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Preparation and evaluation of Eudragit L100-PEG proliponiosomes for enhanced oral delivery of celecoxib

Cited 5 time in Web of Science Cited 6 time in Scopus
Authors

Kim, Min-Hwan; Kim, Dong Hyun; Nguyen, Duy-Thuc; Lee, Han Sol; Kang, Nae-Won; Baek, Min-Jun; An, Jiseon; Yoo, So-Yeol; Mun, Yong-Hyeon; Lee, Wonhwa; Kim, Ki-Taek; Cho, Cheong-Weon; Lee, Jae-Young; Kim, Dae-Duk

Issue Date
2020-08
Publisher
Multidisciplinary Digital Publishing Institute (MDPI)
Citation
Pharmaceutics, Vol.12 No.8, pp.1-14
Abstract
PEGylated Eudragit L100 (ELP)-containing proliponiosomes (PLNs) were developed for improved oral delivery of celecoxib (CXB). The successful introduction of PEG 2000 or 5000 to Eudragit L100 (EL) was confirmed via proton nuclear magnetic resonance analysis of which calculated molar substitution ratio of PEG to EL was 36.0 or 36.7, respectively. CXB, ELP, phospholipid, and non-ionic surfactants were dissolved in dimethyl sulfoxide and lyophilized to produce CXB-loaded PLNs (CXB@PLNs). The physical state of CXB@PLNs was evaluated using differential scanning calorimetry and powder X-ray diffractometry, which revealed that crystalline CXB was transformed into amorphous form after the fabrication procedure. The reconstitution of CXB@PLNs in aqueous media generated CXB-loaded liponiosomes with nano-sized mean diameters and spherical morphology. CXB@PLNs displayed enhanced dissolution rate and permeability compared to CXB suspension. In vivo pharmacokinetic studies performed on rats demonstrated the improved oral bioavailability of CXB@PLNs compared to that of CXB suspension. No serious systemic toxicity was observed in the blood biochemistry tests performed on rats. These results suggest that the developed PLNs could be promising oral delivery systems for improving the bioavailability of poorly water-soluble drugs, such as CXB.
ISSN
1999-4923
URI
https://hdl.handle.net/10371/199477
DOI
https://doi.org/10.3390/pharmaceutics12080718
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  • College of Pharmacy
  • Department of Pharmacy
Research Area Biomaterial-based nano-platforms for cancer drug delivery and imaging, Formulation design and development, Functional protein expression and evaluation for drug delivery and therapy applications

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