Formulation and Evaluation of a Self-microemulsifying Drug Delivery System Containing Bortezomib
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- Hong Eon-Pyo
- College of Pharmacy, Kyung Hee University R&D Center, Handok Inc.
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- Kim Ju-Young
- College of Pharmacy, Woosuk University
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- Kim Su-Hyeon
- School of Pharmacy, Sungkyunkwan University
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- Hwang Kyu-Mok
- School of Pharmacy, Sungkyunkwan University
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- Park Chun-Woong
- College of Pharmacy, Chungbuk National University
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- Lee Hyo-Jung
- College of Pharmacy, Chungbuk National University
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- Kim Dong-Wook
- Department of Pharmaceutical Engineering, Cheongju University
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- Weon Kwon-Yeon
- College of Pharmacy, Catholic University of Daegu
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- Jeong Seo Young
- College of Pharmacy, Kyung Hee University
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- Park Eun-Seok
- School of Pharmacy, Sungkyunkwan University
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Abstract
<p>The purposes of the present study were to develop a self-microemulsifying drug delivery system (SMEDDS) containing bortezomib, a proteasome inhibitor. The solubility of the drug was evaluated in 15 pharmaceutical excipients. Combinations of oils, surfactants and cosurfactants were screened by drawing pseudo-ternary phase diagrams. The system exhibiting the largest region of microemulsion was considered optimal. Bortezomib SMEDDS spontaneously formed a microemulsion when diluted with an aqueous medium with a median droplet size of approximately 20–30 nm. In vitro release studies showed that the SMEDDS had higher initial release rates for the drug when compared with the raw drug material alone. Measurement of the viscosity, size, and ion conductivity indicated that a phase inversion from water in an oil system to oil in a water system occurred when the weight ratio of the water exceeded 30% of the entire microemulsion system. In a pharmacokinetics study using rats, the bortezomib microemulsion failed to improve the bioavailability of the drug. The reason was assumed to be degradation of the drug in the microemulsion in the gastrointestinal tract. However, bortezomib in Labrasol® solution (an aqueous solution containing 0.025% Labrasol®) showed significantly increased area under the curve from 0–24 h (AUC0–24 h) and maximum plasma concentration (Cmax) values compared to the drug suspension. The findings of this study imply that oral delivery of a bortezomib and colloidal system containing Labrasol® could be an effective strategy for the delivery of bortezomib.</p>
Journal
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- Chemical and Pharmaceutical Bulletin
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Chemical and Pharmaceutical Bulletin 64 (8), 1108-1117, 2016
The Pharmaceutical Society of Japan
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Keywords
Details 詳細情報について
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- CRID
- 1390001204178962816
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- NII Article ID
- 130005253936
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- NII Book ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL BIB ID
- 027522863
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- PubMed
- 27477648
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed