Effects of triglycerides on the hydrophobic drug loading capacity of saturated phosphatidylcholine-based liposomes

Hong, Soon-Seok; Kim, Sohee; Lim, Soo-Jeong

doi:10.1016/j.ijpharm.2015.02.013

Cited by 52 publications

(32 citation statements)

References 33 publications

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“…To obtain a liposomal dispersion with improved homogeneity, additional sonication for 7 minutes was performed by using a cell disruptor (Bioruptor ® , UCD-200T, Cosmo Bio Co., Ltd, Tokyo, Japan) set at 250 W. Unloaded/precipitated PTX was removed from PTX-loaded liposomes by immediate filtering of liposomal dispersions through 0.8 µm syringe membrane filter. 27,29 Entrapped PTX in liposomes was quantified by HPLC analysis as described in the following section.…”

Section: Preparation Of Liposomesmentioning

confidence: 99%

“…27 Approximately 6 mol% of PTX could be loaded in triglyceride-incorporated 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC):cholesterol (CHOL) liposomes, a concentration of ~tenfold higher than that achieved using oil-free counterparts. However, the produced PTX-loaded liposomes were inadequate as in intravenous dosage form due to the large particle size of resultant liposomes.…”

Section: Introductionmentioning

confidence: 99%

“…DMPC and C300 were selected as saturated PC and oil component, respectively, based on our previously reported data. 27 In the absence of triglyceride incorporation, DMPC:CHOL:PE-PEG liposomes accommodated 6.6-fold higher concentration of PTX compared to DMPC:CHOL liposomes. Our data conflict with earlier studies that reported the greatly reduced PTX loading in PEGylated liposomes compared to conventional liposomes.…”

mentioning

confidence: 99%

“…Taken together, these results suggest that incorporation of C300 within phospholipid bilayer contributed to preventing the fusion/aggregation of saturated PC-based/PEGylated liposomes, thereby greatly retarding the PTX leakage/precipitation. Based on our recent findings that the incorporation of MCT or LCT commonly decreases the lipid chain ordering of liposomal membranes, 27 we next investigated whether the stabilizing effect is also observed in case of other triglycerides. Either Labrafac (MCT) or soybean oil (LCT) also improved PTX retention in DMPC:CHOL:PE-PEG liposomes ( Figure 3A), demonstrating that the stabilizing effect was commonly shared by MCT or LCT.…”

mentioning

confidence: 99%

“…The incorporation of C300 at ~2 mg/mL in liposomes was sufficient to retard the PTX precipitation, suggesting that the triglyceride effect was saturated at a content required to fluidize the DMPC:CHOL liposomes. 27 effect of triglyceride on the formulation stability of unsaturated Pc-based liposomes carrying PTX To investigate the effect of triglyceride incorporation on the unsaturated PC-based liposomes, DOPC-or SoyPC-based liposomes were prepared in the absence or presence of C300. C300 incorporation greatly induced the time-dependent increase of mean droplet size of both of DOPC-and SoyPCbased liposomes during storage: after 7 days storage, 3.5-and 4.8-fold increase in the particle size were observed in DOPC:CHOL:PE-PEG:C300 and SoyPC:CHOL:PE-PEG:C300 liposomes in contrast to 1.4-and 1.2-fold increase in corresponding C300(−) liposomes, respectively ( Figure 4A).…”

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confidence: 99%

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Development of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation

Hong

Choi

Kim

et al. 2016

IJN

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Studies have highlighted the challenge of developing injectable liposomes as a paclitaxel (PTX) carrier, a challenge attributable to the limitations in liposomal stability caused by PTX loading. Poor stability of PTX-loaded liposomes is caused by PTX-triggered aggregation or fusion of liposomal membranes and is exacerbated in the presence of PEGylated lipid. In the present study, the effect of triglyceride incorporation on the stability of PTX-loaded/PEGylated liposomes was explored. Incorporation of a medium chain triglyceride Captex 300 into saturated phosphatidylcholine (PC)-based liposomes (1,2-dimyristoyl- sn -glycero-3-phosphocholine [DMPC]:cholesterol [CHOL]:N-(Carbonyl-methoxypolyethyleneglycol 2000)-1, 2-distearoyl- sn -glycero-3-phospho-ethanolamine [PE-PEG]), produced a fine, homogeneous, and membrane-filterable PTX-loaded liposomes fulfilling the requirement of an injectable lipid formulation. Triglyceride incorporation also greatly inhibited the time-dependent leakage of PTX from saturated PC-based liposomes, which appears to be mediated by the inhibition of liposome fusion. In contrast, triglyceride incorporation induced the destabilization and PTX leakage of unsaturated PC-based liposomes, indicating the opposite effect of triglyceride depending on the fluidity status of PC constituting the liposomal membrane. PTX release profile and the in vitro and in vivo anticancer efficacy of triglyceride-incorporated DMPC:CHOL:PE-PEG liposomes were similar to Taxol ® while the toxicity of liposomal PTX was significantly lower than that of Taxol. Taken together, triglyceride incorporation provided an injectable PTX formulation by functioning as a formulation stabilizer of PEGylated/saturated PC-based liposomes.

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Section: Preparation Of Liposomesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

mentioning

confidence: 99%

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confidence: 99%

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Development of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation

Hong

Choi

Kim

et al. 2016

IJN

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Determinants of HDL Cholesterol Efflux Capacity after Virgin Olive Oil Ingestion: Interrelationships with Fluidity of HDL Monolayer

Fernández‐Castillejo¹,

Rubió²,

Hernáez

et al. 2017

Molecular Nutrition Food Res

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Scope Cholesterol efflux capacity of HDL (CEC) is inversely associated with cardiovascular risk. HDL composition, fluidity, oxidation, and size are related with CEC. We aimed to assess which HDL parameters were CEC determinants after virgin olive oil (VOO) ingestion. Methods and Results Post-hoc analyses from the VOHF study, a crossover intervention with three types of VOO. We assessed the relationship of 3-week changes in HDL-related variables after intervention periods with independence of the type of VOO. After univariate analyses, mixed linear models were fitted with variables related with CEC and fluidity. Fluidity and Apolipoprotein (Apo)A-I content in HDL was directly associated, and HDL oxidative status inversely, with CEC. A reduction in free cholesterol, an increase in triglycerides in HDL, and a decrease in small HDL particle number or an increase in HDL mean size, were associated to HDL fluidity. Conclusions HDL fluidity, ApoA-I concentration, and oxidative status are major determinants for CEC after VOO. The impact on CEC of changes in free cholesterol and triglycerides in HDL, and those of small HDL or HDL mean size, could be mechanistically linked through HDL fluidity. Our work points out novel therapeutic targets to improve HDL functionality in humans through nutritional or pharmacological interventions.

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Targeted delivery of liposomal Ribociclib to SLC7A5 transporters in breast cancer cells

Afsharzadeh,

Varshosaz,

Mirian

et al. 2023

Invest New Drugs

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Effects of triglycerides on the hydrophobic drug loading capacity of saturated phosphatidylcholine-based liposomes

Cited by 52 publications

References 33 publications

Development of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation

Development of paclitaxel-loaded liposomal nanocarrier stabilized by triglyceride incorporation

Determinants of HDL Cholesterol Efflux Capacity after Virgin Olive Oil Ingestion: Interrelationships with Fluidity of HDL Monolayer

Targeted delivery of liposomal Ribociclib to SLC7A5 transporters in breast cancer cells

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