Structural characterization of novel phospholipid lipid nanoparticles for controlled drug delivery

Wang, Qi; Gong, Tao; Sun, Xun; Zhang, Zhirong

doi:10.1016/j.colsurfb.2011.01.034

Cited by 16 publications

(6 citation statements)

References 25 publications

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“…Confocal laser scanning microscopy (CLSM) (FV1000; Olympus Corp., Tokyo, Japan) was employed to visualize the microenvironment of the major components in the emulsion, lipid based depot and lipid nanoparticles (6,24). The fluorescent emulsions were labeled with two fluorescent probes, nile red and fluorescein-cholesterol complex.…”

Section: Methodsmentioning

confidence: 99%

Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors

Liu

Xia

et al. 2016

Oncology Reports

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The aim of the present study was to develop a lipid emulsion loaded with a paclitaxel-cholesterol complex (PTX-CH Emul) in order to improve the safety and efficacy of paclitaxel (PTX) and evaluate its antitumor activity against commercially available formulation Taxol®. PTX-CH Emul resembling a low density lipoprotein lipid structure, exhibited an ideal particle size, high drug loading capability, high drug encapsulation efficiency and excellent stability. PTX-CH Emul showed superior in vitro anticancer efficacy against triple-negative MDA-MB-231 breast cancer cells when compared with a paclitaxel emulsion (PTX Emul) and Taxol. The IC70 value of PTX-CH Emul was almost 1.5- and 2.4-fold lower than that of PTX Emul and Taxol, respectively. Compared with PTX Emul and Taxol, PTX-CH Emul exhibited stronger and more rapid inhibitory effects on 3D tumor spheroids of MDA-MB-231 cells. Additionally, in vivo tumor-targeting study showed that PTX-CH Emul had higher specificity and efficiency in intratumoral accumulation as compared to PTX Emul. Finally, the maximum tolerated dose (MTD) of PTX-CH Emul was 2.25‑fold higher than that of Taxol, suggesting that PTX-CH Emul exhibited better safety profiles in vivo than Taxol. At the MTDs, PTX-CH Emul exhibited superior antitumor efficacy in nude mice bearing MDA-MB-231 xenografts in comparison to Taxol. Therefore, PTX-CH Emul as reported here showed high potential as a drug carrier for PTX in clinical applications involving the targeting of triple-negative breast cancer.

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Section: Methodsmentioning

confidence: 99%

Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors

Liu

Xia

et al. 2016

Oncology Reports

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“…The schematic model of SN38-PC-LNs was shown in Figure 8. SN38 bounded to phospholipids through the interactions between its active groups with the polar groups of lipids to yield the phospholipids complex, thus leading to high DL (Wang et al, 2011). Multiple phospholipid complex molecules orderly arranged to form a spherical domain.…”

Section: Discussionmentioning

confidence: 99%

“…Multiple phospholipid complex molecules orderly arranged to form a spherical domain. The extra phospholipids which were not involved in the complex reaction accumulated at the surface of the nanoparticles, acting as surfactants, and stabilized the nano-system due to the reduction of the surface energy (Wang et al, 2011).…”

Section: Discussionmentioning

confidence: 99%

Lipid nanoparticles loaded with 7-ethyl-10-hydroxycamptothecin-phospholipid complex:in vitroandin vivostudies

et al. 2014

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7-Ethyl-10-hydroxy-camptothecin (SN38), the active metabolite of irinotecan (CPT-11), is an effective antineoplastic agent against many malignancies. Although it is 100-fold to 1000-fold more potent than CPT-11, the clinical utility of SN38 has been extremely restricted because of its poor solubility in any pharmaceutically acceptable solvents. The aim of this study was to develop SN38 nanoparticles (SN38-PC-LNs) using pharmaceutically acceptable excipients, and investigate the therapeutic efficacies in vitro and in vivo. SN38-phospholipid complex (SN38-PC) was prepared and loaded into lipid nanoparticles. The particle size was approximately 200 nm with a narrow size distribution. A high encapsulation efficiency of 88.11% ± 1.41% and drug loading of 9.55% ± 0.84% were achieved under the optimal condition. SN38-PC-LNs exhibited potent cytotoxic effects against a panel of human tumor cell lines (HT-29, HepG2, A549 and MCF-7). In vivo evaluation proved the enhanced antitumor efficacy of SN38-PC-LNs in mice bearing S180 tumor as well. The results from this study demonstrated an effective formulation of SN38 has been developed, which is promising for the delivery of SN38 for tumor chemotherapy.

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“…As advanced lipid-based nanocarriers, LNs were prepared by solvent evaporation and high-pressure homogenization as previously described [10]. In brief, 60 mg of soybean phospholipids and 100 μg of Dil were dissolved in 10 ml of acetone and gently agitated at 50 °C for 1 h to form clear mixture.…”

Section: Preparation and Characterization Of Phospholipid Complex-loamentioning

confidence: 99%

Lipid nanovehicles with adjustable surface properties for overcoming multiple barriers simultaneously in oral administration

Shan

et al. 2017

International Journal of Pharmaceutics

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Lipid nanoparticles (LNs) are widely investigated for oral drug delivery, and for achieving significant advantages in colloidal stability, biocompatibility and scaled-up possibility. However, researchers face challenge of developing methods to improve the ability of LNs in overcoming multiple barriers (i.e., mucus and epithelium barrier) in gastrointestinal (GI) tract because of the contradictory requirement of nanoparticle (NP) surface properties in the two processes. Therefore, we designed novel LNs with adjustable surface properties by coating lipid core with hydrophobic substitutes grafting N-(2-hydroxypropyl) methacrylamide copolymer (pHPMA). In the present study, different substitutes (i.e., monocyclic, polycyclic, and linear segments) were grafted on pHPMA backbone. Screening studies demonstrated that type and grafting degree of substitutes both influenced hydrophilic-hydrophobic properties of NP surface and improved penetration through mucus. When a hydrophilic-hydrophobic balance was achieved, NPs showed elevated mucus permeability compared with bare LNs; this phenomenon subsequently contributed to higher cellular uptake. Moreover, β-sitosterol (SITO)-modified pHPMA-coated (grafting degree: 5%) LNs (5% SITO-LNs) exhibited the highest mucus permeability, transepithelial transport, and in situ absorption. Interestingly, even with the highest surface hydrophilicity, 5% SITO-LNs with Caco-2 cells did not show impaired membrane affinity, which was not observed in other groups. Further investigations of mechanism demonstrated that membrane affinity was significantly enhanced by β-SITO-mediated interaction with Niemann-Pick C1-like 1 (NPC1L1) protein on cell membranes. These results proved that hydrophobic substitutes play a critical role in altering hydrophilic-hydrophobic property of particle surface and improving penetration through multiple barriers. β-SITO-induced specific interaction can provide additional benefits to efficiency of oral delivery of LNs.

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Structural characterization of novel phospholipid lipid nanoparticles for controlled drug delivery

Cited by 16 publications

References 25 publications

Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors

Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors

Lipid nanoparticles loaded with 7-ethyl-10-hydroxycamptothecin-phospholipid complex:in vitroandin vivostudies

Lipid nanovehicles with adjustable surface properties for overcoming multiple barriers simultaneously in oral administration

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