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Open Access Preparation of an alternative freeze-dried pH-sensitive cyclosporine A loaded nanoparticle formulation and its pharmacokinetic profile in rats

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This work aimed to produce and develop new pH-sensitive cyclosporine A (CyA) loaded nanoparticles (CyA-NP) based on the enterically soluble copolymer Eudragit® S100 and to improve the poor bioavailability of lipophilic CyA. CyA-NP and freeze-dried nanoparticles (Lac-CyA-NP, 3% lactose as cryoprotectant) were prepared using a quasi-emulsion solvent diffusion technique and freeze-drying. The encapsulation efficiency, particle size and in vitro release characteristics from the vehicle of CyA were studied individually. The bioavailability of CyA-NP and Lac-CyA-NP was evaluated in rats at a dose of 15 mg/kg as compared to Neoral®. The mean particle size of CyA-NP was 44 ± 3 nm, while the encapsulation efficiency reached 99.7%. The particle size and encapsulation efficiency of the freeze-dried formulation remained relatively stable by using 3% lactose (W/V) as a cryoprotective agent before freeze-drying and after dissolving. Significantly pH-dependent release profiles were revealed when the pH of the medium was above 6.0. The relative bioavailabilities of CyA-NP and Lac-CyA-NP were 162.1% and 130.1% compared with Neoral® after oral administration at the same dosage. The results showed that the pH-sensitive CyA-loaded nanoparticles were a potential vehicle for developing a high performance CyA carrier system.
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Document Type: Research Article

Affiliations: 1: College of Pharmacy, Soochow University, Jiangsu, Suzhou, China 2: College of Pharmacy, Soochow University, Jiangsu, Suzhou, 215123, China, Email: [email protected]

Publication date: 2009-01-01

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  • Pharmazie is a leading journal in the field of pharmaceutical sciences. As a peer-reviewed scientific journal, Pharmazie is regularly indexed in the relevant databases like Web of science, Journal Citation Reports and many others. The journal is open for submissions from the whole spectrum of pharnaceutical sciences including Pharmaceutical Chemistry, Experimental and Clinical Pharmacology, Drug Analysis, Pharmaceutics, Pharmaceutical Biology, Clinical Pharmacy etc.
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