, SH-E5) was purchased from Anhui Sunhere Pharmaceutical Excipients Co., Ltd. (Hefei, China). Topiramate was purchased from MSN organics private Ltd. (Telangana, India). Triethyl citrate (TEC) and sucralose were purchased from Jiangxi Alpha Hi-tech Pharmaceutical CO., Ltd. (Pingxiang, China). Polyvinyl pyrrolidone (PVP, K30) was from JRS Pharma.

Qianmeng Huang, Peng Yan, Youshan Li, Jinsong Ding, A novel orodispersible film load with dual-coated sustained-release microparticles for pediatric drug delivery, International Journal of Pharmaceutics, Volume 677, 2025, 125654, ISSN 0378-5173, https://doi.org/10.1016/j.ijpharm.2025.125654.

Read also our introduction article on Disintegrants here: