JOURNAL OF DISPERSION SCIENCE AND TECHNOLOGY
·
2023
·
IF 2.2
Junwei Liu,Meihong Zhang,Chuanbin Wu,Xin Pan,Zhengwei Huang
Erastin is the most classical small molecular ferroptosis inducer but its clinical application is hindered due to its poor solubility. Nanotechnology has been used to improve ferroptosis inducer erastin’s solubility. The recently reported erastin-incorporated nanosystems (e.g., nanoparticulate ferritin, poly(ethylene glycol) methyl ether-blockpoly(lactide-co-glycolide) (mPEG-PLGA) nanoparticle, exosome, and liposome) could to some degree elevate its solubility, but were still poor in loading capacity. To be specific, the maximum entrapment efficiency and drug loading in previous studies were approximately 36% and 3.7%, respectively. In order to improve drug loading capacity, we constructed a novel carrier based on Vitamin E d-α-Tocopherol polyethylene glycol 1000 succinate (TPGS) and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®) blended micelles. The erastin@TPGS/Soluplus® micelles were prepared by thin film hydration method, and formulation details including dosage of Soluplus®, the weight ratio of TPGS to Soluplus®, the weight ratio of erastin to TPGS/Soluplus® were optimized. The physicochemical properties of the erastin micelles were measured by DLS, TEM, FTIR, and TG-DSC analysis. The products exhibited a nanoscale and uniform particle size (78.11 ± 0.54 nm) and neutral surface charge (-0.43 ± 0.32 mV). Significantly improved entrapment efficiency (89.63 ± 1.81%) and drug loading rate (10.03 ± 0.14%) were obtained, which was over 2-fold of current reports. The in vitro release study demonstrated that erastin could release in a sustained yet complete manner, and the drug release might be governed by multiple mechanisms including anomalous diffusion of non-Fickian diffusion, matrix erosion and sustained release. In summary, this proposed erastin nanosystem provides a new strategy for improving loading capacity, and may probably augment ferroptosis-inducing therapy for cancer treatment.
研究领域:
药学
·
肿瘤学
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
·
2023
·Vol. 103
·期 7
·3628-3637
·
IF 4.1
Yuanyuan Xue,Youwu Liao,Haiqiao Wang,Shuang Li,Zhengqing Gu,Michael Adu-Frimpong,Jiangnan Yu,Ximing Xu,Hugh D. C Smyth,Yuan Zhu
BACKGROUND Astaxanthin is a type of food-derived active ingredient with antioxidant, antidiabetic and non-toxicity functions, but its poor solubility and low bioavailability hinder further application in food industry. In the present study, through inclusion technologies, micellar solubilization and electrospray techniques, we prepared astaxanthin nanoparticles before optimizing the formulation to regulate the physical and chemical properties of micelles. We accomplished the preparation of astaxanthin nanoparticle delivery system based on single needle electrospray technology through use of 2-hydroxypropyl-β-cyclodextrin and Soluplus® to improveme the release behavior of the nanocarrier. RESULTS Through this experiment, we successfully prepared astaxanthin nanoparticles with a particle size of approximately 80 nm, which was further verified with scanning electron microscopy and transmission electron microscopy. Furthermore, the encapsulation of astaxanthin molecules into the carrier nanoparticles was verified via the results of attenuated total reflectance intensity and X-ray powder diffraction techniques. The in vitro release behavior of astaxanthin nanoparticles was different in media that contained 0.5% Tween 80 (pH 1.2, 4.5 and 6.8) buffer solution and distilled water. Also, we carried out a pharmacokinetic study of astaxanthin nanoparticles, in which it was observed that astaxanthin nanoparticle showed an effect of immediate release and significant improved bioavailability. CONCLUSION 2-hydroxypropyl-β-cyclodextrin and Soluplus® were used in the present study as a hydrophilic nanocarrier that could provide a simple way of encapsulating natural function food with repsect to improving the solubility and bioavailability of poorly water-soluble ingredients. © 2023 Society of Chemical Industry.
研究领域:
食品科学
·
药物递送系统
·
纳米技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Drug Delivery and Translational Research
·
2021
·Vol. 12
·期 3
·603-614
·
IF 4.617
Shi Feng,Chen Lin,Wang Yaping,Liu Jing,Adu-Frimpong Michael,Ji Hao,Toreniyazov Elmurat,Wang Qilong,Yu Jiangnan,Xu Ximing
The objective of this study was to fabricate a novel drug delivery system using Soluplus® (polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer) and glycyrrhizic acid to improve solubility, bioavailability, and anti-hyperuricemic activity of aloe emodin (AE). The AE-loaded mixed micelles (AE-M) were prepared by thin-film hydration method. The optimal AE-M contained small-sized (30.13 ± 1.34 nm) particles with high encapsulation efficiency (m/m, %) of 90.3 ± 1.08%. The release rate of AE increased in the micellar formulation than that of free AE in the four media (DDW, pH 7.0; phosphate buffer solution, pH 7.4; phosphate buffer solution, pH 6.8; and hydrochloric acid aqueous solution, pH 1.2). In comparison to free AE, the pharmacokinetic study of AE-M showed that its relative oral bioavailability increased by 3.09 times, indicating that mixed micelles may promote gastrointestinal absorption. More importantly, AE-M effectively reduced uric acid level by inhibiting xanthine oxidase (XOD) activity in model rats. The degree of ankle swelling, serum levels of interleukin (IL)-1, and IL-6-related inflammatory factors levels all decreased in the gouty arthritis model established via monosodium urate (MSU) crystals. Taken together, the AE-M demonstrated the potential to improve the bioavailability, anti-hyperuricemic activity, and anti-inflammation of AE. Graphical abstract
研究领域:
药剂学
·
药物递送系统
·
代谢疾病
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2023
·
IF 8.2
Yinglan Li,Jie Xu,Qingran Guan,Huaizhen Zhang,Zhuang Ding,Qingpeng Wang,Zhengping Wang,Jun Han,Min Liu,Yanna Zhao
Solid dispersions (SDs) possess the potential to enhance the bioavailability of insoluble active pharmaceutical ingredients (APIs) by effectively converting them into amorphous state. However, SDs have a tendency to recrystallize unless appropriate excipients are employed. The objective of this study was to evaluate the ability of hypromellose acetate succinate HF (HPMCAS-HF) and Soluplus® to inhibit the recrystallization of β-carotene and improve its in vivo bioavailability through the fabrication of ternary β-carotene solid dispersions (SDs) with the aid of specific surfactant. Due to rapid micellization , the dissolution profiles of β-carotene SDs based on HPMCAS-HF/Span 20 (5:5, w/w) or Soluplus®/Span 20 (6:4, w/w) combinations exhibited significant improvement, which were almost 7–10 times higher than β-carotene bulk powder. DSC and PXRD analysis indicated a notable reduction in the crystallinity degree of β-carotene within the SDs. The stability study demonstrated a half-life of β-carotene in the SDs exceeding 30 days. Additionally, the in vivo pharmacokinetics analysis confirmed that the cellulose derivatives/surfactant combinations significantly enhanced the bioavailability of β-carotene by 1.37-fold and 2.3-fold, respectively. Notably, the HPMCAS-HF/Span 20 combination exhibited superior performance. Consequently, the HPMCAS-HF/Span 20 combination held potential for the advancement of an effective drug delivery system for β-carotene.
研究领域:
药剂学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2025
·Vol. 26
·期 1
·1-14
·
IF 4
Fan Fan,Zhou Feng,Zhang Jiayu,Yang Junhui,Zhuang Kai,Shan Yudong,Jiang Lei,Zhang Jiantao
Amorphous solid dispersion (ASD) is one of the most studied strategies for improving the dissolution performance of poorly water-soluble drugs, but ASDs often have low drug loadings, thereby necessitating larger dosage sizes. This study intended to create Soluplus® (SOL)-based microparticle ASDs with high drug loading (up to 60 w/w%) and long-term stability (at least 16 months) using electrospraying to enhance the dissolution of poorly water-soluble celecoxib (CEL). X-ray diffraction (XRD) and differential scanning calorimetry (DSC) analyses showed that the electrosprayed SOL-CEL microparticles were amorphous, and Fourier transform infrared spectroscopy (FTIR) data indicated the presence of hydrogen bonding between SOL and CEL in the microparticles, which helped stabilize the ASDs. In vitro dissolution studies demonstrated that these ASDs improved the CEL dissolution rate by up to 8.2-fold compared to the crystalline form. Electrospraying presents a promising alternative to conventional methods like hot-melt extrusion (HME) and spraying drying (SD) for the production of ASDs, providing simplicity, high drug loading capability and long-term stability, thus catering to a variety of poorly water-soluble drugs. Graphical
研究领域:
药剂学
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Yinglan Li,Qipeng Wei,Jianshuo Su,Huaizhen Zhang,Zhiping Fan,Zhuang Ding,Min Wen,Min Liu,Yanna Zhao
In this study, the interaction among multifunctional excipients, including polysaccharides, cellulose derivatives, and surfactants, was particularly investigated, together with its impact on the physicochemical properties of astaxanthin amorphous solid dispersions (ASTX ASDs). It was indicated that Span 20 could rapidly form hemimicelles or aggregates in the presence of hypromellose acetate succinate HF (HPMCAS-HF, HF) or Soluplus®, while octenyl succinic anhydride modified starch (OSA-starch) efficiently assisted in the coalescence inhibition of drug-excipients aggregates, which was jointly beneficial to the recrystallization inhibition of amorphous ASTX. ASTX ASDs were further prepared with OSA-starch, HPMCAS-HF/Soluplus®, and Span 20 as the wall materials. DSC, SEM, and XRD confirmed that crystalline ASTX had transformed to amorphous state in the ASDs, while FT-IR spectra provided evidence suggesting the existence of hydrogen bonds and hydrophobic interaction between ASTX and the excipients. The dissolution of ASTX ASDs in different media revealed significant promotion, while the pharmacokinetic results further demonstrated the oral bioavailability of ASTX ASDs enhanced remarkably, exhibiting 2.75-fold (SD 1 ) and 1.87-fold (SD 2 ) increase, respectively, compared to ASTX bulk powder. In summary, the cellulose derivatives-surfactant interaction had great impact on the physicochemical properties of ASTX ASDs, and their combinations exhibited great potential for delivering the hydrophobic bioactive compounds efficiently.
研究领域:
药学
·
材料科学
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）