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Mechanistic insights into drug loading effect on dissolution performance of Loratadine–Soluplus® amorphous solid dispersions
Journal article   Peer reviewed

Mechanistic insights into drug loading effect on dissolution performance of Loratadine–Soluplus® amorphous solid dispersions

Jannat Falah Hassan, Kawther Khalid Ahmed and Tze Ning Hiew
Journal of pharmaceutical sciences, Vol.115(3), 104188
03/01/2026
DOI: 10.1016/j.xphs.2026.104188
PMID: 41621710

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Abstract

•Low drug load (3–5 %) resulted in fast, congruent loratadine–Soluplus® release.•High drug load (10–15 %) slowed release and caused incongruent polymer-first behavior.•Larger LLPS droplets at high load destabilized supersaturation, leading to precipitation.•Intrinsic dissolution, DLS, and SEM/EDX together offer a straightforward approach to probe drug–polymer interplay in ASD performance, providing a framework to guide formulations of other poorly water-soluble drugs. Amorphous solid dispersions (ASDs) hold promising potential towards modulating the solubility of poorly soluble drugs. However, their use is limited by poor understanding of release mechanism and kinetics, especially with Soluplus®. In this study, we explored loratadine–Soluplus® ASDs with different drug loadings (DLs) from 3% to 15% to unveil drug content impact on dissolution, colloidal behavior, and surface composition. All formulations were fully amorphous and showed a single, composition-dependent glass transition temperature. Intrinsic dissolution testing revealed fast, nearly complete release and stable supersaturation for low-load ASDs (3–5% DL), while higher-load ASDs (10–15% DL) released more slowly, generated larger nanodroplets on liquid–liquid phase separation (LLPS), and showed precipitation upon standing. SEM imaging suggested similar surface morphology before and after partial dissolution, but EDX elemental analysis revealed congruent drug–polymer release at low DL and incongruent (polymer-first) release at high DL. These findings identify an optimum drug-loading window where ASD generates and sustains supersaturation status for loratadine, and highlight mechanistic links between DL, LLPS droplet size, and incongruent release that explain reduced performance at higher loadings.
 Amorphous solid dispersion Congruent release Intrinsic dissolution Liquid–liquid phase separation Loratadine Soluplus

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