QbD Approach for Development of a Mucoadhesive Thermosensitive Gel for Oral Application: Risk Assessment Followed by Screening and Optimization

基于质量源于设计(QbD)的口腔用粘膜粘附性温敏凝胶开发:风险评估、筛选和优化

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Abstract

The study aimed to develop a mucoadhesive thermosensitive buccal gel capable of forming an artificial clot after application in the extraction socket and providing prolonged release for metronidazole (MZ) and ibuprofen (IB). The critical quality attributes of the product were systematically evaluated using Ishikawa (cause-effect) diagrams as a risk assessment tool, considering the factors related to the formulation, process, and methodology. Subsequently, Failure Mode and Effects Analysis (FMEA) was used to identify the critical parameters of the formulation and process characterized by a high probability of occurrence and a significant impact on product performance. The influence of qualitative and quantitative formulation variables was further investigated using two experimental designs, applied for both screening and optimization purposes. The rheological, adhesion, and in vitro release properties of the drugs were studied, and the optimized formulation for these characteristics contains Poloxamer 407 20.99% and HPMC K100M:K4M 1:1, 0.74%. The release of MZ and IB was prolonged over 8 h and followed Peppas's kinetics. The optimized formula had an appropriate pH and an acceptable ex vivo mucoadhesion time. Stability studies revealed the preservation of mechanical properties and a recovery coefficient for MZ and IB of over 90%, after 12 months of storage. The optimized formula may be a potential candidate for the prevention of alveolar osteitis.

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