Materials Advances
·
2022
·Vol. 3
·期 5
·2417-2424
·
IF 0
Yufang Wang,Jianzhu Wang,Mingshuang Sun,Jiyan Zhang,Yanping Bi
Escaping from the immune system to achieve a long circulation time is an essential prerequisite for targeting liposomes. Monomethoxy-poly(ethylene glycol)–distearoylphosphatidylethanolamine (mPEG–DSPE) is the most commonly used stealth polymer for long circulating liposomes. With its monomethoxy end moving freely on the liposomal surface, the linear PEG chains of mPEG–DSPE construct a hydration layer to repel complement proteins and thus evade immune clearance. We describe in this work a new kind of PEG derivative whose two ends were grafted with cholesterol (cholesterol–PEG–cholesterol, CPC). According to the in vitro and in vivo results, the presence of CPC in liposomes was shown to reduce the uptake by phagocyte cells while extending the circulation time. The stealth performance of CPC liposomes is closely related to the molecular weight of PEG moieties. CPC6k performed better than CPC2k, CPC4k and the commonly used mPEG2k–DSPE. CPC on the liposomal surface would not let the free end of PEG act as the immune recognition site, meanwhile, the PEG chain of CPC tends to adopt a twisted ring-like conformation rather than a linear conformation, which is considered to be associated with the stealth effect. This finding adds to the range of stealth liposomes and may be valuable for developing new drug carriers.
研究领域:
药剂学
·
生物医学工程
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产品关联
DOI
Journal of Biomedical Nanotechnology
·
2015
·Vol. 11
·期 4
·711-721
·
IF 5.338
Yang Linjie,Jiang Jizong,Hong Jingyi,Di Jing,Liao Yonghong,Kuang Haixue,Wang Xiangtao
The objective of this study was to evaluate the feasibility of producing 10-hydroxycamptothecin nanosuspensions with high drug payload and to then determine the in vitro and in vivo characteristics of these nanosuspensions. Using cholesterol-PEG600 as a stabilizer, 10-hydroxycamptothecin
nanosuspensions were successfully prepared using a precipitation-combined high-pressure homogenization method. A satisfactory drug payload of 90.39% (w/w) was achieved. The obtained nanosuspensions were spherical, with a mean particle size of 115.0 ± 0.4 nm, and they were monodisperse
with a polydispersity index of 0.134 ± 0.001. The 10-hydroxycamptothecin remained in the same crystalline form in both the nanosuspensions and the bulk powder. In vitro, the 10-hydroxycamptothecin nanosuspensions released the encapsulated drug with nearly zero-order kinetics,
and the accumulative release reached 90% within 72 hours. In vitro cytotoxicity assay showed that the 10-hydroxycamptothecin nanosuspensions had significantly enhanced cytotoxicity against HepG2 cells compared to the commercially available 10-hydroxycamptothecin injections. The in
vivo study with H22 tumor-bearing mice and intravenous injection of the drug showed that in contrast to the 10-hydroxycamptothecin injections, the 10-hydroxycamptothecin nanosuspensions exhibited significantly enhanced biodistribution, particularly in the lung (393.40-fold AUC0–24
h, liver (192.35-fold AUC0–24 h, spleen (141.67-fold AUC0–24 h and tumor (64.21-fold AUC0–24 h. The 10-hydroxycamptothecin nanosuspensions also showed improved antitumor therapeutic efficacy over the injections (89.83% vs. 30.56%). This
suggests that cholesterol-PEG600 may be an effective stabilizer for the preparation of hydrophobic drug nanosuspensions and that 10-hydroxycamptothecin nanosuspensions are a promising drug delivery system for tumor treatment.
研究领域:
药剂学
·
肿瘤学
·
生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
Acta Pharmaceutica Sinica B
·
2022
·
IF 14.903
Xiaonan Chen,Yiqing Zou,Shuqi Zhang,Pengchao Fang,Shuxuan Li,Pengyu Li,Yingying Sun,Gang Yuan,Haiyan Hu
Helicobacter pylori ( H. pylori ), creating a global infection rate over 50%, presents great challenges in clinical therapies due to its complex pathological microenvironment in vivo . To improve the eradication efficacy, herein we fabricated a pharmaceutical vesicle RHL/Cl-Ch-cal where cholesterol-PEG, calcitriol and first-line antibiotic clarithromycin were co-loaded in the rhamnolipid-composed outer lipid layer. RHL/Cl-Ch-cal could quickly penetrate through gastric mucus layer to reach H. pylori infection sites, and then effectively destroyed the architecture of H. pylori biofilms, killed dispersed H. pylori and inhibited the re-adhesion of residual bacteria (called biofilms eradication tetralogy). Moreover, RHL/Cl-Ch-cal activated the host immune response to H. pylori by replenishing cholesterol to repair lipid raft on the cell membrane of host epithelial cells. Finally, RHL/Cl-Ch-cal killed the intracellular H. pylori through recovering the lysosomal acidification and assisting degradation. In experiments, RHL/Cl-Ch-cal demonstrated prominent anti- H. pylori efficacy in the classical H. pylori -infected mice model. Therefore, the study provides a “comprehensive attack” strategy for anti- H. pylori therapies including biofilms eradication tetralogy, immune activation and intracellular bacteria killing.
研究领域:
药学
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微生物学
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免疫学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
Biomaterials Science
·
2025
·
IF 5.7
Xueting Wei,Jiajia Luo,Xianghua Zhong,Xuebing Tao,Xinyang Liu,Xi Peng,Kunyu Zhang,Peng Shi
Mesenchymal stromal cells (MSCs) hold great promise for tissue regeneration due to their potent paracrine effects. However, the absence of extracellular matrix (ECM) support following transplantation significantly compromises their survival and therapeutic efficacy. To address this, we developed a single-cell encapsulation strategy using an ECM-mimetic supramolecular hydrogel system based on host–guest chemistry. In this approach, cholesterol–polyethylene glycol–adamantane is inserted into the MSC membrane via hydrophobic interactions, enabling the subsequent formation of a uniform hydrogel coating through specific recognition between cyclodextrin- and adamantane-modified hyaluronic acids. This facile and biocompatible strategy achieves high encapsulation efficiency without the need for complex equipment, while preserving cell viability and function. Encapsulated MSCs exhibited enhanced resistance to pathological stress, improved survival, and superior therapeutic efficacy in a rat model of myocardial infarction. These findings highlight the potential of supramolecular single-cell encapsulation to augment MSC-based therapies for tissue repair and regenerative medicine.
研究领域:
再生医学
·
生物医学工程
·
细胞治疗
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生物材料
·
组织工程
✓ 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）