JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2022
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IF 5.062
Xin Chen,Duanxiu Li,Yanwen Duan,Yong Huang
Drug co-amorphization is an emerging technology to improve the pharmacokinetic properties of drugs and overcome their side effects. Herein co-amorphization of sinomenine (SIN), an anti-rheumatoid arthritis alkaloid, and an antihistamine drug tranilast (TRA) was investigated for the sustained release of SIN and alleviating its histamine-release adverse reactions. The full co-amorphization of SIN-TRA was determined by powder X-ray diffraction and modulated temperature differential scanning calorimetry , while their CO 2 − and N + –H stretching vibrations in FTIR and protonated nitrogen signals in N 1s X-ray photoelectron spectra suggest the proton transfer between SIN and TRA. These intermolecular interactions could also be observed in their 1D and 2D NMR spectra. All co-amorphous samples exhibited sustained SIN release and excellent physical stability. Therefore, our study not only characterized the strong intermolecular interactions between SIN and TRA, but also discovered a promising drug combination strategy for the sustained release of SIN and reduction of its side effects.
研究领域:
药剂学
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药物化学
✓ 已验证
产品关联
DOI
高影响因子
CRYSTAL GROWTH & DESIGN
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2013
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IF 4.689
Na Geng,Jia-Mei Chen,Zi-Jian Li,Long Jiang,Tong-Bu Lu
The cocrystals and salts of an antiallergic drug, tranilast, were synthesized to improve its solubility and photostability. Two tranilast cocrystals with urea (1) and nicotinamide (2), as well as two salts with cytosine (3) and sodium ion (4), were obtained and characterized by infrared spectra, thermogravimetric analyses, differential scanning calorimetry, and powder and single crystal X-ray diffractions. The results of single crystal structure analyses of 1–3 indicate that tranilast combines amide groups in coformers via R22(8) synthon, resulting in a 1:1 stoichiometry. The complexes showed advantages in terms of solubility and photostability in comparison to pure tranilast. The maximum solubility values of 1–3 in phosphate buffer of pH 6.8 are approximately 1.6, 1.9, and 2.0 times as large as that of tranilast, and the residual of tranilast is 79.5, 92.9, 88.5, 86.2, and 87.4% for tranilast and 1–4, respectively, under the fluorescent lamp irradiation for 96 h.
研究领域:
药物化学
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材料科学
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分析化学
✓ 已验证
DOI
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2024
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IF 4.5
Kai-chao Wen,Zheng-an Li,Ji-heng Liu,Chuan Zhang,Feng Zhang,Feng-qian Li
The implantation of bare metal ureteral stents may lead to bacterial colonization and scar hyperplasia. To effectively address these issues, PLGA nanoparticles co-loaded with tranilast and gallium phytate (PG-TRL-PLGA-NPs) were prepared using an emulsifying solvent volatilization technique. The PG-TRL-PLGA-NPs possess a dual function of antibacterial and proliferation inhibition, which could be used for stent functional coating. The PG-TRL-PLGA-NPs displayed a regular spherical morphology with a smooth surface, and average particle size of 163 ± 1.37 nm, Zeta potential of −16.09 mV, drug loading capacity of 9.4 ± 0.6%, and encapsulation efficiency of 97.5 ± 0.4% could be achieved. FTIR, XRD, and DSC analysis demonstrated that PG-TRL-PLGA-NPS was successfully nano-encapsulated without chemical reaction among TRL, PG, and PLGA. In vitro release profiles of TRL and gallium ions from PG-TRL-PLGA-NPs exhibited a sustained-release effect, with 89.7 ± 0.9% and 3.2 ± 0.15 mg/L released in 14 days, respectively. Furthermore, it was observed the potent antibacterial activity (against S. aureus and E. coli .) of PG-TRL-PLGA-NPs, also significantly inhibited SV-HUC-1 cell proliferation through experiments involving cell migration, cell cycle, and apoptosis studies. These results provide valuable insights into the stent coatings of PG-TRL-PGLA NPs with potential functions of antibacterial and proliferative inhibitory.
研究领域:
药学
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纳米技术
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生物材料
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药物递送系统
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生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
Biomaterials Research
·
2026
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IF 9.8
Ayesha Younas,Muhammad Sohail,Yueting Li,Quan Zhou,Yonghui Shen,Shuanghu Wang,Yaru Shi,Zhenqiu Shang,Chuxiao Shao,Jian Xiao
Hypertrophic scars (HSs) are a prevalent skin condition that imposes substantial functional, financial, and aesthetic burdens, with existing treatments often leading to recurrence, pain, and adverse effects. To address these issues, we propose a first-in-class fast-dissolving sodium alginate-based microneedle patch (sMN) that achieves sequential, dual-release kinetics by integrating tranilast (TS) and glabridin (GL)-loaded nanoparticles (GLNPs), termed TS+GLNPs@sMN. Our system uniquely integrates rapid TS release for immediate “OFF” switching, suppression of fibroblast activation, stabilization of mast cells, and relief of pruritus, with sustained GL release from GLNPs for prolonged “ON” switching, which promotes fibroblast apoptosis and modulates scar matrix deposition. This sequential “OFF-to-ON” paradigm mirrors the temporal progression of HS pathophysiology, with early inflammatory events preceding fibrotic remodeling. The cone-shaped microneedle patch (~565 μm) demonstrated efficient skin penetration/recovery, even drug distribution, fast dissolution (180 ± 20 s), high loading capacity, and desirable release kinetics. In vitro evaluations confirmed promising anti-proliferative, anti-migratory, and anti-angiogenic effects. Preliminary in vivo biocompatibility in mice was satisfactory, with no skin irritation and normal complete blood count, renal, and hepatic function. In vivo studies in a rabbit ear HS model demonstrate accelerated HS healing, reduced HS thickness, epidermal thickness index (ETI), scar elevation index (SEI), and collagen deposition, along with decreased profibrotic markers, inflammatory cytokines, and angiogenic factors. Overall, the TS+GLNPs@sMN patch offers a minimally invasive, self-administrable, dual-action therapeutic strategy for enhanced HS management, with safety and efficacy in preclinical models.
✓ 已验证
DOI
PubMed
高影响因子
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