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International Journal of Nanomedicine · 2019 · IF 4.471

Transdermal permeability of triamcinolone acetonide lipid nanoparticles

Zhenmiao Qin,Feng Chen,Demei Chen,Yong Wang,Yinfeng Tan,Junfeng Ban

Background Triamcinolone acetonide (TAA) is an effective and the most commonly used corticosteroid hormone for the treatment of hypertrophic scars (HSs). However, the clinically used dosage has poor tissue permeability and injection safety. By contrast, lipid nanoparticles (LNPs) have the advantage of high affinity for the skin.Materials and methods This article describes the preparation of TAA-LNPs using poly(lactic-co-glycolic acid) as a carrier material, which have good biocompatibility and biodegradability. Based on a systematic investigation of its physicochemical properties, a rabbit ear HSs model was established to evaluate the percutaneous permeability of TAA-LNPs in scar tissue in vitro as well as to assess its curative effect and skin irritation.Results The results showed that the TAA-LNPs formed uniform and round particles under fluoroscopy and had a complex structure in which a nanoparticle core was surrounded by multiple vesicles. The particles were 232.2±8.2 nm in size, and the complimentary potential was -42.16 mV. The encapsulation efficiency was 85.24%, which is greater than that of other common liposomes and nanoparticles. A test of in vitro scar tissue permeability showed that penetration into scar tissue was twofold and 40-fold higher for TAA-LNPs than for common liposome and commercial suspensions, respectively. The concentration of the absorbed drug effectively inhibited fibroblast proliferation, achieved a therapeutic effect in HSs, and did not stimulate intact or damaged skin.Conclusion The preparation of TAA into LNPs for transdermal administration can enhance transdermal permeation performance and the safety of this drug, which is beneficial for the treatment of HSs.

研究领域: 药剂学 · 生物医学工程 · 皮肤科学
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Microsystems & Nanoengineering · 2025 ·Vol. 11 ·期 1 ·1-17 · IF 9.9

Paper battery powered iontophoresis microneedles patch for hypertrophic scar treatment

Gao Jie,Chen Fuqian,Wang Chen,Yang Jingbo,Zheng Ying,Liu Bin,Nie Gang,Zhu Linyu,Wu Shuo,Xie Xi,Jiang Lelun

Hypertrophic scar (HS) is a plaque fibrous and indurated dermal lesion that may cause physical, psychological, and cosmetic challenges for patients. Intralesional injection of triamcinolone acetonide (TA) is commonly used in clinical practice, which cause unbearable pain and uneven drug delivery within HS tissue. Herein, we developed a paper battery powered iontophoresis-driven microneedles patch (PBIMNP) for self-management of HS. The high integration of PBIMNP was achieved by incorporating a paper battery as the power source for iontophoresis. The transdermal drug delivery strategy of PBIMNP combined microneedles and iontophoresis techniques, involving “pressing and poking, phase transformation, and diffusion and iontophoresis”, which can actively deliver 90.19% drug into the HS tissue with excellent in vitro drug permeation performance. PBIMNP administration effectively reduced the mRNA and protein levels, leading to a decrease in the expression of TGF- β 1 and Col I associated with HS formation, demonstrating its efficacy in HS treatment. The microneedles and wearable design endow the PBIMNP as a highly promising platform for self-administration on HS treatment.

CAS / MDL: 9000-70-8
研究领域: 医学 · 生物工程 · 药剂学
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Bioactive Materials · 2021 · IF 14.593

Bilayer dissolving microneedle array containing 5-fluorouracil and triamcinolone with biphasic release profile for hypertrophic scar therapy

Beibei Yang,Yating Dong,Yifeng Shen,Ailin Hou,Guilan Quan,Xin Pan,Chuanbin Wu

Hypertrophic scar (HS) is an undesirable skin abnormality following deep burns or operations. Although intralesional multi-injection with the suspension of triamcinolone acetonide (TA) and 5-fluorouracil (5-Fu) has exhibited great promise to HS treatment in clinical, the difference of metabolic behavior between TA and 5-Fu remarkably compromised the treatment efficacy. Besides, the traditional injection with great pain is highly dependent on the skill of the experts, which results in poor compliance. Herein, a bilayer dissolving microneedle (BMN) containing TA and 5-Fu (TA-5-Fu-BMN) with biphasic release profile was designed for HS therapy. Equipped with several micro-scale needle tips, the BMN could be self-pressed into the HS with uniform drug distribution and less pain. Both in vitro permeation and in vivo HS retention tests revealed that TA and 5-Fu could coexist in the scar tissue for a sufficient time period due to the well-designed biphasic release property. Subsequently, the rabbit ear HS model was established to assess therapeutic efficacy. The histological analysis showed that TA-5-Fu-BMN could significantly reduce abnormal fibroblast proliferation and collagen fiber deposition. It was also found that the value of scar elevation index was ameliorated to a basal level, together with the downregulation of mRNA and protein expression of Collagen I (Col I) and transforming growth factor-β1 (TGF-β1) after application of TA-5-Fu-BMN. In conclusion, the BMN with biphasic release profiles could serve as a potential strategy for HS treatment providing both convenient administrations as well as controlled drug release behavior.

研究领域: 药剂学 · 皮肤科学 · 生物医学工程
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MATERIALS SCIENCE FORUM · 2018 · IF 0

Easy Preparation of Bacterial Cellulose/Triamcinolone Acetonide Composites and their Inhibition for Fibroblasts

Miao Ying Jin,Shi Yan Chen,Bao Xiu Wang,Hua Ping Wang

Wound healing is accompanied by keloids, it is important to develop a wound dressing which can inhibit keloid and relieve pain and pruritus in patients. In this paper, bacterial cellulose/triamcinolone acetonide (BC/TA) composites are prepared by easy solution impregnation method, which the structures of BC/TA composites were analyzed by fourier transform infrared spectroscopy (FTIR). The drug release and inhibition of L929 cells were also analyzed. It can be concluded that BC/TA composites have a sustained release effect on TA and can effectively inhibit proliferation of L929 in the range of 0.5-2.0 mg/cm2.

CAS / MDL: 7440-25-7
研究领域: 生物医学工程 · 药理学
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2025 · IF 4.9

Enhanced inflammatory arthritis therapy with gallic acid-modified triamcinolone acetonide: A sucrose acetate isobutyrate-based sustained release depot

Yuhang Wang,Jiang Yu,Xuejing Li,Haolin Zhang,Tengfei Zhou,Yiguo Jiang,Yongjun Wang

Inflammatory arthritis primarily involves rheumatoid arthritis (RA) and inflammatory osteoarthritis (OA), both characterized by shared inflammation in the articular joints and cartilage degeneration. These conditions lead to joint pain, loss of function, and a decline in quality of life. Triamcinolone acetonide (TA), an intermediate-acting synthetic glucocorticoid, is widely used as an anti-inflammatory agent for the treatment of inflammatory arthritis. However, its clinical application faces challenges such as rapid clearance from the joint cavity following intra-articular (IA) administration, the risk of joint damage with repeated injections, and the invasive nature of the IA injection route. To address these drawbacks, we propose sucrose acetate isobutyrate (SAIB), a biocompatible matrix, as a promising strategy for sustained drug release via intramuscular (IM) injection. Building on this approach, we designed a gallic acid-modified triamcinolone acetonide derivative (TA-GA) and incorporated it into the SAIB matrix to create the TA-GA-SAIB depot. The modification of TA with gallic acid (GA) effectively mitigates the burst release commonly observed in SAIB formulations, attributed to hydrogen bonding interactions between TA-GA and the SAIB matrix. Benzyl alcohol (BA) was selected as the optimal solvent to achieve minimal burst release during the in vitro drug release study. The TA-GA-SAIB depot exhibited sustained in vivo drug release, enhanced anti-inflammatory effects, and significant improvement in cartilage damage, along with excellent safety and biocompatibility. The synergy between the SAIB matrix and TA-GA not only enables sustained drug release but also improves therapeutic efficacy, making it a promising system for the treatment of inflammatory arthritis via intramuscular administration.

CAS / MDL: 149-91-7 76-25-5
研究领域: 药学 · 炎症免疫学
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JOURNAL OF POLYMERS AND THE ENVIRONMENT · 2022 ·Vol. 30 ·期 6 ·2579-2588 · IF 4.705

Fabrication of a Novel Fibrous Mat Based on Gliadin/Ethylcellulose Incorporated with Triamcinolone for Treatment of Oral Ulcers

Alipour Mahdieh,Aghazadeh Marziyeh,Ramezani Soghra,Taherzadeh Sana,Ghorbani Marjan,Aghazadeh Zahra

Eelectrospun fibrous mats for oral ulcer dressing should be able to attach oral mucosa in a high moisture environment and provide desirable therapeutic effects. Ethylcellulose and Gliadin are appropriate polymers in this regard. In the current study, first, Triamcinolone was integrated into Gliadin/Ethylcellulose fibrous mats (Triamcinolone/Gliadin/Ethylcellulose). Then, the chemical structure, thermal stability, mechanical properties, and morphology of Triamcinolone/Gliadin/Ethylcellulose fibrous mats were evaluated by Fourier Transform Infrared Spectroscopy, thermal gravimetric analysis (TGA), Tensile stress analysis, and scanning electron microscopy, respectively. Moreover, the biocompatibility, anti-inflammatory, and antioxidative effects of these fibrous mats were evaluated on human gingival fibroblasts. The results of SEM confirmed the uniform structure of the fabricated fibrous mats. The mechanical strength and the thermal stability of fibrous mats containing Triamcinolone were improved compared with Gliadin/Ethylcellulose fibrous mats. In vitro analysis showed the non-cytotoxicity of these fibrous mats on HGFs. Moreover, expression levels of TNF α and IL 6 in fabricated mats were 0.995 pg/mL and 0.44 pg/mL, which were significantly less than the control group. Also, the measurement of ROS activity showed significant decreases in stimulated HGFs. According to these results, it seems that the Triamcinolone/Gliadin/Ethylcellulose would be a practical mat for application in the treatment of oral inflammatory ulcers.

CAS / MDL: 9004-57-3
研究领域: 材料科学 · 药剂学 · 生物医学工程 · 牙科材料
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2020 · IF 5.162

Dextran sulfate-triamcinolone acetonide conjugate nanoparticles for targeted treatment of osteoarthritis

Peng She,Shuai Bian,Yuanqiang Cheng,Shujun Dong,Jianguo Liu,Wanguo Liu,Chunsheng Xiao

Osteoarthritis (OA) is a synovial inflammatory condition characterized by cartilage destruction and osteophyte formation. Macrophages play a central role in OA pathogenesis by producing proinflammatory cytokines. Intra-articular corticosteroid administration can relieve refractory pain and inflamed effusion of knee joints. However, limitations, such as rapid clearance from the joint space, potential damage to articular cartilage, and accelerated joint degeneration, may hamper the clinical application of corticosteroids. In this study, we reported the design and preparation of dextran sulfate-triamcinolone acetonide conjugate (DS-TA) nanoparticles (NPs) for treating OA by specifically targeting scavenger receptor class A (SR-A) on activated macrophages. We verified the excellent targeting specificity of DS-TA NPs to SR-A by flow cytometry and confocal laser scanning microscopy. DS-TA NPs were found to effectively reduce the viability of activated macrophages (RAW 264.7 cells) and the expression of proinflammatory cytokines. Intra-articular injection of DS-TA NPs effectively alleviated the structural damages to the joint cartilage, as confirmed in histopathological analysis. Additionally, DS-TA NPs decreased the expression of proinflammatory cytokines, including IL-1β, IL-6, and TNF-α, in the cartilage tissue. Thus, DS-TA NPs are a potential therapeutic nanomedicine for the targeted treatment of OA.

研究领域: 药理学 · 纳米医学 · 风湿病学 · 炎症研究
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Frontiers in Bioengineering and Biotechnology · 2023 · IF 5.7

Microneedle patches containing mesoporous polydopamine nanoparticles loaded with triamcinolone acetonide for the treatment of oral mucositis

Qu Xiaoying,Guo Xiaoli,Zhu Tingting,Zhang Zhe,Wang Wanchun,Hao Yuanping

Oral mucositis (OM) is the most common disease of the oral mucosa, which affects people’s daily production and life. Triamcinolone ointment is the common clinical drug for OM treatment. However, the hydrophobic properties of triamcinolone acetonide (TA) and the complex microenvironment of the oral cavity led to its low bioavailability and unstable therapeutic effects on ulcer wounds. Herein, dissolving microneedle patches (MNs) composed of mesoporous polydopamine nanoparticles (MPDA) loaded with TA (TA@MPDA), sodium hyaluronic acid (HA), and Bletilla striata polysaccharide (BSP) are prepared as the transmucosal delivery system. The prepared TA@MPDA-HA/BSP MNs exhibit well-arranged microarrays, high mechanical strength and fast solubility (<3 min) properties. In addition, the hybrid structure improves the biocompatibility of TA@MPDA and expedites oral ulcer healing in the SD rat model through the synergistic anti-inflammatory and pro-healing effects of microneedle ingredients (hormones, MPDA and Chinese herbs extracts), with 90% less amount of TA compared with Ning Zhi Zhu®. TA@MPDA-HA/BSP MNs are shown to be their great potential as novel ulcer dressings for OM management.

研究领域: 药学 · 纳米技术 · 药物递送系统 · 口腔健康 · 生物医学工程
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JOURNAL OF NANOBIOTECHNOLOGY · 2024 ·Vol. 22 ·期 1 ·1-22 · IF 10.6

Deep eutectic solvent self-assembled reverse nanomicelles for transdermal delivery of sparingly soluble drugs

Li Bin,Jiao Siwen,Guo Shiqi,Xiao Ting,Zeng Yao,Hu Yingwei,Li Xiaojuan,Xiong Sha,Xu Yuehong

Background Transdermal delivery of sparingly soluble drugs is challenging due to their low solubility and poor permeability. Deep eutectic solvent (DES)/or ionic liquid (IL)-mediated nanocarriers are attracting increasing attention. However, most of them require the addition of auxiliary materials (such as surfactants or organic solvents) to maintain the stability of formulations, which may cause skin irritation and potential toxicity. Results We fabricated an amphiphilic DES using natural oxymatrine and lauric acid and constructed a novel self-assembled reverse nanomicelle system (DES-RM) based on the features of this DES. Synthesized DESs showed the broad liquid window and significantly solubilized a series of sparingly soluble drugs, and quantitative structure-activity relationship (QSAR) models with good prediction ability were further built. The experimental and molecular dynamics simulation elucidated that the self-assembly of DES-RM was adjusted by noncovalent intermolecular forces. Choosing triamcinolone acetonide (TA) as a model drug, the skin penetration studies revealed that DES-RM significantly enhanced TA penetration and retention in comparison with their corresponding DES and oil. Furthermore, in vivo animal experiments demonstrated that TA@DES-RM exhibited good anti-psoriasis therapeutic efficacy as well as biocompatibility. Conclusions The present study offers innovative insights into the optimal design of micellar nanodelivery system based on DES combining experiments and computational simulations and provides a promising strategy for developing efficient transdermal delivery systems for sparingly soluble drugs.

研究领域: 药剂学 · 纳米技术 · 药物递送系统 · 材料科学 · 计算化学
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Frontiers in Bioengineering and Biotechnology · 2023 · IF 5.7

Drug-loaded mucoadhesive microneedle patch for the treatment of oral submucous fibrosis

Xian Cheng,Yanqing Yang,Zhengwei Liao,Qiao Yi,Yueying Zhou,Xiaohan Dai,Yanping Liu,Ousheng Liu

Oral submucous fibrosis is a chronic, inflammatory and potentially malignant oral disease. Local delivery of triamcinolone to lesion site is a commonly used therapy. The existing methods for local drug delivery include topical administration and submucosal injection. However, in the wet and dynamic oral microenvironment, these methods have drawbacks such as limited drug delivery efficiency and injection pain. Therefore, it is urgently needed to develop an alternative local drug delivery system with high efficiency and painlessness. Inspired by the structure of band-aid, this study proposed a novel double-layered mucoadhesive microneedle patch for transmucosal drug delivery. The patch consisted of a mucoadhesive silk fibroin/tannic acid top-layer and a silk fibroin microneedle under-layer. When applying the annealing condition for the medium content of β-sheets of silk fibroin, the microneedles in under-layer displayed both superior morphology and mechanical property. The mechanical strength of per needle (0.071N) was sufficient to penetrate the oral mucosa. Sequentially, the gelation efficiency of silk fibroin and tannic acid in top-layer was maximized as the weight ratio of tannic acid to silk fibroin reached 5:1. Moreover, in vitro results demonstrated the double-layered patch possessed undetectable cytotoxicity. The sustained release of triamcinolone was observed from the double-layered patch for at least 7 days. Furthermore, compared with other commercial buccal patches, the double-layered patch exhibited an enhanced wet adhesion strength of 37.74 kPa. In addition, ex vivo mucosal tissue penetration experiment confirmed that the double-layered patch could reach the lamina propria, ensuring effective drug delivery to the lesion site of oral submucous fibrosis. These results illustrate the promising potential of the drug-loaded mucoadhesive microneedle patch for the treatment of oral submucous fibrosis.

CAS / MDL: 7550-35-8 497-19-8
研究领域: 药学 · 生物医学工程 · 材料科学 · 牙科医学
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CARBOHYDRATE POLYMERS · 2021 · IF 9.381

Preparation of triamcinolone acetonide-loaded chitosan/fucoidan hydrogel and its potential application as an oral mucosa patch

Weiping Zheng,Yuanping Hao,Danyang Wang,Hailin Huang,Fangze Guo,Zhanyi Sun,Peili Shen,Kunyan Sui,Changqing Yuan,Qihui Zhou

Oral inflammatory diseases (OIDs) are among the most common lesions in the oral cavity, affecting the quality of human life and even causing oral cancer. However, most of the current oral mucosa patches still have some limitations, particularly instant, poor mechanical strength and conformability, low adhesion to tissue, and foreign body sensation. Herein, triamcinolone acetonide (TA)-loaded chitosan/fucoidan (CF) composite hydrogels were prepared via chemical crosslinking. The macro/microscopic morphologies and (bio)physicochemical properties of composite hydrogels were investigated. Incorporating fucoidan in chitosan hydrogels greatly enhanced their swelling behavior, mechanical strength, and adhesion properties. Further, the addition of TA in CF hydrogels improved their elastic feature, inhibited inflammatory response, and promoted the formation of mature and well-organized collagen fibers. The developed composite hydrogels displayed not only good antibacterial properties but also good cytocompatibility and histocompatibility . Thus, the designed hydrogels allow the development of oral mucosa patches as a potential treatment for OIDs.

研究领域: 药学 · 材料科学 · 生物医学工程 · 牙科
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Colloid and Interface Science Communications · 2024 · IF 4.7

Fabrication of micro-porous polymeric coating with dynamic drug-eluting property on plastic biliary stent for antiproliferative treatment

Baozhang Shi,Hao Wei,Hongyue Miu,Liangliang Li,Jianing Zhu,Yubing Huo,Liping Xu,Wei Sun

The current study aims to construct additional drug-eluting carrier for commercially available biliary stent, providing a practical strategy for the cost-efficient treatment of benign biliary stricture. Specifically, the commercially available biliary stent was endowed with porous polylactic acid coating via in-situ pore-formation induced by solvent treatment. The drug-eluting stent with fibroblast inhibition effect was successfully established by efficiently loading the antiproliferative drug of triamcinolone acetonide into the porous coating. The drug release behavior could be dynamically controlled by adjusting the pore morphology of the porous coating. The in-vitro coating degradation and the fibroblast inhibition effect of the drug-eluting stents were further evaluated to prove the effectiveness of the fabricated porous coating as an antiproliferative drug carrier.

CAS / MDL: 81-88-9 76-25-5
研究领域: 生物医学工程 · 药学 · 材料科学
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