Solubility enhancement of BCS Class II drug by solid phospholipid dispersions: Spray drying versus freeze-drying.
作者： Sophia Yui Kau Fong , Asiye Ibisogly , Annette Bauer-Brandl
DOI: 10.1016/J.IJPHARM.2015.10.029
关键词:
摘要: The poor aqueous solubility of BCS Class II drugs represents a major challenge for oral dosage form development. Using celecoxib (CXB) as model drug, the current study adopted novel solid phospholipid nanoparticle (SPLN) approach and compared effect two commonly used industrial manufacturing methods, spray- freeze-drying, on dissolution enhancement CXB. CXB was formulated with Phospholipoid E80 (PL) trehalose at different CXB:PL:trehalose ratios, which 1:10:16 optimal formulation. Spherical amorphous SPLNs average diameters <1μm were produced by spray-drying; while 'matrix'-like structures PL dispersion larger particle sizes prepared freeze-drying. Formulations from both methods significantly enhanced rates, apparent solubility, molecularly dissolved concentration in phosphate buffer (PBS, pH 6.5) biorelevant fasted state simulated intestinal fluid (FaSSIF, (p<0.05). While similar rates found, spray-dried had (29- to 132-fold) well molecular (18-fold) equilibrium strong capability attain 'true' supersaturation makes them promising bioavailability poorly soluble drugs.
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