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Development and Characterization of DOPEPEG2000 Coated Oleic Acid Liposomes Encapsulating Anticancer Drugs

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Journal of Surfactants and Detergents

Abstract

Liposomes have been widely investigated as drug carriers for a broad range of anticancer drugs. However, their application as a drug delivery system may be challenging due to low encapsulation of active ingredient and poor stability which leads to uncontrolled delivery of bioactive ingredients. The present study aims at incorporating 1,2-dioleoyl-sn-glycero-3-phosphoethanolamide-N-[methoxy(polyethylene glycol)-2000 (DOPEPEG2000) into oleic acid (OA) liposomes in order to prolong the lifetime in blood circulation. The pH transition curve of oleic was obtained by titration of sodium oleate solution with 0.05 mol dm−3 HCl to determine the region where liposomes were abundantly present. The critical vesicle concentration (CVC) was then determined by surface tension measurements. Dry lipid liposomes were hydrated with phosphate buffer at just over twice the CVC value. Optical polarizing microscopy (OPM) showed the presence of liposomes while transmission electron microscopy (TEM) confirmed that the liposomes prepared were spherical in shape and less than 200 nm in size. The incorporation of DOPEPEG2000 into the oleic acid liposomes reduced the average particle size and zeta potential to mimic the red blood cells. The encapsulation efficiency of various anticancer drugs was more than 60% while more than 20% of the drugs were released after 24 h. The results suggest that DOPEPEG2000: oleic acid at a molar ratio of 1:50 fulfilled the requirements for intravenous drug delivery.

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Acknowledgements

This work was fully funded by the University of Malaya through Postgraduate Research Grants (PG123-2012B and PG094-2014A) and Fundamental Research Grant Scheme FP013-2015A. Vicit Rizal has been supported by the Ministry of Higher Education through the MyBrain15 scholarship program. The authors would like to give thanks to members of the Colloid Lab, Department of Chemistry, Assoc. Prof Dr. Ivy Chung and members of Translational Core Laboratory, Faculty of Medicine, UM, Dr. Teo Yin Yin, Khalisanni Khalid, Ainnul Azizan, Dr. Joyce Lee Poh Foong (UTAR) and En. Amir from the Material Characterization Laboratory, Department of Physics for their advice and technical support.

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Correspondence to Misni Misran.

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Eh Suk, V.R., Misran, M. Development and Characterization of DOPEPEG2000 Coated Oleic Acid Liposomes Encapsulating Anticancer Drugs. J Surfact Deterg 20, 321–329 (2017). https://doi.org/10.1007/s11743-016-1914-8

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  • DOI: https://doi.org/10.1007/s11743-016-1914-8

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