Dissolution enhancement of the poorly soluble drug nifedipine by co-spray drying with microporous zeolite beta

Dissolution enhancement of nifedipine (NIF), a BSC class II drug, was achieved after co-spray drying with zeolite beta (BEA) in two drug to carrier ratios (1: 1, 1: 2). Extraction studies revealed almost 100% encapsulation efficiency. Physisorption studies suggested successful drug incorporation within the carrier's pore network, as well as on its external surface area. A shift of ζ-potential towards less negative values following drug loading indicated possible drug deposition onto zeolite's surface. The physical state of loaded NIF was evaluated by means of FT-IR, DSC and XRD analyses, all corroborating towards drug's significant amorphization.The in vitro dissolution rate of NIF from the co-spray dried formulations was substantially enhanced in simulated gastric (pH 1.2) and intestinal fluids (pH 6.8), compared to crystalline drug.Results demonstrated the potential of zeolitic particles for the dissolution enhancement of sparingly soluble drugs, which in turn may increase their oral bioavailability.

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