Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 496, Issue 2, Pages 382-391Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2015.10.029
Keywords
Solid phospholipid nanoparticles; Amorphous solid dispersion; Solubility; Spray-drying; Freeze-drying; Celecoxib
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Funding
- Phospholipid Research Centre, Heidelberg, Germany
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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 a novel solid phospholipid nanoparticle (SPLN) approach and compared the effect of two commonly used industrial manufacturing methods, spray- and freeze-drying, on the solubility and dissolution enhancement of CXB. CXB was formulated with Phospholipoid E80 (PL) and trehalose at different CXB: PL: trehalose ratios, of which 1: 10: 16 was the optimal formulation. Spherical amorphous SPLNs with average diameters <1 mu m were produced by spray- drying; while amorphous 'matrix'-like structures of solid PL dispersion with larger particle sizes were prepared by freeze-drying. Formulations from both methods significantly enhanced the dissolution rates, apparent solubility, and molecularly dissolved concentration of CXB in phosphate buffer (PBS, pH 6.5) and in biorelevant fasted state simulated intestinal fluid (FaSSIF, pH 6.5) (p < 0.05). While similar dissolution rates were found, the spray-dried SPLNs had a larger enhancement in apparent solubility (29- to 132-fold) as well as molecular solubility (18-fold) of CXB at equilibrium (p < 0.05). The strong capability of the spray-dried SPLNs to attain 'true' supersaturation state makes them a promising approach for bioavailability enhancement of poorly soluble drugs. (C) 2015 Elsevier B.V. All rights reserved.
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