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JOURNAL OF NANOBIOTECHNOLOGY · 2025 ·Vol. 23 ·期 1 ·1-20 · IF 12.6

Black phosphorus nanosheets encapsulated microneedle for multifunctional therapy for androgenic alopecia

Xiong Sha,Li Zhongjun,Jiao Siwen,Xiao Ting,Wu Yan,Chen Chen,Guo Shiqi,Li Xiaojuan,Pan Zhiyuan,Li Jianqing,Xu Yuehong

Background Androgenetic alopecia (AGA), a chronic and progressive disease, significantly impacts the patients’ social, emotional, and mental well-being. Current treatment for AGA are mainly limited by drug side effects and the stratum corneum (SC) barrier of scalp. Results To address these issues, we developed a microneedle (MN) system loaded with black phosphorus nanosheets (BP) encapsulating baicalin (BA), a natural ingredient, for effective treatment of AGA. We first fabricated BP-BA based on the BP properties of high drug loading capacity and excellent photothermal conversion efficiency. Upon 635 nm laser irradiation, BP-BA demonstrated efficient photothermal conversion to mild thermal of ~ 42 °C. This mild thermal effect controlled BA’s stimuli-responsive release, enhanced cellular uptake, and effectively modulated gene expression in dihydrotestosterone-treated human dermal papilla cells, downregulating negative regulators such as SRD5A2, AR, DKK1, and TGFB1, while upregulating positive regulators like CTNNBIP1 and VEGFA. Furthermore, we encapsulated BP-BA to MN fabricating BP-BA@MNs to overcome the SC barrier. Compared with BP-BA@MNs without laser irradiation, BP-BA@MNs with laser irradiation significantly enhanced drug penetration into the subcutaneous area and accumulation at the follicular site. Importantly, BP-BA@MNs demonstrated synergistic efficacy against testosterone-induced AGA in vivo through combining BA chemotherapy, BP-mediated mild photothermal therapy, and MN delivery, as well as good biocompatibility and biosafety, and the underlying synergistic mechanism was elucidated in terms of follicular microenvironment reconstruction. Conclusions This combining BP mild photothermal and MN system is a promising approach for follicular targeted drug delivery, providing a multifunctional strategy for addressing the clinical needs of anti-AGA. Graphical

研究领域: 药剂学 · 皮肤病学 · 生物医学工程
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EUROPEAN POLYMER JOURNAL · 2021 · IF 4.598

Polyether fluorinated amphiphilic diblock polymer: Preparation, characterization and application as drug delivery agent

BinXiao Wei,Xiang Guo,YuTao Cui,ShouChun Ma,Wei Li,YongPing Bai

Amphiphilic polymers or polymeric surfactants forming nano micelles in water have been considered as suitable candidates for loading poor water solubility drugs as they are often featured as excellent bioavailability, biodegradation and entrapment ability. Therefore, in this paper we prepared a series of polyether MPEG-EPTF fluorinated diblock polymers (copolymer of poly(ethylene glycol) monomethyl ether and fluorinated epichlorohydrin) with different composition and molecular weight through living cationic polymerization. The critical micelle concentration (CMC) of these fluorinated polymers and the effect of structure on surface activity are researched in this paper. The particle sizes of nano micelles determined by transmission electron microscopy (TEM) are less than 100 nm, which can perfectly meet the size requirements of micelles used in human body. Besides, the fluorinated amphiphilic polymer can also be employed to load and carry baicalin so as to enhance its solubility in water, and the drug loading (DL) and entrapment efficiency (EE) of these nano systems are very outstanding, reaching to approximately 77.58% and 38.79% respectively. Cumulative release pattern in vitro tested by UV–vis had shown that little amounts baicalin (about 20%) are released over 60 h in vitro.

CAS / MDL: 9004-74-4 2258654-78-1
研究领域: 材料科学 · 药学
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MOLECULAR PHARMACEUTICS · 2023 · IF 4.9

A Multifunctional Liposome for Synergistic Chemotherapy with Ferroptosis Activation of Triple-Negative Breast Cancer

Jingjing Chai,Jiawei Hu,Tao Wang,Xing Bao,Jiajie Luan,Yan Wang

There is an urgent need to develop efficient treatments for highly invasive triple-negative breast cancer (TNBC) with a high rate of postoperative. Baicalin (BA) has shown inhibitory effects on several tumor cells and could activate ferroptosis in some tumor cells by producing reactive oxygen species (ROS). For overcoming the shortcomings of BA in clinical applications and enhancing the effect of ferroptosis in TNBC, herein, a multifunctional liposome (BA-Fe(III) coordination-polymer-loaded liposome, BA-Fe(III) Lipo) was developed for synergistic chemotherapy of TNBC with ferroptosis activation. Fe(III) released from BA-Fe(III) Lipo could be efficiently reduced to Fe(II) in the presence of high glutathione in tumor microenvironment, which in turn catalyzed the oxidation of unsaturated fats through lipid peroxidation for more ROS production. In addition, BA-Fe(III) Lipo activated tumor cell ferroptosis by down-regulating the enzymatic activity of ferritin heavy chain 1 protein and glutathione peroxidase. This study provided a novel therapeutic strategy for the treatment of TNBC by ingeniously combining chemotherapy with the activation of ferroptosis, which presented potential clinical applications.

CAS / MDL: 1510-21-0 39382-08-6
研究领域: 肿瘤学 · 药剂学 · 生物化学
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RSC Advances · 2015 ·Vol. 5 ·期 52 ·41377-41384 · IF 3.84

Synthesis of surface nano-molecularly imprinted polymers for sensitive baicalin detection in biological samples

Xiaoli Gu,Hongliang He,Chong-zhi Wang,Yankun Gao,Hongjuan Zhang,Junli Hong,Shuhu Du,Lina Chen,Chun-su Yuan

Surface molecularly imprinted polymers (MIP@SBA-15) imprinted on the surface of hybrid nanostructured organic/inorganic materials (SBA-15) were prepared for the selective extraction and detection of baicalin (BA) in biological samples. The surface morphologies and characteristics of the imprinted and non-imprinted polymers were characterized by Fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), transmission electron microscopy (TEM), thermogravimetric analysis (TGA) and nitrogen adsorption–desorption isotherms. The results indicated that the polymers were successfully grafted onto the surface of SBA-15 and possessed a highly ordered mesoporous structure. In binding tests, MIP@SBA-15 reached saturated adsorption within 80 min and exhibited significant specific recognition toward BA with a large adsorption capacity. In addition, the prepared MIP@SBA-15 was used as a selective sorbent for solid-phase extraction of BA from biological samples. Recoveries of BA from the liver and spleen ranged from 90.6% to 90.9% with RSD <3.7%. All these results reveal that this method is simple, rapid and sensitive for effectively extracting and detecting trace BA in biological samples.

CAS / MDL: 2530-85-0
研究领域: 分析化学 · 药物分析 · 材料科学
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ACS Applied Polymer Materials · 2021 · IF 4.089

Fluorinated Polymeric Surfactant with a Pluronic-like Structure and Its Application as a Drug Carrier

Binxiao Wei,Yutao Cui,Shouchun Ma,Yu Wang,Xiang Guo,Jinwu Xiao,Wei Li,Aimin Pang,Yongping Bai

Pluronics (PEO-PPO-PEO or PPO-PEO-PPO), as the first commercially used polymeric surfactants, designed and manufactured by BASF, have been applied in the development of many pharmaceutical formulations and drug load as well as delivery. Herein, the Williamson ether synthesis reaction was used to prepare hydrophobic monomer fluorinated epichlorohydrin (EPTF) considered as an intermediate state before. In addition, ABA triblock amphiphilic polymers (molecular weight ranging from 2083 to 8888 g/mol with the polymer dispersity index (PDI) lower than 1.52) with a Pluronic-like structure were synthesized by the living cationic polymerization of polyethylene oxide (PEO) and EPTF. The structures of EPTF and polymeric surfactants were characterized by Fourier infrared transform spectroscopy (FI-IR), nuclear magnetic resonance (NMR), and gel permeation chromatography (GPC). Moreover, these kinds of polymeric surfactants can not only reduce the surface tension of water but also self-assemble in water to form micelles with a much lower critical micelle concentration (CMC) ranging from 8.13 × 10–5 to 1.95 × 10–3 g/L. Baicalin, low-water-solubility anticancer drug, can be loaded into this polymeric surfactant to form nanomicelles by a solvent evaporation method. The particle size, colloidal stability, and loaded content were characterized by dynamic light scattering (DLS), transmission electron microscopy (TEM), and ultraviolet–visible (UV–vis) spectrometry. These results indicate that hydrophobic anticancer drugs, like baicalin, can be loaded into these kinds of surfactants with a much higher concentration (maximum 380.776 μg/mL) and excellent storage stability, overcoming their low water solubility so as to increase their therapeutic efficacy.

研究领域: 药剂学 · 材料科学 · 肿瘤学
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Journal of Materials Chemistry B · 2015 ·Vol. 3 ·期 39 ·7734-7744 · IF 4.726

Sterically stabilized spongosomes for multidrug delivery of anticancer nanomedicines

Yiyin Chen,Angelina Angelova,Borislav Angelov,Markus Drechsler,Vasil M. Garamus,Regine Willumeit-Römer,Aihua Zou

Multidrug delivery devices are designed to take advantage of the synergistic effects of anticancer agents in combination therapies. Here we report novel liquid crystalline self-assembled nanocarriers enhancing the activity of the phytochemical anticancer agent baicalin (BAI) in combination with Brucea javanica oil (BJO), which ensures safe formulations for clinical applications. Small-angle X-ray scattering (SAXS) and cryogenic transmission electron microscopy (cryo-TEM) evidenced the multicompartment, sponge-type nano-organization of the blank and multidrug-loaded liquid crystalline carriers. Physico-chemical stability of the sponge nanoparticles was achieved through PEGylation of the lipid membranes, which make up the drug nanocarriers. The proposed green nanotechnology for nanocarrier preparation by supramolecular self-assembly provided a multidrug encapsulation efficiency as high as 75%. The apoptosis study with the human lung carcinoma cell line A549 demonstrated improved efficacy of the multidrug delivery nanocarriers in comparison to the single-drug reservoirs. The obtained results evidenced the synergistic anticancer apoptotic effects of the multidrug-loaded nanosponge carriers and suggested the opportunity for in vivo translation towards the treatment of lung, gastrointestinal, and ovarian cancers.

CAS / MDL: 21967-41-9
研究领域: 药剂学 · 癌症治疗 · 纳米技术 · 细胞生物学
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