Capacity of cholesteryl hemisuccinate in ion pair/phospholipid complex to improve drug-loading, stability and antibacterial activity of clarithromycin intravenous lipid microsphere

Luo, Lifeng; Chen, Qiuyue; Gong, Haoyu; Liu, Lu; Zhou, Licheng; He, Haibing; Yin, Tian; Tang, Xing

doi:10.1016/j.colsurfb.2018.08.038

Cited by 11 publications

(6 citation statements)

References 33 publications

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“…Meanwhile, the decrease of the droplet size afterward may be due to the obvious coalescence (Figure ) and oiling-off of droplets with larger particle sizes (Figure ) and resulting in a greater fraction of droplets with smaller particle sizes . It has been reported that a derivative of Chol (cholesteryl hemisuccinate) could help stabilize the interface and endow the emulsion with good thermal stability . Consistent with the literature, the two emulsions with Chol exhibited thermal stability better than that of the other two emulsions without Chol in this study.…”

Section: Results and Discussionsupporting

confidence: 87%

“…8 It has been reported that a derivative of Chol (cholesteryl hemisuccinate) could help stabilize the interface and endow the emulsion with good thermal stability. 39 Consistent with the literature, the two emulsions with Chol exhibited thermal stability better than that of the other two emulsions without Chol in this study. And the thermal stability of the SPL + Chol-stabilized emulsion was inferior to that of the SPL + SM + Chol-stabilized emulsion because the affinity for Chol of SPL was weaker than that of SM.…”

Section: Physical Characteristics and Morphology Of Emulsions Duringsupporting

confidence: 92%

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Improving the Physicochemical Stability of Soy Phospholipid-Stabilized Emulsions Loaded with Lutein by the Addition of Sphingomyelin and Cholesterol: Inspired by a Milk Fat Globule Membrane

Liang,

Liu,

Zhu

et al. 2023

J. Agric. Food Chem.

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The emulsifying performance of glycerophospholipids alone is inferior to proteins, etc., while the sphingomyelin (SM) and cholesterol (Chol) naturally existing in biological membranes could interact with glycerophospholipids to influence the polar lipid arrangement. Inspired by the natural membranes, the effect of SM and Chol on the physicochemical stability of soy phospholipid (SPL)-stabilized emulsions during storage or under environmental stresses was determined. The results indicated that the addition of SM and/or Chol could improve the storage stability of the emulsions and protective effect on lutein significantly (p < 0.05). Except for UV irradiation, the addition of Chol significantly improved the stability of the emulsions against acid, salt, and heat. The strong intermolecular hydrogen bonds and condensed assembly formed by SM and Chol contributed to the best stability of SPL + SM + Chol-stabilized emulsions. The results gave insight into improving the emulsifying properties of glycerophospholipids with SM and Chol.

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Section: Results and Discussionsupporting

confidence: 87%

Section: Physical Characteristics and Morphology Of Emulsions Duringsupporting

confidence: 92%

Improving the Physicochemical Stability of Soy Phospholipid-Stabilized Emulsions Loaded with Lutein by the Addition of Sphingomyelin and Cholesterol: Inspired by a Milk Fat Globule Membrane

Liang,

Liu,

Zhu

et al. 2023

J. Agric. Food Chem.

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“…CHEMS (pH), a cholesterol derivative, is a pH-sensitive excipient. Like cholesterol, CHEMS also has natural lipophilicity and membrane stabilization activity ( 19 , 20 ). CHEMS self-assemble into a bimolecular layer in alkaline and neutral aqueous media and therefore fuse with the bimolecular layer of niosomes, whereas they rupture the bimolecular layer in acidic media to facilitating drug release ( 21 ).…”

Section: Introductionmentioning

confidence: 99%

Galactose-Modified PH-Sensitive Niosomes for Controlled Release and Hepatocellular Carcinoma Target Delivery of Tanshinone IIA

Jun

Deng

et al. 2021

AAPS PharmSciTech

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Increasing the drug tumor-specific accumulation and controlling their release is considered one of the most effective ways to increase the efficacy of drugs. Here, we developed a vesicle system that can target hepatoma and release drugs rapidly within tumor cells. This non-ionic surfactant vesicle is biodegradable. Galactosylated stearate has been used to glycosylate the vesicles to achieve liver targeting; replacement of a portion (Chol:CHEMS = 1:1) of cholesterol by cholesteryl hemisuccinate (CHEMS) allows for a rapid release of drugs in an acidic environment. In vitro release experiments confirmed that galactose-modified pH-sensitive niosomes loaded with tanshinone IIA had excellent drug release performance in acid medium. In vitro experiments using ovarian cancer cells (A2780), colon cancer cells (HCT8), and hepatoma cell (Huh7, HepG2) confirmed that the preparation had specific targeting ability to hepatoma cells compared with free drugs, and this ability was dependent on the galactose content. Furthermore, the preparation also had a more substantial inhibitory effect on tumor cells, and subsequent apoptosis assays and cell cycle analyses further confirmed its enhanced anti-tumor effect. Results of pharmacokinetic experiments confirmed that the vesicle system could significantly extend the blood circulation time of tanshinone IIA, and the larger area under the curve indicated that the preparation had a better drug effect. Thus, the results of biodistribution experiments confirmed the in vivo liver targeting ability of this preparation. Niosomes designed in this manner are expected to be a safe and effective drug delivery system for liver cancer therapy.

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“…The reason for this may be the formation of AIP increasing the lipophilicity and enabling APT to be better encapsulated within the core oil phase. Additionally, CHEMS, a derivative of cholesterol, had been reported to be a membrane stabilizer and can stabilize the interface membrane to provide AIPE with good thermal stability (38).…”

Section: High-temperature Stabilitymentioning

confidence: 99%

Aprepitant Intravenous Emulsion Based on Ion Pairing/Phospholipid Complex for Improving Physical and Chemical Stability During Thermal Sterilization

et al. 2020

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An aprepitant (APT) cholesteryl hemisuccinate (CHEMS) ion pair complex emulsion (AIPE) with high lecithin content was prepared to improve sterilization stability through the film dispersion homogenization method; therefore, it could be a promising delivery system of APT. Medium-chain triglycerides (MCT) was selected as the oil phase to improve the solubility and stability of APT in oil phase. DSC, XRD, FT-IR, and 1 H-NMR spectroscopies confirmed that the APT-CHEMS ion pair (AIP) was formed between CHEMS and APT. The formation of AIP significantly increased the hydrophobicity of APT, allowing it to be completely embedded in the oil phase core to improve chemical stability and decrease hydrolysis of APT in the water phase. Also, CHEMS had a strong affinity with lecithin and could stabilize lipid membranes, forming a stronger and thicker interface membrane to increase the physical stability of AIPE. As a result, AIPE could withstand autoclaving at 120°C for 8 min without any change of particle size or content. Furthermore, AIPE with a potential of − 53.4 mV remained stable through spatial repulsion during sterilization. The encapsulation efficiency of AIPE was over 90% and the particle size was 106.8 ± 65.62 nm(0.286). Pharmacokinetic study in rats was comparable with that of CINVANTI which yielded a relative bioavailability of 114.31% indicating that the AIPE had similar pharmacokinetic processes in vivo with the analog of CINVANTI®. The AUC0-t of the AIPE was 4.31-fold that of the APT solution.

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Capacity of cholesteryl hemisuccinate in ion pair/phospholipid complex to improve drug-loading, stability and antibacterial activity of clarithromycin intravenous lipid microsphere

Cited by 11 publications

References 33 publications

Improving the Physicochemical Stability of Soy Phospholipid-Stabilized Emulsions Loaded with Lutein by the Addition of Sphingomyelin and Cholesterol: Inspired by a Milk Fat Globule Membrane

Improving the Physicochemical Stability of Soy Phospholipid-Stabilized Emulsions Loaded with Lutein by the Addition of Sphingomyelin and Cholesterol: Inspired by a Milk Fat Globule Membrane

Galactose-Modified PH-Sensitive Niosomes for Controlled Release and Hepatocellular Carcinoma Target Delivery of Tanshinone IIA

Aprepitant Intravenous Emulsion Based on Ion Pairing/Phospholipid Complex for Improving Physical and Chemical Stability During Thermal Sterilization

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