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Evaluation of Oleic Acid and Polyethylene Glycol Monomethyl Ether Conjugate (PEGylated Oleic Acid) as a Solubility Enhancer of Furosemide

1
School of Pharmacy, The University of Texas at El Paso, 1101 N Campbell St, El Paso, TX 79902, USA
2
Department of Biomedical Engineering, College of Engineering, The University of Texas at El Paso, 500 W University Ave, El Paso, TX 79968, USA
3
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Ajman University, Ajman 2758, UAE
4
Department of Pharmaceutical Sciences, School of Pharmacy, High Point University, High Point, NC 27240, USA
*
Author to whom correspondence should be addressed.
Processes 2019, 7(8), 520; https://doi.org/10.3390/pr7080520
Received: 16 July 2019 / Revised: 1 August 2019 / Accepted: 5 August 2019 / Published: 7 August 2019
(This article belongs to the Special Issue Protein Biosynthesis and Drug Design & Delivery Processes)
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Abstract

Poor aqueous solubility limits the therapeutic efficacy of many marketed and investigational drugs. Synthesis of new drugs with improved solubility is challenging due to time constraint and expenses involved. Therefore, finding the solubility enhancers for existing drugs is an attractive and profitable strategy. In this study, PEGylated oleic acid (OA-mPEG5000), a conjugate of oleic acid and mPEG5000 was synthesized and evaluated as a solubilizer for furosemide. OA-mPEG5000 was evaluated as a nanocarrier for furosemide by formulating polymersomes. Solubility of furosemide in milli-Q water and aqueous OA-mPEG5000 solution was determined using shake flask method. At 37 °C, the solubility of furosemide in OA-mPEG5000 (1% w/w) and milli-Q water was 3404.7 ± 254.6 µg/mL and 1020.2 ± 40.9 µg/mL, respectively. Results showed there was a 3.34-fold increase in solubility of furosemide in OA-mPEG5000 compared to water at 37 °C. At 25 °C, there was a 3.31-fold increase in solubilization of furosemide in OA-mPEG5000 (1% w/w) (90.0 ± 1.45 µg/mL) compared to milli-Q water (27.2 ± 1.43 µg/mL). Size, polydispersity index and zeta potential of polymersomes ranged from 85–145.5 nm, 0.187–0.511 and −4.0–12.77 mV, respectively. In-vitro release study revealed a burst release (71%) within 1 h. Significant enhancement in solubility and formation of polymersomes suggested that OA-mPEG5000 could be a good solubilizer and nanocarrier for furosemide. View Full-Text
Keywords: oleic acid; mPEG; furosemide; OA-mPEG5000; solubility; polymersomes; BCS class IV; PEGylated oleic acid oleic acid; mPEG; furosemide; OA-mPEG5000; solubility; polymersomes; BCS class IV; PEGylated oleic acid
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Kalhapure, R.S.; Bolla, P.K.; Boddu, S.H.; Renukuntla, J. Evaluation of Oleic Acid and Polyethylene Glycol Monomethyl Ether Conjugate (PEGylated Oleic Acid) as a Solubility Enhancer of Furosemide. Processes 2019, 7, 520.

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