Development of Paediatric Formulation of Baclofen for Improved Safety and Palatability

PurposeThe aim of present investigation was to develop oral jelly containing Baclofen-loaded chitosan microspheres for bioavailability enhancement, sustained release, and improved palatability. This is expected to improve the patient compliance by overcoming the difficulties in swallowing. Preformulation studies were performed for drug authentication.MethodsMicrospheres were prepared by emulsification thermal crosslinking method, and optimization of the parameters was done using 3(2) factorial design. The optimized formulation of microspheres was characterized for size, shape, drug content, in vitro drug dissolution, surface morphology, mucoadhesion, and micromeritic properties. The Baclofen microspheres were loaded in an oral jelly which possessed all the desired characteristics. In vivo pharmacokinetic study for the optimized batch and the marketed dosage form were performed in rabbits.ResultsThe in vivo result suggested that the oral bioavailability of jelly of Baclofen-loaded microspheres was 3.77 folds higher than that of the marketed formulation. Stability study of final optimized formulation indicated that the prepared formulation was stable at the storage conditions used.ConclusionThe developed formulation is a promising and paediatric patient compliant dosage form for improved safety and palatability of Baclofen.

Automated summary

The purpose of this study was to develop an oral jelly containing Baclofen-loaded chitosan microspheres to improve bioavailability, achieve sustained release, and enhance palatability. Preformulation studies were conducted for drug authentication. Microspheres were prepared using an emulsification thermal crosslinking method and optimized using factorial design. The optimized microsphere formulation was characterized for various properties and loaded into an oral jelly. In vivo pharmacokinetic studies showed that the bioavailability of the jelly with Baclofen-loaded microspheres was 3.77 times higher than that of the marketed formulation.