DRUG DELIVERY
·
2022
·
IF 6.819
Ming Yuan,Jiangxiu Niu,Qinghan Xiao,Huiyuan Ya,Yansong Zhang,Yanli Fan,Lingmei Li,Xueke Li
Hyaluronic acid (HA), as a hygroscopic and biocompatible molecule, has displayed unique permeation enhancement in transdermal delivery systems. Hence, indomethacin (IND) was encapsulated in HA-modified transfersomes (IND-HTs) to enhance transdermal IND delivery to reduce adverse effects in this study. The physiochemical properties of IND-HTs were characterized. Results showed that the prepared IND-HTs were spherical and revealed good entrapment efficiency (87.88 ± 2.03%), with a nanometric particle size (221.8 ± 93.34 nm). Then, IND-HTs were further incorporated into a carbopol 940 hydrogel (IND-HTs/Gel) to prolong retention capacity on the skin. The in vitro release and skin permeation experiments of IND-HTs/Gel were carried out with the Franz diffusion cells. It was found that IND-HTs/Gel exhibited sustained drug release, as well as superior drug permeation and flux across the skin. Confocal laser scanning microscopy showed improved penetration of HTs/Gel with a wider distribution and higher fluorescence intensity. The hematoxylin–eosin stained showed that HA improved the transdermal effect by changing the microstructure of skin layers and decreasing skin barrier function. In addition, IND-HTs/Gel showed significant analgesic activity in hot plate test and no potentially hazardous skin irritation. This study indicated that the developed IND-HTs/Gel could be a promising alternative to conventional oral delivery of IND by topical administration.
研究领域:
药剂学
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皮肤科学
·
生物材料
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2023
·
IF 15.1
Mi Wang,Zhenyuan Wang,Jichuan Zhang,Liguo Zhang,Wei Wang,Jingbo Zhan,Ya Liao,Chengyu Wu,Wen Yu,Jiaheng Zhang
Salicylic acid (H[Sal]) is an attractive bionic acid that is widely used in cosmetics and drugs for the treatment of skin diseases, owing to its excellent anti-acne, anti-inflammatory, antibacterial, oil-control, stratum-corneum-conditioning, and anti-photoaging abilities. However, H[Sal] is a relatively strong irritant and cannot be used on sensitive skin, and its poor water solubility limits the amounts that can be included in formulas, resulting in poor transdermal efficiency and bioavailability. In this study, we develop matrinium salicylate ([Mat][Sal]), a supramolecular ionic salt that is less cytotoxic and irritates the skin less than H[Sal], while exhibiting enhanced water-solubility, transdermal-delivery, and bioactivity properties. The anticancer, antioxidant, anti-inflammatory, and antibacterial properties of [Mat][Sal] are found to be superior or comparable to those of H[Sal]. The molecular structure of [Mat][Sal] is thoroughly investigated, including through single-crystal structure refinement, to gain an in-depth understanding of its properties. Moreover, in-vitro skin penetration experiments show that forming a salt with matrine increase the transdermal efficiency of H[Sal] while not damaging the skin barrier. The transdermal mechanisms of H[Sal] and [Mat][Sal] are studied both experimentally and using molecular dynamics simulations, which show that, compared to H[Sal], [Mat][Sal] reacts more strongly with the skin, and [Sal] − diffuses more rapidly in the skin owing to its higher water solubility and the ion-pair effect. Furthermore, [Mat][Sal] exhibits satisfactory anti-acne capabilities in a clinical-efficacy trial, highlighting its great potential for use in biomedical and cosmetics applications.
研究领域:
药理学
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化妆品科学
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分子生物学
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产品关联
DOI
高影响因子
COMPOSITES COMMUNICATIONS
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2021
·
IF 6.617
Zhi Zeng,Han-bo Feng,Meng-en Hao,Yi Zhang
Currently, high protein and fat food in daily diet often causes the prevalence of gout, which is common treated with colchicine as specific medicine. Transdermal delivery with microemulsion is very attractive for topical colchicine delivery due to its permeation enhancement across the skin barrier. However, the lack of controlled drug release ability compromises the performance of microemulsion for transdermal delivery. Herein, a colchicine transdermal delivery vehicle with one-pot approach that synchronously achieved in situ colchicine encapsulation during nano-hydroxyapatite (Hap) formation inside water/lecithin/n-propanol/isopropyl myristate microemulsion as microreactor was proposed. The optimal formulation was determined at the composition proportion (w/w) of 13% lecithin, 26% n-propanol, 53% IPM, and 8% water. This composite formulation not only possessed high transdermal flux and enhanced drug loading efficiency, but also exhibited a tunable sustained-release behaviour. This composite system combined the transdermal permeation advantage of microemulsion and controlled drug release capacity of nano-Hap, implying a promising vehicle for transdermal delivery of colchicine to produce desirable pharmacological effects.
研究领域:
药剂学
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材料科学
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皮肤病学
✓ 已验证
DOI
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2025
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IF 4.9
Yuxu Chen,Yuanyu Xu,Jingqing Zhang,Xinjun Xu
Acne vulgaris is a common skin condition affecting individuals of various age groups, significantly impacting their quality of life. Although azelaic acid (AZA) is widely used in acne treatment due to its anti-inflammatory, antibacterial, and tyrosinase inhibitory properties, its low aqueous solubility limits its transdermal absorption and reduces therapeutic efficacy. Dissolving microneedles (DMNs), fabricated from water-soluble materials, have shown great potential as a strategy for improving transdermal drug delivery. However, DMNs face challenges in encapsulating poorly soluble drugs like AZA. In this study, we developed cyclodextrin-based supramolecular DMNs loaded with AZA, in which the microneedles are composed entirely of inclusion complexes to enhance the transdermal delivery efficiency of AZA for treating acne. AZA was encapsulated into hydroxypropyl-β-cyclodextrin (HP-β-CD) and sulfobutylether-β-cyclodextrin (SBE-β-CD) using a solvent evaporation technique, resulting in respective 34.9-fold and 25.4-fold increases in AZA solubility. The inclusion complexes demonstrated superior antibacterial activity in inhibition zone assays and enhanced tyrosinase inhibitory activity compared to free AZA in aqueous solution, suggesting enhanced dispersion and biological activity. The DMNs exhibited excellent mechanical strength and maintained a high drug-loading capacity of AZA, facilitating efficient penetration through the stratum corneum. In vitro permeation test showed 24-h percutaneous permeability rates at 68.69 ± 3.79 % and 73.59 ± 4.23 % for AZA/HP-β-CD DMNs and AZA/SBE-β-CD DMNs, respectively. Additionally, the DMNs demonstrated no cytotoxicity toward L929 cells and displayed hemocompatibility. Overall, the developed supramolecular DMNs system presents a promising approach for enhancing the transdermal delivery of AZA, with the potential to enhance therapeutic outcomes in acne treatment.
研究领域:
药剂学
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皮肤病学
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生物医学工程
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产品关联
DOI
高影响因子
Current Drug Delivery
·
2021
·Vol. 18
·期 10
·1585-1594
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IF 2.565
Chen Jianmin,Wang Meixia,Ran Mengnan,Liu Xinying,Liu Siwan,Ruan Zhipeng,Jin Nan
Background: The clinical application of glabridin in treating skin diseases has been constrained by the limitations of its poor chemical stability and low skin permeability. Objective: Here, we describe Tip-loading Dissolving Microneedles (TDMNs) encapsulating drugs only in the
tips of needles for glabridin delivery with improved stability and skin permeability. Methods: The TDMNs fabricated by solvent casting technique had sufficient mechanical strength to penetrate through the excised rat's skin without fracture. Drug delivery efficiency and drug residual
in the skin of TDMNs were 63.16% and 49.28%, respectively. Glabridin encapsulated in the tips of TDMNs was effectively delivered into the abdominal skin of rat, and the in vivo delivery efficiency was inversely proportional to the drug doses. Results: Transepidermal Water Loss (TEWL)
significantly increased to 34.80 g/m2·h after the application of TDMNs and returned to normal levels (11.31 g/m2·h) after 8 h, indicating that the TDMNs were well tolerated. The stability of glabridin at room temperature was appreciably improved when loaded in TDMNs. Conclusion:
These results suggest that intradermal delivery of glabridin by TDMNs is a safe and efficient alternative to currently available routes of administration.
研究领域:
药剂学
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皮肤科学
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生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
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2016
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IF 1.566
Wenqiang Ba,Zhou Li,Lisheng Wang,Ding Wang,Weiguo Liao,Wentao Fan,Yinai Wu,Fengyun Liao,Jianye Yu
The purpose of the present study was to prepare and optimize sinomenine (SIN) pluronic lecithin organogels system (PLO), and to evaluate the permeability of the optimized PLO in vitro and in vivo. Box–Behnken design was used to optimize the PLO and the optimized formulation was pluronic F127 of 19.61%, lecithin of 3.60% and SIN of 1.27%. The formulation was evaluated its skin permeation and drug deposition both in vitro and in vivo compared with gel. Permeation and deposition studies of PLO were carried out with Franz diffusion cells in vitro and with microdialysis in vivo. In vitro studies, permeation rate (Jss) of SIN from PLO was 146.55 ± 2.93 μg/cm2/h, significantly higher than that of gel (120.39 μg/cm2/h) and the amount of SIN deposited in skin from the PLO was 10.08 ± 0.86 μg/cm2, significantly larger than that from gel (6.01 ± 0.04 μg/cm2). In vivo skin microdialysis studies showed that the maximum concentration (Cmax) of SIN from PLO in “permeation study” and “drug-deposition study” were 150.27 ± 20.85 μg/ml and 67.95 μg/ml, respectively, both significantly higher than that of SIN from gel (29.66 and 6.73 μg/ml). The results recommend that PLO can be used as an advantageous transdermal delivery vehicle to enhance the permeation and skin deposition of SIN.
研究领域:
药剂学
·
药物递送系统
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生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2023
·
IF 5.2
Yuyan Yang,Shaowei Yan,Bin Yu,Chang Gao,Kuan Chang,Jing Wang
Emulsion systems are widely used as carriers for diverse actives processing moisturizing, anti-aging, whitening and other functions. Recently, emulsions containing lamellar gel phase have been attracting more and more research interests since it improves the physical stability of degradable actives. In the present work, o/w emulsions containing lamellar gel phase composed of ceteareth-20 (O-20) and mixed fatty alcohols (FA) were developed for retinyl propionate (RP) stabilization and transdermal delivery . The lamellar gel phase was confirmed by XRD combined with cryo-SEM, and main factors for lamellar gel phase formation were investigated and discussed. Moreover, effects of carrier oil on the emulsion properties were studied and the result showed that introduction of carrier oil benefits RP retention, rheological and transdermal properties. This study proves that O-20/FA based lamellar phase emulsion is promising system for RP stabilization and utilization in cosmetic formulations.
研究领域:
化妆品科学
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药物递送系统
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材料科学
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2014
·
IF 3.785
Shumin Ge,Yuanyuan Lin,Haoyang Lu,Qi Li,Jian He,Bao Chen,Chuanbin Wu,Yuehong Xu
This project was carried out to exploit the feasibility of using microemulsion (ME) as an alternative carrier for percutaneous delivery econazole nitrate (ECN) and elucidate the underlying mechanism of permeation enhancement. The ME was developed based on Labrafil M 1944 Cs as oil phase, Solutol HS15 and Span 80 as surfactants, Transcutol P as cosurfactant and water as aqueous phase. The solubility of ECN was firstly determined for screening the ingredients of the system. Pseudo-ternary phase diagrams were constructed to formulate ME and select surfactant and cosurfactant. Central composite design-response surface methodology (CCD-RSM) was utilized to optimize the formulation of ME. The ECN loaded ME was characterized in terms of morphology, particle size and size distribution, pH value, refractive index, viscosity and conductivity, and storage stability of the ECN loaded ME was assayed. Percutaneous permeation of ECN from ME in vitro through rat skin was investigated in comparison with PBS aqueous suspension (1%, w/w), and results showed that ME enhanced drug retention in the skin and permeation through the skin, the enhancement of ME on skin deposition was further visualized through fluorescent-labeled ME by confocal laser scanning microscope (CLSM). The action mechanism of ME on improving percutaneous delivery was studied by performing a pretreatment test. It can speculate that ME does not simply behave as enhancer but it also acts as drug carrier. Furthermore, ME-skin interaction was elucidated through transmission electron microscope (TEM), and attenuated total reflectance fourier-transform infrared (ATR-FTIR). TEM was performed to visualize the micro morphological change of skin. ATR-FTIR was carried out to investigate the molecular vibrations of the components of stratum corneum (SC). The results indicate that the ME system may be a promising vehicle for percutaneous delivery of ECN.
研究领域:
药剂学
·
药物递送系统
·
皮肤生物学
✓ 已验证
DOI
高影响因子
International Journal of Nanomedicine
·
2019
·
IF 4.471
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
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生物医学工程
·
皮肤科学
✓ 已验证
DOI
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2024
·
IF 4.5
Xiaopeng Yang,Le Chang,Qian Lin,Jianing Wang,Peiqi Su,Xin Chen,Zijuan Yi,Yanming Dong,Jingwen Luo
Transdermal drug delivery against skin cancer may be more effective than oral or injection delivery because patients may be more likely to complete the treatment and it may be less likely to trigger gastrointestinal side effects. Here we developed doxorubicin-loaded nanoparticles based on cationic polyethyleneimine-oleic acid for transdermal delivery , and we applied the nanoparticles to skin pre-treated with metal microneedles to facilitate their passage through the tough epithelial barrier. The cationic nanoparticles were extremely small, which probably also facilitated their transdermal passage. They accumulated in subcutaneous melanoma tumors in mice, slowing tumor growth and inducing apoptosis. These therapeutic effects were weaker but still significant when skin was not pretreated with microneedles. Our results suggest a promising new platform for transdermal treatment of skin cancer and potentially other skin diseases.
研究领域:
药学
·
肿瘤学
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
DRUG DELIVERY
·
2022
·
IF 6.819
Jiangxiu Niu,Ming Yuan,Hongying Li,Yao Liu,Liye Wang,Yanli Fan,Yansong Zhang,Xianghui Liu,Lingmei Li,Jingxiao Zhang,Chenyu Zhao
Challenges associated with topical analgesics and anti-inflammatory drugs include poor drug penetration and retention at the desired lesion site. Therefore, improving these challenges would help to reduce the toxic and side effects caused by drug absorption into the systemic circulation and improve the therapeutic efficacy of topical therapeutic drugs. Pentapeptide (KTTKS) is a signal peptide in skin tissue, it can be recognized and bound by signal recognition particles. In the current study, we successfully prepared novel indomethacin (IMC) loaded KTTKS-modified ethosomes (IMC-KTTKS-Es), and the physicochemical properties and topical efficacy were investigated. Results showed that the prepared IMC-KTTKS-Es displayed a particle size of about 244 nm, a negative charge, good deformability, and encapsulation efficiency (EE) exceeding 80% for IMC, with a sustained release pattern. In vitro percutaneous permeation studies revealed that the skin retention was increased after the drug was loaded in the IMC-KTTKS-Es. Confocal laser scanning microscopy also showed improved skin retention of IMC-KTTKS-Es. In addition, IMC-KTTKS-Es showed improved topical analgesic and anti-inflammatory activity with no potentially hazardous skin irritation. This study suggested that the IMC-KTTKS-Es might be an effective drug carrier for topical skin therapy with a good safety profile.
研究领域:
药剂学
·
皮肤生物学
·
药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2020
·
IF 4.389
Yongqiang Zhang,Yingying Cao,Xiangzhan Meng,Chunshan Li,Hui Wang,Suojiang Zhang
A microemulsion system based on ionic liquid (IL) and deep eutectic compound was proposed to improve the transdermal delivery of artemisinin. Deep eutectic lidocaine ibuprofen (Lid·Ibu) was selected as the oil phase, and the imidazolium ionic liquid, 1-hydroxyethyl-3-methylimidazolium chloride ([HOEmim]Cl), was incorporated into the aqueous phase as a transdermal enhancer. The ingredients for the microemulsion in this study were selected, and their ratios were optimized. The optimal microemulsion carrier was composed of 45 wt% of water phase, 45 wt% surfactant phase (containing Tween-80, Span-20, and ethanol (co-surfactant) with the weight ratio of 1:1:1), and 10 wt% Lid·Ibu as the oil phase with artemisinin loading of 1.0 wt% (all the ratios were based on the total weight of microemulsion). Physical properties of this microemulsion, including particle size (41.95 ± 0.85 nm), viscosity (26.65 ± 0.13 mPa·s) and density (1.02 g/cm 3 ), were measured. In-vitro transdermal assay showed a remarkable enhancement of artemisinin transport through the skin, with the permeation flux being 3-fold of the value for iso propyl myristate system in 6 h. The impact of IL-based microemulsion (ILME) on stratum corneum (SC) was investigated by DSC, ATR-FTIR and AFM, which unveiled that the ILME possesses the ability of reducing the SC barrier by disrupting the regular arrangement of keratin, resulting in enhancement of transdermal delivery of artemisinin. This current work suggested that the microemulsion proposed here had an excellent capability to promote the transdermal delivery of artemisinin, which might also be a promising vehicle for the skin delivery of other hydrophobic natural drugs.
研究领域:
药剂学
·
皮肤科学
·
药物化学
✓ 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）