Study of azathioprine encapsulation into liposomes

Journal of Microencapsulation
M GulatiS Singh

Abstract

The factors influencing the encapsulation of azathioprine (AZA) into liposomes were investigated to find out the conditions for its optimal entrapment. Similar studies for comparison were also carried out on 6-mercaptopurine (6-MP), of which AZA is a prodrug. AZA and also 6-MP show higher encapsulation efficiencies in MLVs as compared to LUVs. Variation in phospholipid composition does not seem to affect the loading capacity of either of the two drugs. The encapsulation efficiency of both the drugs improves upon addition of cholesterol in the bilayer, but the effect is seen only up to 30% cholesterol. Thereafter the effect becomes constant. AZA shows better incorporation in the positively charged liposomes as compared to those with neutral or negative charge. The entrapment of 6-MP is, however, found to be independent of the charge on the liposomes. Entrapment efficiency for both the drugs markedly depends on the pH of the hydration medium, yielding better entrapment efficiencies at high pH values. The rise in solute concentration initially causes increase in the entrapment of the two drugs which is followed by a decreasing phase.

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Citations

Apr 6, 2007·AAPS PharmSciTech·Rania M HathoutAhmed S Guinedi
Feb 13, 2010·AAPS PharmSciTech·Khaled Mohamed Hosny
Jan 26, 2012·International Journal of Nanomedicine·Prabhakara PrabhuG S Nisha
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Jul 26, 2014·Saudi Pharmaceutical Journal : SPJ : the Official Publication of the Saudi Pharmaceutical Society·Ehab I TahaMohsen A Bayomi
Apr 27, 2018·The Journal of Pharmacology and Experimental Therapeutics·Young LeeJaipal Singh
Apr 14, 2018·Frontiers in Microbiology·Sanjay ChhibberSandeep Kaur
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Apr 22, 2018·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Rea D SignorellJean-Christophe Leroux
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Sep 7, 2021·European Journal of Drug Metabolism and Pharmacokinetics·Ahmed B BayoumyNanne K H de Boer

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