Morphological transformation of self-assembled nanostructures prepared from cholesteryl acyl didanosine and the optimal formulation of nanoparticulate systems: Effects of solvents, acyl chain length and poloxamer 188

Jin, Yiguang; Ai, Ping; Xin, Rui; Chen, Fan

doi:10.1016/j.jcis.2008.07.014

Cited by 14 publications

(7 citation statements)

References 47 publications

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“…This insertion 'joins' the particle, compacting the SLN by filling void spaces, overcoming steric hindrance, resulting in a reduced particle size. Poloxamers with higher chains, (F127 > F68), have longer PEO terminal chains protruding from the particle after insertion which can potentially explain the larger particle size in F127 compared to F68 [15,27]. Also, upon adsorption of poloaxmer on particle surface, the hydrophilic field on the particle is greatly enlarged-the extent depending on the molecular weight of the poloaxmer-resulting in an increased particle size.…”

Section: Effect Of Surfactants On Particle Sizementioning

confidence: 99%

SLNs can Serve as the New Brachytherapy Seed: Determining Influence of Surfactants on Particle Size of Solid Lipid Microparticles and Development of Hydrophobised Copper Nanoparticles for Potential Insertion

Mistry¹,

Sarker²

2016

J Chem Eng Process Technol

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Solid lipid nanoparticles (SLNs) or technically speaking, larger solid lipid microparticles are emerging as a noninvasive technique for drug-delivery, carrying forward advantages of conventional nanostructured systems and eliminating their drawbacks. This study involves the analysis of solid lipid microparticles generated via hot high-shear homogenization technique with tristearin as the main lipid component and phosphate buffer (pH 7.00) as the aqueous phase (phase volume 0.2). This study aims to identify the effects of the chosen lipid, and four non-ionic surfactants (Tween®20, Tween®80, Lutrol F68 and Lutrol F127) on particle size of solid lipid microparticles. Samples generating particle sizes of less than 200 nm were further analysed via SEM to determine morphological characteristics of SLNs. SLN composition is crucial as it determines various chemical and physical properties of the particle itself. Firstly, selection of lipids is key, as it the major component of the particle. Lipids display different polymorphic transitions upon crystallization affecting loading efficiency, drug distribution, drug loading, particle size, particle shape and overall stability. Secondly, selection of surfactants is vital as they overcome stability problems with reducing surface tension, particle aggregation and steric interactions. The aim of this study was to determine the optimal functioning surfactant concentration that would produce particle sizes less than 200 nm. SLNs generated in this study displayed a reduced particle size (90-150 nm) when using 2% w/v Tween®80 plus 5:1 F68; higher molecular weight surfactant, with a low molecular weight poloxamer. Based on previous research, these results can be explained via the surfactant characteristics in solution. The length of the fatty acid chains associated with Tween®20 and 80 provide a potential behavioural pattern on the SLN; longer chains surrounding the SLN structure increase stability of the particle but also increase particle size. Poloxamer use is that of a co-surfactant, fulfilling what Tween® fails to complete. In which higher molecular weight poloxamers can potentially explain the large particle size as the longer PEO terminal chains protrude from the particle after its insertion.

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Section: Effect Of Surfactants On Particle Sizementioning

confidence: 99%

SLNs can Serve as the New Brachytherapy Seed: Determining Influence of Surfactants on Particle Size of Solid Lipid Microparticles and Development of Hydrophobised Copper Nanoparticles for Potential Insertion

Mistry¹,

Sarker²

2016

J Chem Eng Process Technol

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“…A novel technology involving antiretroviral prodrugs with amphiphilic properties have been developed by Jin and co-workers (Jin et al, 2008(Jin et al, , 2009(Jin et al, , 2010. The molecular selfassembly properties of those prodrugs in aqueous media permit the formation of nanostructures with amphiphilic characteristics, allowing them to cross biomembranes and deliver themselves in vivo without carriers (Jin et al, 2008).…”

Section: Self-assembled Drug Delivery Systems Of Antiretroviral Prodrugsmentioning

confidence: 99%

“…The molecular selfassembly properties of those prodrugs in aqueous media permit the formation of nanostructures with amphiphilic characteristics, allowing them to cross biomembranes and deliver themselves in vivo without carriers (Jin et al, 2008). Recently, a series of cholesteryl derivatives of antiviral nucleoside analogues were synthesized by this group, which involved acyclovir, zidovudine and didanosine.…”

Section: Self-assembled Drug Delivery Systems Of Antiretroviral Prodrugsmentioning

confidence: 99%

“…The morphologies and the morphological transformation of cholesterylsuccinyl didanosine was investigated as a prodrug with representative self-assembly behavior in aqueous media. Results showed that the resulted nanoparticulate system had a narrow size distribution, which allowed heat sterilization and showed a site-specific distribution for the anti-HIV therapy after IV administration (Jin et al, 2008). Another example of this technology was the synthesis of the amphiphilic prodrug anti-HIV zidovudine, cholesteryl-phosphonyl zidovudine.…”

Section: Self-assembled Drug Delivery Systems Of Antiretroviral Prodrugsmentioning

confidence: 99%

See 1 more Smart Citation

Exploring the Nanotechnology-Based Drug Delivery Systems for AIDS Treatment

Carvalho¹,

Mainardes²,

Gremião³

2011

Understanding HIV/AIDS Management and Care - Pandemic Approaches in the 21st Century

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“…Gel permeation chromatography was one of such separating method commonly used. 31,32 In this study, the entrapment efficiency of CyA was measured by gel permeation chromatography using Sephadex G-50. CyA-loaded cubic nanoparticles were eluted through Sephadex G-50 (2 g) columns (φ1.5 cm × 30 cm) after preconditioning with 30 mL water.…”

Section: Dovepressmentioning

confidence: 99%

Pharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine A encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles

Lai

Lü²,

Yin³

et al. 2009

IJN

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Efforts to improve the oral bioavailability of cyclosporine A (CyA) remains a challenge in the field of drug delivery. In this study, glyceryl monooleate (GMO)/poloxamer 407 cubic nanoparticles were evaluated as potential vehicles to improve the oral bioavailability of CyA. Cubic nanoparticles were prepared via the fragmentation of a bulk GMO/poloxamer 407 cubic phase gel by sonication and homogenization. The cubic inner structure formed was verified using Cryo-TEM. The mean diameters of the nanoparticles were about 180 nm, and the entrapment efficiency of these particles for CyA was over 85%. The in vitro release of CyA from these nanoparticles was less than 5% at 12 h. The results of a pharmacokinetic study in beagle dogs showed improved absorption of CyA from cubic nanoparticles as compared to microemulsion-based Neoral ® ; higher C max (1371.18 ± 37.34 vs 969.68 ± 176.3 ng mL

show abstract

Morphological transformation of self-assembled nanostructures prepared from cholesteryl acyl didanosine and the optimal formulation of nanoparticulate systems: Effects of solvents, acyl chain length and poloxamer 188

Cited by 14 publications

References 47 publications

SLNs can Serve as the New Brachytherapy Seed: Determining Influence of Surfactants on Particle Size of Solid Lipid Microparticles and Development of Hydrophobised Copper Nanoparticles for Potential Insertion

SLNs can Serve as the New Brachytherapy Seed: Determining Influence of Surfactants on Particle Size of Solid Lipid Microparticles and Development of Hydrophobised Copper Nanoparticles for Potential Insertion

Exploring the Nanotechnology-Based Drug Delivery Systems for AIDS Treatment

Pharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine A encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles

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