An injectable liquid crystal system for sustained delivery of entecavir

Lim, Jae-Hyuk; Ki, Min-Hyo; Joo, Min Kyung; An, Sung-Won; Hwang, Kyu-Mok; Park, Eun-Seok

doi:10.1016/j.ijpharm.2015.05.049

Cited by 27 publications

(14 citation statements)

References 40 publications

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“…However, BC interaction shows an antagonistic effect on PS (Fig 1). This might be due to the possible attraction between the cationic E and the anionic LEC producing more compact smaller particles [12]. In contrast, the stirring speed (D) shows a negative effect on PS.…”

Section: Optimization Of Elph Using Bbdmentioning

confidence: 97%

“…However, the oral administration of E is associated with poor patient compliance and adverse reactions, resulting from intake of E on empty stomach, necessitating the fabrication of sustained release formulation [6]. In this context, long-acting parenteral formulations of E have been well-investigated by various research groups, including liquid crystals [12], lipidic prodrug [13], albumin nanoparticles [8] and PLGA microspheres [6].…”

Section: Introductionmentioning

confidence: 99%

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An integrated vitamin E-coated polymer hybrid nanoplatform: A lucrative option for an enhanced in vitro macrophage retention for an anti-hepatitis B therapeutic prospect

et al. 2020

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A platform capable of specifically delivering an antiviral drug to the liver infected with hepatitis B is a major concern in hepatology. Vaccination has had a major effect on decreasing the emerging numbers of new cases of infection. However, the total elimination of the hepatitis B virus from the body requires prolonged therapy. In this work, we aimed to target the liver macrophages with lipid polymer hybrid nanoparticles (LPH), combining the merit of polymeric nanoparticles and lipid vesicles. The hydrophilic antiviral drug, entecavir (E), loaded LPH nanoparticles were optimized and physicochemically characterized. A modulated lipidic corona, as well as, an additional coat with vitamin E were used to extend the drug release enhance the macrophage uptake. The selected vitamin E coated LPH nanoparticles enriched with lecithin-glyceryl monostearate lipid shell exhibited high entrapment for E (80.47%), a size � 200 nm for liver passive targeting, extended release over one week, proven serum stability, retained stability after refrigeration storage for 6 months. Upon macrophage uptake in vitro assessment, the presented formulation displayed promising traits, enhancing the cellular retention in J774 macrophages cells. In vivo and antiviral activity futuristic studies would help in the potential application of the ELPH in hepatitis B control.

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Section: Optimization Of Elph Using Bbdmentioning

confidence: 97%

Section: Introductionmentioning

confidence: 99%

An integrated vitamin E-coated polymer hybrid nanoplatform: A lucrative option for an enhanced in vitro macrophage retention for an anti-hepatitis B therapeutic prospect

et al. 2020

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“…The zeta potential of blank nanobubbles was −19.27 ± 2.21 mV. The negative zeta potential of blank nanobubbles may be mainly ascribed to 1,2-dipalmitoyl-sn-glycero-3-phosphatidic acid, which is an anionic phospholipid [ 26 ]. When targeted nanobubbles were loaded with CAIX polypeptides, the zeta potential increased to −14.80 ± 2.12 mV, implying that the positively charged amino groups on CAIX polypeptides neutralized partial negative charge of anionic phospholipid [ 27 ].…”

Section: Resultsmentioning

confidence: 99%

Construction of ultrasonic nanobubbles carrying CAIX polypeptides to target carcinoma cells derived from various organs

et al. 2017

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BackgroundUltrasound molecular imaging is a novel diagnostic approach for tumors, whose key link is the construction of targeted ultrasound contrast agents. However, available targeted ultrasound contrast agents for molecular imaging of tumors are only achieving imaging in blood pool or one type tumor. No targeted ultrasound contrast agents have realized targeted ultrasound molecular imaging of tumor parenchymal cells in a variety of solid tumors so far. Carbonic anhydrase IX (CAIX) is highly expressed on cell membranes of various malignant solid tumors, so it’s a good target for ultrasound molecular imaging. Here, targeted nanobubbles carrying CAIX polypeptides for targeted binding to a variety of malignant tumors were constructed, and targeted binding ability and ultrasound imaging effect in different types of tumors were evaluated.ResultsThe mean diameter of lipid targeted nanobubbles was (503.7 ± 78.47) nm, and the polypeptides evenly distributed on the surfaces of targeted nanobubbles, which possessed the advantages of homogenous particle size, high stability, and good safety. Targeted nanobubbles could gather around CAIX-positive cells (786-O and Hela cells), while they cannot gather around CAIX-negative cells (BxPC-3 cells) in vitro, and the affinity of targeted nanobubbles to CAIX-positive cells were significantly higher than that to CAIX-negative cells (P < 0.05). Peak intensity and duration time of targeted nanobubbles and blank nanobubbles were different in CAIX-positive transplanted tumor tissues in vivo (P < 0.05). Moreover, targeted nanobubbles in CAIX-positive transplanted tumor tissues produced higher peak intensity and longer duration time than those in CAIX-negative transplanted tumor tissues (P < 0.05). Finally, immunofluorescence not only confirmed targeted nanobubbles could pass through blood vessels to enter in tumor tissue spaces, but also clarified imaging differences of targeted nanobubbles in different types of transplanted tumor tissues.ConclusionsTargeted nanobubbles carrying CAIX polypeptides can specifically enhance ultrasound imaging in CAIX-positive transplanted tumor tissues and could potentially be used in early diagnosis of a variety of solid tumors derived from various organs.Electronic supplementary materialThe online version of this article (doi:10.1186/s12951-017-0307-0) contains supplementary material, which is available to authorized users.

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“…PLM has been widely applied for studies of drug/food crystals, including animal/plant crystal materials (fibrins, starch granules, etc.). Lim et al 59 developed an injectable liquid crystal system for sustained delivery of entecavir. PLM was applied to investigate the structure of the liquid crystalline phase and confirmed their typical characteristics and recognized them as the hexagonal phase.…”

Section: Crystal Growth and Designmentioning

confidence: 99%

Instrumental Analytical Techniques for the Characterization of Crystals in Pharmaceutics and Foods

Qiao

et al. 2017

Crystal Growth & Design

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Crystallization has attracted more and more attention from scientists and engineers in the field of pharmaceutics and foods. In order to understand crystals, many instrumental analytical techniques have been developed and applied in this field. In this work, recent application progress of instrumental analytical techniques for the characterization of crystal forms in pharmaceutics and foods has been reviewed and discussed. These techniques include X-ray diffraction, thermal analytical techniques, molecular vibrational spectroscopy, microscopy observation techniques, solid-state nuclear magnetic resonance spectroscopy, nuclear quadrupole resonance spectroscopy, etc. This work will provide a comprehensive guide to scientists and engineers in this field to characterize crystals in pharmaceutics and foods.

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An injectable liquid crystal system for sustained delivery of entecavir

Cited by 27 publications

References 40 publications

An integrated vitamin E-coated polymer hybrid nanoplatform: A lucrative option for an enhanced in vitro macrophage retention for an anti-hepatitis B therapeutic prospect

An integrated vitamin E-coated polymer hybrid nanoplatform: A lucrative option for an enhanced in vitro macrophage retention for an anti-hepatitis B therapeutic prospect

Construction of ultrasonic nanobubbles carrying CAIX polypeptides to target carcinoma cells derived from various organs

Instrumental Analytical Techniques for the Characterization of Crystals in Pharmaceutics and Foods

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