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A nanosystem for water-insoluble drugs prepared by a new technology, nanoparticulation using a solid lipid and supercritical fluid

Authors
 Joo Won Park  ;  Jeong Min Yun  ;  Eun Seong Lee  ;  Yu Seok Youn  ;  Kab Sig Kim  ;  Young Taik Oh  ;  Kyung Teak Oh 
Citation
 ARCHIVES OF PHARMACAL RESEARCH, Vol.36(11) : 1369-1376, 2013 
Journal Title
 ARCHIVES OF PHARMACAL RESEARCH 
ISSN
 0253-6269 
Issue Date
2013
MeSH
Antifungal Agents/chemistry ; Biological Availability ; Chemistry, Pharmaceutical/methods* ; Itraconazole/chemistry* ; Lipids/chemistry* ; Nanoparticles/chemistry* ; Nanoparticles/ultrastructure ; Nanotechnology/methods* ; Particle Size ; Solubility ; Water/chemistry
Keywords
Antifungal Agents/chemistry ; Biological Availability ; Chemistry, Pharmaceutical/methods* ; Itraconazole/chemistry* ; Lipids/chemistry* ; Nanoparticles/chemistry* ; Nanoparticles/ultrastructure ; Nanotechnology/methods* ; Particle Size ; Solubility ; Water/chemistry
Abstract
While the number and diversity of lead compounds has increased with the development of science technologies, ca. 90 % ofnew chemical entities under development have shown low aqueous solubility, classified as class II or IV of the biopharmaceutics classification system (BCS). The low aqueous solubility hinders their clinical translations due to low bioavailability and dissolution-limited absorption of orally-administered drugs. Several technologies have been employed to improve the solubility of poorly water-soluble drugs. In this paper, a new method of nanoparticulation using fat and a supercritical fluid (NUFS) for the formulation of hydrophobic drugs was applied to solve the low solubility problem. A typical BCS class II drug, itraconazole, was selected and formulated with hydroxypropyl methylcellulose, emulsification, and anticoagulating agents for NUFS. The non-spherical itraconazole nanoparticles prepared by NUFS were ~300-500 nm in size with a ~15-fold improved dissolution rate compared to non-nanoparticles of itraconazole (i.e., raw itraconazole). In addition, a high drug content of ~46 % by weight and a drug loading efficiency greater than 85 % were achieved. Therefore, the new technology for nano-platforms could be a promising solution for solubilization of poorly water-soluble drugs, resulting in improved bioavailability.
Full Text
http://link.springer.com/article/10.1007%2Fs12272-013-0187-2
DOI
10.1007/s12272-013-0187-2
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Radiology (영상의학교실) > 1. Journal Papers
Yonsei Authors
Oh, Young Taik(오영택) ORCID logo https://orcid.org/0000-0002-4438-8890
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/88543
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