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Two Novel Freeze-Dried pH-Sensitive Cyclosporine A Nanoparticles: Preparation, in vitro Drug Release, and in vivo Absorption Enhancement Effects

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Abstract:

The present study was aimed at preparation and performance evaluation of pH-sensitive cyclosporine A (CyA) nanoparticles (CyA-NPs) to improve the poor bioavailability of lipophilic CyA. CyA-NPs were prepared with two types of Eudragit® copolymers (Eudragit ® S100 and Eudragit® L100) by a quasi-emulsion solvent diffusion technique. Freeze-dried formulations (Lac-CyA-S100-NP and Lac-CyA-L100-NP) were also prepared. The physical properties, particle size, encapsulation efficiency, and in vitro drug release characteristics were studied. The in vivo bioavailability of CyA-NP and Lac-CyA-S100-NP was investigated in rats at a dose of 15 mg/kg and compared with that of the commercial formulation, Sandimmune Neoral®. The mean particle size of the CyA-NPs was less than 50 nm, and the encapsulation efficiency was over 99%. Characteristics of the freeze-dried nanoparticles were found to remain relatively stable when lactose was used as a cryoprotectant. In vitro release studies revealed that the CyA-NPs exhibited significant pH-sensitivity. The relative bioavailabilities of CyA-L100-NP, CyA-S100-NP, and Lac-CyA-S100-NP were 117.3%, 162.1%, and 130.1%, respectively, when compared with that of Neoral®. Therefore, CyA-NPs were considered to be promising oral delivery systems for enhancement of the absorption of the poorly soluble drug, CyA. Freeze-dried nanoparticles could be developed into a novel and effective CyA formulations.





Keywords: Nanoparticle; bioavailability; cyclosporine A; enhancement absorption; freeze-drying; pharmacokinetics

Document Type: Research Article

DOI: http://dx.doi.org/10.2174/157341309789378140

Publication date: November 1, 2009

More about this publication?
  • Current Nanoscience publishes authoritative reviews and original research reports, written by experts in the field on all the most recent advances in nanoscience and nanotechnology. All aspects of the field are represented including nano- structures, synthesis, properties, assembly and devices. Applications of nanoscience in biotechnology, medicine, pharmaceuticals, physics, material science and electronics are also covered. The journal is essential to all involved in nanoscience and its applied areas.
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