Physicochemical stability of phospholipid-dispersed suspensions of crystalline itraconazole

Werling, Jane; Graham, Sabine; Owen, Heather; Nair, Lakshmy; Gonyon, Thomas; Carter, Phillip W.

doi:10.1016/j.ejpb.2008.01.030

Cited by 16 publications

(4 citation statements)

References 29 publications

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“…In contrast to the formulations with PBS, all investigated nanoemulsions containing SOS, irrespective of coemulsifier type or preparation method, remained unchanged upon autoclaving in terms of droplet size, PDI, and charge, and the parameter values were stable within 4 months of storage at 25 C. Thus, the stability of nanoemulsions against heat-stress during autoclaving was possibly promoted by the presence of sodium oleate which, in addition to pH buffering, might increase the negative charge of the droplet surface layer, contributing to the nanoemulsion electrostatic stabilization (Werling et al, 2008).…”

Section: Stability Study -Unloaded Nanoemulsionsmentioning

confidence: 68%

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Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation

Đorđević

Cekić

Savić

et al. 2015

International Journal of Pharmaceutics

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This paper describes design and evaluation of parenteral lecithin-based nanoemulsions intended for brain delivery of risperidone, a poorly water-soluble psychopharmacological drug. The nanoemulsions were prepared through cold/hot high pressure homogenization and characterized regarding droplet size, polydispersity, surface charge, morphology, drug-vehicle interactions, and physical stability. To estimate the simultaneous influence of nanoemulsion formulation and preparation parameters--co-emulsifier type, aqueous phase type, homogenization temperature--on the critical quality attributes of developed nanoemulsions, a general factorial experimental design was applied. From the established design space and stability data, promising risperidone-loaded nanoemulsions (mean size about 160 nm, size distribution <0.15, zeta potential around -50 mV), containing sodium oleate in the aqueous phase and polysorbate 80, poloxamer 188 or Solutol(®) HS15 as co-emulsifier, were produced by hot homogenization and their ability to improve risperidone delivery to the brain was assessed in rats. Pharmacokinetic study demonstrated erratic brain profiles of risperidone following intraperitoneal administration in selected nanoemulsions, most probably due to their different droplet surface properties (different composition of the stabilizing layer). Namely, polysorbate 80-costabilized nanoemulsion showed increased (1.4-7.4-fold higher) risperidone brain availability compared to other nanoemulsions and drug solution, suggesting this nanoemulsion as a promising carrier worth exploring further for brain targeting.

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Section: Stability Study -Unloaded Nanoemulsionsmentioning

confidence: 68%

“…Besides the role of an auxiliary stabilizer of the phospholipid surface layer (Shi et al, 2009;Werling et al, 2008), sodium oleate also served as a buffering agent to maintain the pH of prepared nanoemulsion formulations to a desirable value.…”

Section: Preparation and Characterization Of Nanoemulsionsmentioning

confidence: 99%

Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation

Đorđević

Cekić

Savić

et al. 2015

International Journal of Pharmaceutics

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“…The major contribution to hydrolysis is specific acid−base catalysis, 218 but buffer catalysis also occurs, with acetate, tris, and citrate ions all providing general acid−base catalysis. 223 During the course of the reaction, the production of free fatty acid (FFA) lowers the pH, 231 and this pH change is frequently used as a means of monitoring hydrolysis rates. The lysolipid that initially forms following hydrolysis is subject to a transesterifcation reaction, resulting in acyl migration to form predominantly the 1-acyl species regardless of the initial site of hydrolysis.…”

Section: Nonenzymatic Glycerophospholipid Hydrolysismentioning

confidence: 99%

The Chemical Reactivity of Membrane Lipids

Duché,

Sanderson

2024

Chem. Rev.

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It is well-known that aqueous dispersions of phospholipids spontaneously assemble into bilayer structures. These structures have numerous applications across chemistry and materials science and form the fundamental structural unit of the biological membrane. The particular environment of the lipid bilayer, with a water-poor low dielectric core surrounded by a more polar and better hydrated interfacial region, gives the membrane particular biophysical and physicochemical properties and presents a unique environment for chemical reactions to occur. Many different types of molecule spanning a range of sizes, from dissolved gases through small organics to proteins, are able to interact with membranes and promote chemical changes to lipids that subsequently affect the physicochemical properties of the bilayer. This Review describes the chemical reactivity exhibited by lipids in their membrane form, with an emphasis on conditions where the lipids are well hydrated in the form of bilayers. Key topics include the following: lytic reactions of glyceryl esters, including hydrolysis, aminolysis, and transesterification; oxidation reactions of alkenes in unsaturated fatty acids and sterols, including autoxidation and oxidation by singlet oxygen; reactivity of headgroups, particularly with reactive carbonyl species; and E/Z isomerization of alkenes. The consequences of reactivity for biological activity and biophysical properties are also discussed. CONTENTS

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“…То есть, в случае фосфолипидной наносистемы с включением олеата [15] соотношение лекарство/липид более чем вдвое выше, чем для системы на основе только фосфатидилхолина [14]. В ряде работ отмечались и другие преимущества включения олеатного аниона в фосфолипидные дисперсии как фактора, повышающего их стабильность [18] и защищающего фосфолипиды от окисления [19]. Фосфолипидная система с добавлением олеата натрия [15] использовалась нами для включения рифампицина в последующих экспериментах in vivo.…”

Section: результатыиобсуждениеunclassified

Drug delivery system on the base of phospholipid nanoparticles for rifampicin

et al. 2013

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Low bioavailability of rifampicin, one of the main antituberculous drug, stimulates searches of its new optimized formulations. The present study has showen possibility of rifampicin embedding into nanoparticles from plant phosphatidylcholine (diameter of 20-30 nm). Addition of sodium oleate to the phospholipid system caused a 2-fold increase of the percent of rifampicin incorporation. After oral administration to rats, the maximal drug observed in plasma one hour after was 0.5 and 4.2 mkg/ml for free rifampicin for rifampicin in phospholipids-oleate nanoparticles, respectively. These levels were maintained for more than two hours of the experiment. High rifampicin bioavailability in the oleate containing phospholipid nanosystem suggests prospectivity of its pharmaceutical elaboration.

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Physicochemical stability of phospholipid-dispersed suspensions of crystalline itraconazole

Cited by 16 publications

References 29 publications

Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation

Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation

The Chemical Reactivity of Membrane Lipids

Drug delivery system on the base of phospholipid nanoparticles for rifampicin

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