Phytantriol-based inverted type bicontinuous cubic phase for vascular embolization and drug sustained release

Han, Ke; Pan, Xin; Chen, Meiwan; Wang, Rongchang; Xu, Yang; Feng, Min; Li, Ge; Huang, Min; Wu, Chuanbin

doi:10.1016/j.ejps.2010.09.012

Cited by 53 publications

(28 citation statements)

References 35 publications

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“…Similar in vitro release results were found for propranolol hydrochloride (21), but the exact mechanism is not clear and needs further investigation. In addition, it should be noted that the drug was not completely released from the lower drug content formulations even after 144 h. This incomplete release was probably attributed to the binding of the drug to the PT as described in a previous research (25).…”

Section: The Influence Of Drug Loadingmentioning

confidence: 99%

“…1). In the phase diagram, each phase was identified by visual observation and CPLM at room temperature (22,25). The solution samples that showed a dark background under CPLM were characterized as isotropic solution phase.…”

Section: Phase Diagrammentioning

confidence: 99%

“…PT and V 2 are too viscous to be injected directly (21,25). In order to obtain an injectable ISV 2 system which will transform into cubic liquid crystalline gel after contact with synovial fluids, a co-solvent of ET was added into the PT-water system (21).…”

Section: Phase Diagrammentioning

confidence: 99%

“…In situ liquid crystal delivery systems have several advantages, such as simple production, easy administration, dose reduction capability, and local and sustained delivery (22). In recent years, injectable in situ liquid crystal formulations with low viscosity have been extensively studied in sustained parenteral drug delivery (22)(23)(24)(25)(26). Han et al (25) developed an ISV 2 system (PT/ethanol (ET)/water, 0.8:1:3.2, w/w/w) as an embolic agent for the treatment of hepatocellular carcinoma.…”

Section: Introductionmentioning

confidence: 99%

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Phytantriol-Based In Situ Liquid Crystals with Long-Term Release for Intra-articular Administration

Chen

Liang

Ma³

et al. 2015

AAPS PharmSciTech

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Abstract. The purpose of this study was to develop an injectable in situ liquid crystal formulation for intraarticular (IA) administration, and in situ forming a viscous liquid crystalline gel with long-term release of sinomenine hydrochloride (SMH) upon water absorption. The pseudo-ternary phase diagram of phytantriol (PT)-ethanol (ET)-water was constructed, and isotropic solutions were chosen for further optimization. The physicochemical properties of isotropic solutions were evaluated, and the phase structures of liquid crystalline gels formed by isotropic solutions in excess water were confirmed by crossed polarized light microscopy (CPLM) and small-angle X-ray scattering (SAXS). In vitro drug release studies were conducted by using a dialysis membrane diffusion method. The optimal in situ cubic liquid crystal (ISV 2 ) (PT/ET/water, 64:16:20, w/w/w) loaded with 6 mg/g of SMH showed a suitable pH, showed to be injectable, and formed a cubic liquid crystalline gel in situ with minimum water absorption within the shortest time. The optimal ISV 2 was able to sustain the drug release for 6 days. An in situ hexagonal liquid crystal (ISH 2 ) system was prepared by addition of 5% vitamin E acetate (VitEA) into PT in the optimal ISV 2 system to improve the sustained release of SMH. This ISH 2 (PT/VitEA/ET/water, 60.8:3.2:16:20, w/w/w/w) was an injectable isotropic solution with a suitable pH range. The developed ISH 2 was found to be able to sustain the drug release for more than 10 days and was suitable for IA injection for the treatment of rheumatoid arthritis (RA).KEY WORDS: in situ cubic liquid crystal; in situ hexagonal liquid crystal; phytantriol; sinomenine hydrochloride; sustained drug release.

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Section: The Influence Of Drug Loadingmentioning

confidence: 99%

Section: Phase Diagrammentioning

confidence: 99%

Section: Phase Diagrammentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Phytantriol-Based In Situ Liquid Crystals with Long-Term Release for Intra-articular Administration

Chen

Liang

Ma³

et al. 2015

AAPS PharmSciTech

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“…20,21 The abilities of cubic phases to incorporate drugs for controlled release and enhanced drug bioavailability make it an interesting drug delivery system for oral, topical (or mucosal), and intravenous administration, with extensive applications in a multitude of dosage forms. 18,[22][23][24][25][26] However, few studies have assessed the application of cubic phases in ibuprofen oral drug delivery. Therefore, the objective of this study was to develop a nanoparticulate delivery system by using PYT and F127, which could solubilize ibuprofen in aqueous media, reaching the clinically relevant concentration and delivering ibuprofen in a controlled manner.…”

Section: Introductionmentioning

confidence: 99%

Cubic phase nanoparticles for sustained release of ibuprofen formulation characterization and enhanced bioavailability study

Dian¹,

Yang²,

Li³

et al. 2013

IJN

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Abstract:In order to improve the oral bioavailability of ibuprofen, ibuprofen-loaded cubic nanoparticles were prepared as a delivery system for aqueous formulations. The cubic inner structure was verified by cryogenic transmission electron microscopy. With an encapsulation efficiency greater than 85%, the ibuprofen-loaded cubic nanoparticles had a narrow size distribution around a mean size of 238 nm. Differential scanning calorimetry and X-ray diffraction determined that ibuprofen was in an amorphous and molecular form within the lipid matrix. The in vitro release of ibuprofen from cubic nanoparticles was greater than 80% at 24 hours, showing sustained characteristics. The pharmacokinetic study in beagle dogs showed improved absorption of ibuprofen from cubic nanoparticles compared to that of pure ibuprofen, with evidence of a longer half-life and a relative oral bioavailability of 222% (P , 0.05). The ibuprofen-loaded cubic nanoparticles provide a promising carrier candidate with an efficient drug delivery for therapeutic treatment.

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A Biodegradable Stent with Surface Functionalization of Combined‐Therapy Drugs for Colorectal Cancer

Xie

Zheng

Han

et al. 2018

Adv Healthcare Materials

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treatment for colorectal cancer patients with advanced acute obstruction, high emergent surgical risk, multiple transfer rate, and/or in poor general health. [4] However, postoperative complications and in-stent restenosis caused by tumor ingrowth are major problems for patients undergoing stent displacement. [4][5][6] However, conventional stents made from metal materials only meet the requirements of mechanical expansion and temporary treatment. [5,6] Therefore, development of new intestinal stents with good biocompatibility, degradability, and drug delivery functions is of particular importance. [7] The concept of this type of intestinal stent with drug delivery functions is shown in Figure 1, where the stenosis site can be expanded and the tumor site can be locally treated by drugs released from the stent. 5-Fluorouracil (5-FU) has been used for the treatment of patients with CRC, [2] however, the short half-life (10-20 min), low utilization rate (10-30%), poor sensitivity, and toxicity to normal cells [8,9] are problems. Hence, development of a device that can encapsulate and stabilize 5-FU is important for the improved utilization of the drug to achieve desired clinical outcomes. In previous studies, a drug-loaded polydioxanone weft-knitted stent was developed to treat CRC by slow releasing 5-FU. [2,3] The half maximal inhibitory concentration (IC 50 ) and the median lethal dose (LD 50 ) demonstrated that these drug-loaded membranes had better antitumor effectsIn-stent restenosis caused by tumor ingrowth is a major problem for patients undergoing stent placement because conventional stents often lack sustainable antitumor capabilities. The aim of this work is to develop a silk fibroin (SF)based nanofibrous membrane that is loaded with combined-therapy drugs by using electrospinning technologies, which is further coated on a polydioxanone (PDO) stent and used for the treatment of colorectal cancer (CRC). In order to improve treatment effectiveness, a combination of therapeutic drugs, i.e., curcumin (CUR) and 5-fluorouracil (5-FU), is dissolved into SF solution and then eletrospun onto the surface of the PDO stent. The morphology, secondary structure, and in vitro drug release profiles of the membranes are characterized. The antitumor efficacy is assessed in vitro and in vivo using a human CRC cell line and normal cells, and tumor-bearing nude mice. In vitro and in vivo studies on the nanofibrous memembrane-coating demonstrate improved antitumor effects for the CUR/5-FU dual drug system which can be attributed to cell cycle arrest in the S phase in association with induced apoptosis in tumor cells by blocking signal transducer and activator of transcription 3 (Stat3) and nuclear factor kappa beta (NF-kB) signaling pathways, suggesting potential in the treatment of CRC in the future.

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Phytantriol-based inverted type bicontinuous cubic phase for vascular embolization and drug sustained release

Cited by 53 publications

References 35 publications

Phytantriol-Based In Situ Liquid Crystals with Long-Term Release for Intra-articular Administration

Phytantriol-Based In Situ Liquid Crystals with Long-Term Release for Intra-articular Administration

Cubic phase nanoparticles for sustained release of ibuprofen formulation characterization and enhanced bioavailability study

A Biodegradable Stent with Surface Functionalization of Combined‐Therapy Drugs for Colorectal Cancer

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