Different trends for preparation of budesonide pellets with enhanced dissolution rate

The current research attempts different approaches to overcome the poor dissolution of budesonide (a poorly water-soluble drug) from pellet formulations. Various methods such as liqui-pellet (LP) and pellets made of solid dispersion (SDP) were employed and compared to conventional pellets (CP). In SDP method, budesonide:PVP solid dispersion was prepared followed by extrusion-pelletization. Solid dispersion of budesonide-PVP was also layered to the surface of placebo pellets (LSDP). In LP technique, budesonide dispersed in PEG 400 was mixed with Avicel or Avicel lactose and was extruded-spheronized. Pellets were evaluated for their shape, size, mechanical properties and dissolution rate. The pellets made by LSDP method were significantly harder than CP or PSDP.

Highlights

• Different approaches for budesonide pellet preparation were investigated.
• Conventional pellets and pellets containing solid dispersion of drug:PVP K30 showed similar release rates.
• Liqui-pellet formulations with higher dissolution rate demonstrated weak mechanical properties.
• Solid dispersion layering on placebo pellets was the most successful approach for dissolution enhancement.

LP with a loading factor greater than 0.34 was very soft compared to CP and SDP. Pelletization of budesonide SD (PSDP) did not have a tremendous effect on the dissolution enhancement of budesonide compared to CP whilst LSDP showed faster drug release. In conclusion, the layering of budesonide solid dispersion on placebo pellets (LSDP) was the most promising approach for the production of pellets with the highest dissolution rate so that more than 80% of the drug was released within the first 5 min. Also this formulation had proper mechanical properties. This method has the capability to overcome the poor dissolution of budesonide associated with the pellet containing Avicel, and could be employed for the dissolution enhancement of other poorly water-soluble drugs in pellet form.

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Materials

Budesonide was obtained from Jaber Ebne Hayyan Pharmaceutical Company (Tehran, Iran). Lactose monohydrate (Merck Millipore, Germany), Avicel pH 102 (Merck Millipore, Germany), polyvinylpyrrolidone (PVP K30) (Rahavard Tamin, Iran), polyethylene glycol 400 (PEG 400) (Dr. Mojallaly, Iran), colloidal silicon dioxide (Aerosil 300), (Evonik Industries AG, Hanau, Germany), and sodium lauryl sulfate (SLS) (Scharlau, Spain) were used. All other reagents and solvents were of analytical grades.

Fatemeh Soltani, Hossein Kamali, Abbas Akhgari, Hadi Afrasiabi Garekani, Ali Nokhodchi, Fatemeh Sadeghi,
Different trends for preparation of budesonide pellets with enhanced dissolution rate,
Advanced Powder Technology, Volume 33, Issue 8, 2022, 103684, ISSN 0921-8831,
https://doi.org/10.1016/j.apt.2022.103684.