INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2023
·
IF 5.8
Chuanhui Teng,Wei Lv,Yuqin Chen,Linfeng Liu,Jiaqing Yin,Shengnan Li,Zhiyi Min,Qi Zhang,Weichong He,Kunfang Ma,Xinrui Li,Xiang Cao,Hongliang Xin
Since ischemic stroke occurs by a combination of multiple mechanisms, therapies that modulate multiple mechanisms are required for its treatment. The combination of edaravone (EDA) and borneol can significantly ameliorate the symptoms of neurological deficits in cerebral ischemia–reperfusion model in rats. In this study, the solubility of borneol and edaravone was improved by hydroxypropyl-β-cyclodextrin and PEG 400 . Furthermore, a nasal temperature-sensitive hydrogel containing both edaravone and borneol inclusion complex (EDA-BP TSG S ) was developed to overcome the obstacles of ischemic stroke treatment including the obstruction of the blood–brain barrier (BBB) and the unavailability and untimely of intravenous injection. The effectiveness of the thermosensitive hydrogel was investigated in transient middle cerebral artery occlusion/reperfusion model rats (MCAO/R). The results showed that EDA-BP TSG S could significantly alleviate the symptoms of neurological deficits and decrease the cerebral infarct area and the degree of brain damage. In summary, nasal EDA-BP TSG S is a secure and effective brain-targeting formulation that may provide a viable option for the clinical prophylaxis and treatment of ischemic stroke.
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Frontiers in Pharmacology
·
2023
·
IF 5.6
Fanchang Wu,Mingjun Huang,Xue Zuo,Ruiye Xie,Jinman Liu,Junyu Ke,Weirong Li,Qi Wang,Yong Liang
Alzheimer’s disease (AD) poses a significant threat to the global elderly population. Traditional Chinese medicine (TCM) has been widely utilized in the treatment of AD. Osthole, a bioactive ingredient classified as an “emperor” in many TCM formulas, has been demonstrated to effectively alleviate AD symptoms. However, its low bioavailability in the brain has limited its clinical application. This study aimed to increase the intracerebral bioavailability of osthole by using borneol as a “courier,” based on the classical “Emperor–Minister–Assistant–Courier” model, and to investigate the enhanced pharmacological performance of osthole on AD. Results indicated that a suitable in situ thermosensitive gel matrix for intranasal administration mixed with osthole and borneol consists of P407 at 20%, P188 at 7%, and PEG300 at 6%. The concentration of osthole in the cerebrospinal fluid increased almost tenfold after intranasal administration of osthole/borneol compared to oral administration. Mechanisms showed that borneol as a “courier” opened up intercellular space and loosened the tight junctions of the nasal mucosa by suppressing ZO-1 and occludin expression, thereby expediting the nose-to-brain route and guiding osthole as “emperor” to its target in the brain. Osthole assisted by borneol demonstrated significantly improved efficiency in suppressing cleaved caspase-3 expression, increasing the Bcl-2/Bax ratio, improving T-SOD and catalase expression, reducing malondialdehyde levels, inhibiting neuron apoptosis, and decreasing Aβ levels by inhibiting BACE1 expression to alleviate cognitive impairment in APP/PS1 mice compared to osthole alone. Overall, our study demonstrated that the intracerebral bioavailability of osthole profoundly improved with intranasal administration of osthole/borneol and provided a wider application of TCM for AD treatment with higher intracerebral bioavailability.
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INDUSTRIAL CROPS AND PRODUCTS
·
2023
·
IF 5.9
Zehao Wang,Ru Zhao,Hongfei Gao,Yang Yang,Xinyu Yang,Huiyan Gu,Lei Yang,Xiaonan Zhang,Tingting Liu
One of the most significant sources of commercial camphor oil is the essential oil of Cinnamomum burmannii (Nees et T. Nees) Blume leaves, which has been manufactured using a variety of distillation techniques, including hydrodistillation and microwave-assisted hydrodistillation. In this study, we employed solvent-free microwave extraction (SFME) to recover hydrosol and essential oil from fresh C. burmannii leaves that had undergone screw extrusion. An optimum yield of 12.35 ± 0.62 mL/kg DW of essential oil was obtained by optimizing the major SFME contributing parameters using a face-centered central composite design (FCCCD). By using SFME, the influence of microwave irradiation power on the yield and quality of the essential oil of fresh leaves of C. burmannii was examined. With the aid of first- and second-order kinetic equations, SFME was contrasted with hydrodistillation and dry distillation. A total of 32 components were detected in the essential oil, and 22 components were detected in the hydrosol obtained by SFME under the optimized conditions. The main components of the essential oil were 1,8-cineole (21.67%), borneol (17.37%) and α -terpineol (7.45%), in descending order, and the main components of the hydrosol were trans -2-hydroxycinnamic acid (21.45%), borneol (22.07%), 1,8-cineole (13.65%) and α -terpineol (11.93%). 1,8-Cineole and borneol were the two components with the highest influence on hierarchical clustering, according to principal component analysis and heatmap analysis. Moreover, box-whisker plots were used to determine and compare the inhibitory activities of the essential oil and its three primary constituents against pancreatic lipase . The outcomes demonstrated that 1,8-cineole played a critical role in the essential oil's ability to inhibit pancreatic lipase, and they also demonstrated a positive correlation between the concentration and the amount of inhibition activity.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2019
·
IF 4.213
Lingwei Meng,Xiaoyang Chu,Haoyue Xing,Xuan Liu,Xin Xin,Liqing Chen,Mingji Jin,Youyan Guan,Wei Huang,Zhonggao Gao
Glioblastoma is a grade IV malignant glioma with high recurrence and metastasis and faces a therapeutic obstacle that the blood-brain barrier (BBB) severely hinders the brain entry and efficacy of therapeutic drugs. Previous studies suggest that borneol (BO) has been used to enhance interested drugs to penetrate the BBB. In this study, a borneol-modified nanomicelle delivery system was established to facilitate the brain entry of doxorubicin for glioblastoma therapy. Herein, we firstly conjugated borneol molecules with DSPE-PEG 2000 -COOH to synthesize a novel carrier DSPE-PEG 2000 -BO and also characterized its structure. Doxorubicin-loaded nanomicelles (DOX BO-PMs) were prepared using DSPE-PEG 2000 -BO via electrostatic interaction and the physicochemical properties were investigated. The average particle size and zeta potential of DOX BO-PMs were respectively (14.95 ± 0.17)nm and (−1.27 ± 0.06)mV, and the drug encapsulation efficiency and loading capacity in DOX BO-PMs were (95.69 ± 0.49)% and (14.62 ± 0.39)%, respectively. The drug release of the DOX BO-PMs exhibited a both time- and pH-dependent pattern. The results demonstrated that DOX BO-PMs significantly enhanced the transport efficiency of DOX across the BBB and also exhibited a quick accumulation in the brain tissues. The in vitro anti-proliferation assay results suggested that DOX BO-PMs exerted a strong inhibitory effect on proliferation of glioblastoma cells. Importantly, in vivo antitumor results demonstrated that DOX BO-PMs significantly inhibited the tumor growth and metastasis of glioblastoma. In conclusion, DOX BO-PMs can improve the glioblastoma therapeutic outcomes and become a promising nanodrug candidate for the application of doxorubicin in the field of glioblastoma therapy.
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ACS Applied Materials & Interfaces
·
2024
·
IF 8.3
Xiaobang Liu,Jiaqun Du,Junpeng Sun,Han Wang,Jinyu An,Yingqiao Li,Yu Hu,Shuai Cheng,Huicong Feng,He Tian,Xifan Mei,Yang Qiu,Chao Wu
Spinal cord injury (SCI) is a serious neurological disease that can result in paralysis. After SCI occurs, the blood–spinal cord barrier (BSCB) is disrupted, and permeability is transiently elevated. However, the permeability of the BSCB returns to normal over time, which prevents many drugs from being used in subsequent treatments. In this study, we designed a borneol-functionalized macrophage membrane encapsulating mesoporous selenium nanoparticles loaded with resveratrol (MSe-Res-BMMs) for SCI treatment. In vivo animal experiments and in vitro cell experiments demonstrated that MSe-Res-BMMs were able to protect neurons from ferroptosis by reducing ROS levels and increasing glutathione peroxidase-4 (GPx-4) activity. In addition, this treatment also reduced ROS-induced inflammation and apoptosis by decreasing the expression of inflammatory factor IL-1β and apoptotic factor Cleaved Caspase-3 at the site of injury. Therefore, MSe-Res-BMMs are expected to provide new therapeutic options for SCI treatment.
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ACTA PHARMACOLOGICA SINICA
·
2024
·
IF 6.9
He Rong-rong,Ma Chuan-rui,He Xin,Dong Yan-xi,Li Hui,Chu Zi-xuan,Yang Xi-he,Wang Jia-qi,Wang Ting,Wang Feng-qing,Du Fei-fei,Rao Ying,Yu Wen-xuan,Gao Xiu-mei,Fan Guan-wei,Cheng Chen,Li Chuan
Translational pharmacological research on traditional medicines lays the foundation for precisely understanding how the medicines function in the body to deliver therapeutic benefits. Borneolum syntheticum (Bingpian) is commonly used in Chinese herbal medicines for coronary heart disease, but its specific cardiovascular impact remains poorly understood. Isoborneol, a constituent of Bingpian, has been found to reduce lipid accumulation in macrophages in vitro, but its oral bioavailability is limited. This investigation aimed to evaluate anti-atherosclerotic effects of Bingpian, based on understanding its first-pass metabolism. Human subjects orally received an herbal medicine containing Bingpian and their plasma samples were analyzed to identify the major circulating compounds of Bingpian, with the metabolism that was also characterized in vitro and in mice. The identified compounds were evaluated for their ability to inhibit macrophage foam-cell formation induced by oxidized low-density lipoprotein. Furthermore, the anti-atherosclerotic effect of repeatedly dosed Bingpian was assessed in ApoE −/− mice fed a high-fat diet. In human subjects, the major circulating compounds of Bingpian were metabolites, rather than their precursor constituents borneol and isoborneol. These constituents were efficiently absorbed in the intestinal tract but underwent significant first-pass metabolism, involving UGT2B7-mediated glucuronidation into borneol-2- O -glucuronide and isoborneol-2- O -glucuronide, respectively, and CYP2A6/2B6/3A-mediated oxidation both into camphor. Despite their poor membrane permeability, hepatic efflux of borneol-2- O -glucuronide and isoborneol-2- O -glucuronide into the systemic circulation was enhanced by MRP3/4. The circulating metabolites, particularly their combinations, markedly inhibited macrophage foam-cell formation induced by oxidized low-density lipoprotein in vitro. Sub-chronic administration of Bingpian (30 mg·kg −1 ·d − 1 , i.g.) for 12 weeks significantly decreased atherosclerotic lesion size and enhanced plaque stability in ApoE −/− mice. Systemic exposure to Bingpian metabolites in mice closely resembles that in humans, suggesting that the pharmacodynamic effects of Bingpian in mice are likely applicable to humans. Overall, the cardiovascular benefits of Bingpian involve reducing atherosclerosis by inhibiting foam-cell formation through its metabolites. This investigation supports that oral Bingpian could be a druggable agent for reducing atherosclerosis.
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Foods
·
2025
·Vol. 14
·期 4
·682
·
IF 5.1
Huanyan Liang,Feifei Lv,Mengting Xian,Chenghua Luo,Lei Zhang,Meihua Yang,Qian Li,Xiangsheng Zhao
This investigation evaluates the comparative efficacy ofCinnamomum burmanniileaf essential oil (YXYO) and its main active ingredients as a novel preservative to protect stored food commodities from fungal infestations, aflatoxin B1(AFB1) contamination caused byAspergillus flavus. Morphological observations utilizing SEM and TEM revealed significant alterations in treated samples, alongside a decrease in ergosterol content and a dose-dependent disruption of the antioxidant system and energy system. Transcriptomic analysis suggested that differentially expressed genes were predominantly associated with spore growth, the cell wall, the cell membrane, oxidative stress, energy metabolism, and aflatoxin biosynthesis. Solid-phase microextraction–gas chromatography–mass spectrometry (SPME-GC-MS) identified ten active ingredients in YXYO, including borneol,α-terpineol, terpinen-4-ol, etc. Moreover, an effective inhibition ofA. flavusinfection in peanuts was observed with the application of 30 μL/disc of YXYO and a blend of its active compounds.
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AAPS PHARMSCITECH
·
2024
·Vol. 25
·期 7
·1-19
·
IF 3.4
Long Yanqiu,Lei Fang,Hu Jie,Zheng Zhiyun,Gui Shuangying,He Ning
The compound Salvia Recipe has been shown to have a relatively significant curative effect in management of cardiovascular and cerebrovascular diseases. This work aimed to prepare a thermosensitive in situ gel (ISG) delivery system that utilizes Poloxamer 407, Poloxamer 188, and hydroxypropyl methylcellulose for ocular administration of the compound Salvia recipe to treat cardiovascular and cerebrovascular diseases. The central composite design-response surface method was utilized to improve the prescription of the gel. The formulated gel was characterized and assessed in terms of stability, retention time, in vitro release, rheology, ocular irritation, pharmacokinetics studies, and tissue distribution. The gel was a liquid solution at room temperature and became semisolid at physiological temperature, prolonging its stay time in the eye. Pharmacokinetics and tissue distribution experiments indicated that thermosensitive ISG had enhanced targeting of heart and brain tissues. Additionally, it could lower drug toxicity and side effects in the lungs and kidneys. The compound Salvia ophthalmic thermosensitive ISG is a promising drug delivery system for the management of cardiovascular and cerebrovascular illnesses. Graphical Abstract
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Bioactive Materials
·
2024
·
IF 18
Yuhsien Lai,Xuesong Wu,Zhuoyu Jiang,Yifei Fang,Xiuting Liu,Dan Hong,Yanyun Jiang,Guozhen Tan,Shiqi Tang,Siyao Lu,David Wei,Sam T. Hwang,Kit S. Lam,Liangchun Wang,Yanyu Huang,Zhenrui Shi
Psoriasis, an immune-mediated inflammatory skin disorder characterized by a chronically relapsing-remitting course, continues to be primarily managed through topical therapy. While oral administration of tyrosine kinase 2 inhibitors (TYK2i) stands as an effective approach for psoriasis treatment, the potential efficacy of topical application of TYK2i remains unexplored. Herein, the carbomer/alginic acid hydrogel is embedded with borneol (BO) as a new topical carrier of TYK2i for achieving enhanced transdermal permeation and anti-psoriasis efficacy. The hydrogel system, i.e., TYK2i-BO-gel, exhibits significantly improved preventative and therapeutic effects in mice models of psoriasiform dermatitis, as evidenced by phenotypical images, psoriasis severity score index (PSI), histology, immunohistochemical staining, and PCR analysis. Remarkably, TYK2i-BO-gel outperforms conventional topical corticosteroid therapy by significantly preventing psoriatic lesion recurrence as measured by a nearly 50 % reduction in ear thickness changes ( p < 0.0001), PSI ( p < 0.0001) and epidermal thickness ( p < 0.05). Moreover, a strengthened anti-inflammatory effect caused by TYK2i-BO-gel is seen in a human skin explant model, implying its potential application for human patients. With the addition of BO, the TYK2i-BO-gel not only increases skin permeability but also inhibits the expression of antimicrobial peptides in keratinocytes and facilitates the anti-Th17 response of TYK2i with suppressed activation of STAT3. Therefore, this work represents the accessibility and effectiveness of TYK2i-BO-hydrogel as a new topical formulation for anti-psoriasis management and shows great potential for clinical application.
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ACS Nano
·
2024
·
IF 15.8
Guanlin Wang,Zizhao Zhai,Wenhao Wang,Xiao Xia,Haihua Guo,Xiao Yue,Xiaoyuan Wang,Bing Zhu,Zhengwei Huang,Xin Pan,Ying Huang,Chuanbin Wu,Xuejuan Zhang
The nanodrug delivery system-based nasal spray (NDDS-NS) can bypass the blood–brain barrier and deliver drugs directly to the brain, offering unparalleled advantages in the treatment of central nervous system (CNS) diseases. However, the current design of NNDS-NS is excessively focused on mucosal absorption while neglecting the impact of nasal deposition on nose-to-brain drug delivery, resulting in an unsatisfactory nose-to-brain delivery efficiency. In this study, the effect of the dispersion medium viscosity on nasal drug deposition and nose-to-brain delivery in NDDS-NS was elucidated. The optimized formulation F5 (39.36 mPa·s) demonstrated significantly higher olfactory deposition fraction (ODF) of 23.58%, and a strong correlation between ODF and intracerebral drug delivery (R2 = 0.7755) was observed. Building upon this understanding, a borneol-modified lipid nanoparticle nasal spray (BLNP-NS) that combined both nasal deposition and mucosal absorption was designed for efficient nose-to-brain delivery. BLNP-NS exhibited an accelerated onset of action and enhanced brain targeting efficiency, which could be attributed to borneol modification facilitating the opening of tight junction channels. Furthermore, BLNP-NS showed superiority in a chronic migraine rat model. It not only provided rapid relief of migraine symptoms but also reversed neuroinflammation-induced hyperalgesia. The results revealed that borneol modification could induce the polarization of microglia, regulate the neuroinflammatory microenvironment, and repair the neuronal damage caused by neuroinflammation. This study highlights the impact of dispersion medium viscosity on the nose-to-brain delivery process of NDDS-NS and serves as a bridge between the formulation development and clinical transformation of NDDS-NS for the treatment of CNS diseases.
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MACROMOLECULES
·
2025
·
IF 5.2
Xiangbin Sun,Yuanyuan Xie,Xiaobing Ma,Yufeng He,Pengfei Song,Rongmin Wang
Bacterial biofilm contamination poses a substantial threat to public health and safety while also leading to considerable economic losses. In this study, a series of both offensive and defensive poly(quaternary phosphonium salt-borneol) copolymers (P(QPx-BOy)), utilizing stereochemically structured borneol as the membrane breaking arrow and quaternary phosphonium salt cations as the electrostatic driving force, were successfully synthesized. Notably, this work exemplifies a novel integration of natural borneol with quaternary phosphonium cations. Subsequently, the molecular structure, molecular weight distribution, microstructure, and corresponding physicochemical properties of the P(QPx-BOy) were characterized using NMR, FT-IR, GPC, SEM, EDS, CA, and DLS. Leveraging the electrostatic interaction between the phosphonium cation and the stereochemical antibacterial mechanism of borneol, P(QPx-BOy) exhibited remarkable antibacterial efficacy against both E. coli and S. aureus, achieving a 100% antibacterial rate with MIC value as low as 30 μg/mL. Furthermore, crystal violet staining assays revealed that borneol’s unique antibiofilm mechanism exerts a significant inhibitory effect on bacterial biofilm formation. Finally, the biocompatibility and antibacterial potential of P(QPx-BOy) were evaluated through cytotoxicity assays and fabric antibacterial tests. Specifically, the integration of borneol essential oil with hydrophilic quaternary phosphonium salt cations effectively addresses the hydrophobic nature of borneol essential oil while mitigating the cytotoxic effects associated with quaternary phosphonium salts. This synergistic combination leverages the strengths of both components, thereby enhancing their suitability for applications in healthcare and public health sectors.
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