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Volume 12
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10.3390/pharmaceutics12080718
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Article

Preparation and Evaluation of Eudragit L100-PEG Proliponiosomes for Enhanced Oral Delivery of Celecoxib

by
Min-Hwan Kim
1,†,
Dong Hyun Kim
2,†,
Duy-Thuc Nguyen
1,
Han Sol Lee
2,
Nae-Won Kang
1,
Min-Jun Baek
1,
Jiseon An
2,
So-Yeol Yoo
2,
Yong-Hyeon Mun
2,
Wonhwa Lee
3,
Ki-Taek Kim
4,
Cheong-Weon Cho
2,
Jae-Young Lee
2,* and
Dae-Duk Kim
1,*
1
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 08826, Korea
2
College of Pharmacy, Chungnam National University, Daejeon 34134, Korea
3
Aging Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejeon 34141, Korea
4
College of Pharmacy and Natural Medicine Research Institute, Mokpo National University, Jeonnam 58554, Korea
*
Authors to whom correspondence should be addressed.
†
These authors have contributed equally to this work.
Pharmaceutics 2020, 12(8), 718; https://doi.org/10.3390/pharmaceutics12080718
Submission received: 26 June 2020 / Revised: 24 July 2020 / Accepted: 29 July 2020 / Published: 30 July 2020
(This article belongs to the Special Issue PEGylation in Drug Delivery Systems)
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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.
Keywords: proliponiosomes; Eudragit L100; PEGylation; celecoxib; oral bioavailability proliponiosomes; Eudragit L100; PEGylation; celecoxib; oral bioavailability
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MDPI and ACS Style

Kim, M.-H.; Kim, D.H.; Nguyen, D.-T.; Lee, H.S.; Kang, N.-W.; Baek, M.-J.; An, J.; Yoo, S.-Y.; Mun, Y.-H.; Lee, W.; et al. Preparation and Evaluation of Eudragit L100-PEG Proliponiosomes for Enhanced Oral Delivery of Celecoxib. Pharmaceutics 2020, 12, 718. https://doi.org/10.3390/pharmaceutics12080718

AMA Style

Kim M-H, Kim DH, Nguyen D-T, Lee HS, Kang N-W, Baek M-J, An J, Yoo S-Y, Mun Y-H, Lee W, et al. Preparation and Evaluation of Eudragit L100-PEG Proliponiosomes for Enhanced Oral Delivery of Celecoxib. Pharmaceutics. 2020; 12(8):718. https://doi.org/10.3390/pharmaceutics12080718

Chicago/Turabian Style

Kim, Min-Hwan, Dong Hyun Kim, Duy-Thuc Nguyen, Han Sol Lee, Nae-Won Kang, Min-Jun Baek, Jiseon An, So-Yeol Yoo, Yong-Hyeon Mun, Wonhwa Lee, and et al. 2020. "Preparation and Evaluation of Eudragit L100-PEG Proliponiosomes for Enhanced Oral Delivery of Celecoxib" Pharmaceutics 12, no. 8: 718. https://doi.org/10.3390/pharmaceutics12080718

APA Style

Kim, M.-H., Kim, D. H., Nguyen, D.-T., Lee, H. S., Kang, N.-W., Baek, M.-J., An, J., Yoo, S.-Y., Mun, Y.-H., Lee, W., Kim, K.-T., Cho, C.-W., Lee, J.-Y., & Kim, D.-D. (2020). Preparation and Evaluation of Eudragit L100-PEG Proliponiosomes for Enhanced Oral Delivery of Celecoxib. Pharmaceutics, 12(8), 718. https://doi.org/10.3390/pharmaceutics12080718

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