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Open AccessArticle

A Liposomal Formulation for Improving Solubility and Oral Bioavailability of Nifedipine

by Ye Bi 1,2,†, Bingcong Lv 3,†, Lianlian Li 3, Robert J. Lee 3,4, Jing Xie 3, Zhidong Qiu 1,5,* and Lesheng Teng 1,3,5,*
1
Key Laboratory of Effective Components of Traditional Chinese Medicine, Changchun University of Chinese Medicine, Changchun 130117, China
2
Practice Training Center, Changchun University of Chinese Medicine, Changchun 130117, China
3
School of Life Sciences, Jilin University, Changchun 130117, China
4
Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
5
Department of Pharmacy, Changchun University of Chinese Medicine, Changchun 130117, China
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2020, 25(2), 338; https://doi.org/10.3390/molecules25020338 (registering DOI)
Received: 2 December 2019 / Revised: 7 January 2020 / Accepted: 9 January 2020 / Published: 14 January 2020
Proliposomes were used to improve the solubility and oral bioavailability of nifedipine. Nifedipine proliposomes were prepared by methanol injection-spray drying method. The response surface method was used to optimize formulation to enhance the encapsulation efficiency (EE%) of nifedipine. The particle size of nifedipine proliposomes after rehydration was 114 nm. Surface morphology of nifedipine proliposomes was observed by a scanning electron microscope (SEM) and interaction of formulation ingredients was assessed by differential scanning calorimetry (DSC). The solubility of nifedipine is improved 24.8 times after forming proliposomes. In vitro release experiment, nifedipine proliposomes had a control release effect, especially in simulated gastric fluid. In vivo, nifedipine proliposomes significantly improved the bioavailability of nifedipine. The area under the concentration-time curve (AUC0–∞) of nifedipine proliposomes was about 10 times than nifedipine after oral administration. The elimination half-life (T1/2β) of nifedipine was increased from 1.6 h to 6.6 h. In conclusion, proliposomes was a promising system to deliver nifedipine through oral route and warranted further investigation. View Full-Text
Keywords: nifedipine; proliposomes; pharmacokinetics; bioavailability nifedipine; proliposomes; pharmacokinetics; bioavailability
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Bi, Y.; Lv, B.; Li, L.; Lee, R.J.; Xie, J.; Qiu, Z.; Teng, L. A Liposomal Formulation for Improving Solubility and Oral Bioavailability of Nifedipine. Molecules 2020, 25, 338.

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