Skip to main content

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

Download Article:
 Download
(PDF 326.7 kb)
 

Abstract:

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.

Document Type: Research Article

DOI: http://dx.doi.org/10.1691/ph.2008.8029

Affiliations: 1: College of Pharmacy, Soochow University, Jiangsu, Suzhou, China 2: College of Pharmacy, Soochow University, Jiangsu, Suzhou, 215123, China, Email: zhangxuenong@163.com

Publication date: January 1, 2009

More about this publication?
  • Pharmazie is one of the world's leading pharmaceutical journals. As a peer-reviewed scientific journal, DiePharmazie is regularly indexed in Current Contents/Life Sciences, Excerpta Medica, Analytical Abstracts, International Pharmaceutical Abstracts, Beilstein Current Facts in Chemistry, Chemical Engineering and Biotechnology Abstracts (CEABA) and Science Citation Index.
  • Information for Authors
  • Submit a Paper
  • Subscribe to this Title
  • Terms & Conditions
  • Ingenta Connect is not responsible for the content or availability of external websites
govi/pharmaz/2009/00000064/00000001/art00005
dcterms_title,dcterms_description,pub_keyword
6
5
20
40
5

Access Key

Free Content
Free content
New Content
New content
Open Access Content
Open access content
Subscribed Content
Subscribed content
Free Trial Content
Free trial content
Cookie Policy
X
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more