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, cyclosporine A, freeze-drying, enhancement absorption, pharmacokinetics, bioavailability
Current Nanoscience
Title: Two Novel Freeze-Dried pH-Sensitive Cyclosporine A Nanoparticles: Preparation, in vitro Drug Release, and in vivo Absorption Enhancement Effects
Volume: 5 Issue: 4
Author(s): Fang Zhi-gang, Pan Ping, Yang Zhi-qiang, Chen Ya-gen, Zhang Jian-kang, Wei Miao, Zhang Xue-nong and Zhang Qiang
Affiliation:
Keywords: Nanoparticle, cyclosporine A, freeze-drying, enhancement absorption, pharmacokinetics, bioavailability
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.
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Cite this article as:
Zhi-gang Fang, Ping Pan, Zhi-qiang Yang, Ya-gen Chen, Jian-kang Zhang, Miao Wei, Xue-nong Zhang and Qiang Zhang, Two Novel Freeze-Dried pH-Sensitive Cyclosporine A Nanoparticles: Preparation, in vitro Drug Release, and in vivo Absorption Enhancement Effects, Current Nanoscience 2009; 5 (4) . https://dx.doi.org/10.2174/157341309789378140
DOI https://dx.doi.org/10.2174/157341309789378140 |
Print ISSN 1573-4137 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6786 |
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