Pharmaceutics · 2026
Milling-Induced Chitosan-HPMC Microstructural Organisation Determines the Stability Window of Concentrated Azelaic Acid Nanosuspensions.
СтатьяНазвание и аннотация: Перевод в очереди
Обработка статьи · этапы, ошибки и управление
Загрузка состояния…
Ошибки и ограничения
История · было → стало
Состояние обновляется каждые 5 секунд, пока блок открыт. Процент показывается только там, где известен объём работы. Пауза останавливает продолжение этапа; текущий запрос к источнику может завершиться.
Miočić Sandra, Rašić Andrea, Torić Jelena, Abrami Michela, Ferderber Kristina, Cetina-Čižmek Biserka, Grassi Mario, Filipović-Grčić Jelena
Аннотация
Objectives: The physical stability of concentrated azelaic acid nanosuspensions cannot be predicted solely from interfacial stabilisation but reflects the interplay between particle size-dependent thermodynamic driving forces, polymer-mediated rheological structuring and the resulting bulk microstructural organisation. This study employed an A-optimal design of experiments (18 runs) to investigate formulation-process relationships in concentrated azelaic acid nanosuspensions (10-20% w/w) stabilised with a dual HPMC-chitosan system. Methods: Particle size, ζ-potential, rheological behaviour, solid-state properties and in vitro permeation across Strat-M® membranes were evaluated, and formulation-process relationships were analysed using multivariate modelling and logistic regression. Results: Particle size (342-1118 nm; R2 = 0.97) was primarily governed by the applied milling regime. Logistic regression demonstrated a size-dependent probability of crystal growth, with the estimated particle-size transition point (predicted probability = 0.5) shifting from approximately 424 nm after preparation to 594 nm following accelerated storage at 40 °C. CHI concentration controlled ζ-potential (+18.5 to +47.9 mV), although ζ-potential alone did not adequately explain the observed storage stability. Where measurable, zero-shear viscosity (68-45,462 mPa·s) reflected substantial differences in low-shear rheological structuring, while formulations containing higher HPMC concentrations generally exhibited improved stability, consistent with polymer-mediated kinetic constraints on crystal growth. In vitro permeation studies using Strat-M® membranes demonstrated permeation behaviour consistent with structured diffusion-controlled systems, exhibiting lower flux but more uniform permeation profiles than the reference formulation under the applied experimental conditions. Conclusions: Integration of multivariate modelling with rheological, solid-state and permeation characterisation provided an integrated understanding of the formulation-process relationships governing the short-term physical stability and comparative in vitro transport behaviour of concentrated dermal AZA nanosuspensions.