EXPLORATORY QUALITY BY DESIGN STUDY OF LIDOCAINE HYDROCHLORIDE EMULGELS Original scientific paper
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A quality by design/quality risk management-driven early-stage screening was conducted for 4% lidocaine hydrochloride (LHCl) oil-in-water emulgels intended for topical use. A quality target product profile was established and critical quality attributes defined to ensure efficacy, safety, and patient acceptability. Nine formulations (B1–B9) were developed to evaluate the influence of key critical material attributes, Carbopol 940, Tween 80, cetostearyl alcohol (CA), and isopropyl myristate (IPM), on physicochemical properties, rheology, spreadability, and in vitro drug release. All formulations showed acceptable pH, homogeneity, and drug content. Droplet size and polydispersity depended strongly on excipient composition: higher Carbopol and CA increased droplet size, whereas Tween 80 reduced it. Amplitude sweep measurements demonstrated elastic-dominant behavior within the linear viscoelastic region; Carbopol and CA enhanced viscoelastic strength and yield stress, while Tween 80 and IPM exhibited a plasticizing effect. Spreadability was comparable across formulations and reflected shear-thinning behavior. In vitro dissolution revealed formulation-dependent LHCl release, with stronger gel networks associated with slower release. Correlation analysis confirmed significant relationships between CA content, rheological parameters, droplet size, and drug release. Overall, LHCl emulgels can be rationally designed using a quality by design (QbD) approach, with rheology and droplet size serving as key determinants of performance.
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