Journal of Oleo Science
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2013
·
IF 1.242
Xin Liu,Teng Chen,Xuesong Liu,Yong Chen,Longhu Wang
The present study investigated the feasibility of ostrich oil utilizing as a promising vehicle for improved skin permeation of sinomenine with reference to vaseline matrix containing different content of chemical enhancers. The fatty acid composition of ostrich oil was analyzed by GC-MS. Penetration enhancing potential of ostrich oil on permeation of sinomenine across rat abdominal skin in vitro was studied using an automatic diffusion cell apparatus. The content of sinomenine percutaneous absorbed was determined by HPLC. Various parameters viz. steady-state skin flux (Jss), permeability coefficient (kP), cumulative amount of sinomenine (Q) and enhancement ratios (ER) were calculated from the permeation data. Fick’s law of diffusion and Scheuplein kinetic were used to evaluate the transdermal absorbent enhancement of ostrich oil to sinomenine. Ostrich oil showed significant penetration effect on sinomenine compared with vaseline matrix containing different content of chemical enhancers, the density sequence as follow: 2% Azone > ostrich oil > 1% Azone plus 1% propylene glycol > 1% Azone > 3% Azone > 1% propylene glycol. The percutaneous endosmic rate constant (Jss) and permeability coefficient (kP) of sinomenine in ostrich oil through rat skin were 10.01 μg/cm2/h and 0.087, respectively. Ostrich oil produced stronger enhancement (ER = 24.31) with greater cumulative amount of drug permeated (255.53 μg/cm2) up to 24 h and caused no skin irritation. The drug release of sinomenine was coincided with Fick’s equation. In summary, ostrich oil containing fatty acids is proposed as a promising adjuvant for use in cosmetics and pharmaceuticals for improved permeation of drug.
研究领域:
药剂学
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皮肤科学
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DOI
高影响因子
TOXICOLOGY IN VITRO
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2024
·
IF 2.6
Nam-Hee Kang,Min Kyung Hyun,Seo Young Bang
After EU ban on animal testing for cosmetics in 2013, there has been an increasing global interest in alternatives test methods. To development for alternatives test method, we need to get the toxic data about in vitro and in vivo of chemicals. However, database sometimes provide limited in vivo and in vitro data on chemicals. Further, the data generated using the OECD TG439 ( in vitro skin irritation) are scattered in difference databases, and it is not easy to navigate through them. Therefore, we complied ‘Reference Chemical Database System for Skin Irritation Alternative Test (RCDS-Skin Irritation)’ to allow easy, one-stop access to test chemical information. We established the systematic RCDS-Skin Irritation by collecting physiochemical properties, CAS number, human data, and in vivo (OECD TG404) data from overseas chemicals database including European Chemicals Agency (ECHA) etc. , and in vitro data using Reconstructed human Epidermis (RhE) (OECD TG439). As a result, we developed the RCDS-Skin Irritation that contains information on 149 chemicals including the data we generated by performing tests using EpiDerm™ SIT, SkinEthic™ RHE and KeraSkin™ SIT. Therefore, the RCDS-Skin Irritation established based on our study will provide insight for safety assessment of chemicals and for development of alternative test methods.
研究领域:
毒理学
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生物学
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产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
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2017
·
IF 3.756
Xin Liang,Yu-lin Chen,Xiao-jing Jiang,Sheng-mei Wang,Ji-wen Zhang,Shuang-ying Gui
The main objective of this study was to develop reversed hexagonal (H II ) mesophase for transdermal delivery of methyl salicylate . The formulation was prepared, characterized and evaluated for its skin penetration in vitro and skin retention in vivo. Preliminary pharmacodynamics and skin irritation were also investigated. The formulation was identified as hexagonal structure. In vitro study exhibited that H II mesophase enhanced the skin permeation by delivering 2.61 times more methyl salicylate than the commercially available cream. Meanwhile, H II mesophase presented higher bioavailability as AUC (0–24) and AUC (0–∞) were 32.894 μg·mL − 1 and 32.935 μg·mL − 1 respectively, while the cream were 12.791 μg·mL − 1 and 12.970 μg·mL − 1 . Preliminary pharmacodynamics studies demonstrated that H II mesophase possessed anti-inflammatory and analgesic effects for inhibiting paw edema , granuloma and pain. MeSa H II mesophase showed no skin irritation on the normal rat skin. Thus, H II mesophase was considered as an effective delivery system for MeSa.
研究领域:
药剂学
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药物递送系统
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皮肤科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PROGRESS IN ORGANIC COATINGS
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2020
·
IF 4.469
Yi Zhang,Wenbo Zhang,Xiao Wang,Qianwen Dong,Xueyi Zeng,Rafael L. Quirino,Qiming Lu,Qingwen Wang,Chaoqun Zhang
Commercial hair-styling spray is often formulated with multiple components that contribute to toxicity and environmental pollution. In this work, a series of bio-based waterborne polyurethanes (CWPU) as hair styling agent were prepared from castor oil-based polyols. The resulting polyurethane dispersions exhibit excellent storage stability for at least 24 months. The effects of the castor oil functionality and chain extender structure on the particle size of the polyurethane dispersions were systematically investigated. Hair-styling performance and skin irritation tests on animals were also carefully performed to assess styling performance and safety of these CWPUs. A series of CWPU films was successfully prepared to study the relationship between the structure and performance of the bio-based polymer films. The resulting films show low moisture uptake rate, high transmittance, hydrophilicity and good mechanical properties. When CWPU films exhibit Young’s modulus >50 MPa, elongation at break in the 15–300 % range, and moisture uptake <4 %, these samples exhibit good hair-styling performance, and even better than commercial hair spray product. The skin irritation test is also proved that there is no evidence of skin irritation for these CWPUs which hold great promise for hair styling applications.
研究领域:
材料科学
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化妆品科学
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环境科学
✓ 已验证
产品关联
DOI
高影响因子
BIOORGANIC CHEMISTRY
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2023
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IF 5.1
Xuejiao Wang,Yuting Liu,Tongyue Wu,Biaofeng Gu,Hao Sun,Huanling He,Haiqin Gong,Hu Zhu
The commercial cationic surfactants (CSAa) with quaternary ammonium (QA) groups have proved to be broad-spectrum bactericide against bacteria, fungi, and viruses. Nevertheless, they inevitably exhibit potent irritation on the skin. In this work, we systematically investigated the regulatory mechanism of the host-guest supramolecular conformation with β-cyclodextrin (β-CD) on the bactericidal performance and skin irritation of CSAa with different head groups and chain lengths. When the ratio of incorporated β-CD is not greater than 1:1, the bactericidal efficiency of CSAa@β-CD (n > 12) remained above 90 % due to the free QA groups and hydrophobic fraction that can act on negatively charged bacterial membranes. And once the ratio of β-CD exceeded 1:1, the β-CD attracted to the bacterial surface by hydrogen bonding might prevent CSAa@β-CD from acting on bacteria, resulting in a decrement in antibacterial performance. Even so, the antibacterial activity of CSAa with long alkyl chains (n = 16, 18) was independent from the complexation of β-CD. Accordingly, both the zein solubilization assay and the neutrophil migration assay on zebrafish skin evidenced that β-CD attenuated the interaction of surfactant with skin model proteins and the inflammatory effect on zebrafish, thereby enhancing skin mildness. In this way, we hope to create a simple but effective brainpower using the host-guest approach to guarantee both bactericidal efficiency and skin mildness without modifying the chemical structure of these commercial biocides.
研究领域:
生物学
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医学
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化学
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产品关联
DOI
PubMed
高影响因子
PHARMACEUTICAL RESEARCH
·
2014
·Vol. 31
·期 8
·1907-1918
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IF 3.952
Chen Yang,Cun Dongmei,Quan Peng,Liu Xiaochang,Guo Wenjia,Peng Lihua,Fang Liang
Purpose Saturated long-chain esters of isopulegol were synthesized and their activities as permeation enhancers for transdermal delivery of amlodipine and flurbiprofen were investigated, in contrast to the saturated fatty acids and isopulegol, as well as their physical mixtures. Methods
In vitro permeation experiments, confocal laser scanning microscopy (CLSM) and attenuated total reflection Fourier transform infrared (ATR-FTIR) spectroscopy were introduced to investigate the regulation of enhancers in the skin permeability and biophysical properties. With in vitro cytotoxicity test and in vivo erythema model, the skin irritation of enhancers was evaluated. Results The esters significantly increased the permeation of amlodipine and flurbiprofen, whereas saturated fatty acids and isopulegol had no such effect and even decreased the drug permeation when they were used alone or in combination. These results were supported by CLSM and ATR-FTIR studies, which revealed that only the esters could decrease the order of the alkyl chains in the skin lipids. Additionally, almost no skin irritation and cytotoxicity were observed for these esters. Conclusions Saturated long-chain esters of isopulegol are shown to be suitable permeation enhancers for transdermal drug delivery. Covalent attachment of isopulegol and saturated fatty acids might represent a promising strategy to design novel and potent permeation enhancers.
研究领域:
药剂学
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生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
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2014
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IF 1.357
Yongli Shi,Yue Li,Jianming Wu,Weiguo Wang,Anjie Dong,Jianhua Zhang
Transdermal drug delivery systems (TDDS) had achieved significant success in medical practice, but still suffered from adhesion failure and skin reaction due to the occlusive properties of hydrophobic pressure sensitive adhesives (PSAs). In order to solve these problems, a novel TDDS patch based on self-adhesive Janus nanofibrous film was prepared by a multilayered electrospinning. This multifunctional patch was a bilayer structure. The subjacent layer was a hydrophobic and adhesive fibrous layer electrospun from polyacrylate PSA (HPSA), and the upper backing layer was a hydrophilic cross-linked poly (vinyl alcohol) (c-PVA) nanofibrous film. The structures of the HPSA/c-PVA composite fibrous films were characterized and their application properties, including adherence performance, water vapor permeability, water-penetration, release characteristics, and skin irritation were evaluated. The results indicated that the HPSA/c-PVA composite fibrous films could provide suitable adhesive properties for TDDS application, excellent capacity for drug loading and release, aesthetical appearance and high safety for use on the skin. Especially, due to the nanofibrous network structures and the hydrophobic–hydrophilic wettability gradient from hydrophobic HPSA layer to the hydrophilic c-PVA layer, the Janus films possessed high breathability and monodirectional water-penetration. Water could penetrate from the hydrophobic to the hydrophilic side, but could not permeate through in the opposite direction. This may provide a feasible solution to the problems caused by the water, sweat, or wound exudate on the skin, when the hydrophobic PSAs were used as matrix for TDDS and wound dressing patches.
研究领域:
材料科学
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药剂学
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生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2023
·Vol. 25
·期 1
·1-18
·
IF 3.3
Liao Shiji,Qiu Guirong,Hu Yanping,Guo Bohong,Qiu Yuqin
Colchicine is the first-line option for both the treatment and prophylaxis of gout flares. However, due to potentially severe side effects, the clinical use of colchicine is limited. A well-tolerated and safe delivery system for colchicine is widely desired. For this purpose, colchicine-loaded inseparable microneedles were fabricated using silk fibroin. Additionally, separable microneedles made of silk fibroin as the needle tips and PVP K30 as the base material were developed. Both types of microneedles were evaluated for their mechanical strength, swelling and dissolution characteristics, insertion abilities, degradation properties, in vitro penetration, skin irritation, and in vivo anti-gout effects. The results demonstrated that separable microneedles had greater mechanical strength and insertion ability. Moreover, the separable microneedles separated quickly and caused little skin irritation. In the pharmacodynamic test, mice with acute gouty arthritis responded significantly to treatment with separable microneedles. In conclusion, the separable silk fibroin-based microneedles provide a promising route for colchicine delivery. Graphical Abstract
研究领域:
药剂学
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药物递送系统
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2021
·
IF 5.875
Qing Hu,Han Lin,Yanfang Wang,Xiaoqin Wang,Jiayi Yao,Xiaoling Fu,Xiangbin Yu
The objective of the present study was to prepare and evaluate a microemulsion-based hydrogel with high malleability as a transdermal delivery carrier for levamisole (LMS). A pseudo-ternary phase diagram and D -optimal mixture design were utilized to screen and optimize the microemulsion , and the formulation comprised 7.5% Maisine TM 35-1, 33% S mix and 59.5% water. The microemulsion was physically stable with an average size of 19.3 ± 0.1 nm and zeta potential of −3.84 ± 0.05 mV. Moreover, a highly malleable alginate-boronic acid (alginate-BA) gel was prepared and could come into close contact with highly curved skin. The optimized microemulsion was loaded into alginate-BA gel and subjected to ex vivo and in vivo investigation. The microemulsion-based gel had desirable characterization, good stability and negligible skin irritation . The results of ex vivo permeation study showed that LMS achieved a significantly higher cumulative amount from the LMS-loaded microemulsion-based gel than that from the LMS-gel. The pharmacokinetic study showed a twofold increase in relative bioavailability compared to the commercial liniment . These results provide insight into the capability of the developed malleable microemulsion-based gel to enhance the transdermal permeation and bioavailability of LMS.
研究领域:
药剂学
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药物递送系统
·
制药技术
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药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
·
2022
·
IF 3.915
Yuze Sheng,Shuang Zhang,Jiawei Ling,Chenlu Hu,Zhenhai Zhang,Huixia Lv
Oxybutynin (OXY) is the most common drug to treat overactive bladder (OAB) syndrome. Transdermal administration is a more ideal route replacing oral administration to resolve problems of low bioavailability and severe side effects. However, commercial transdermal products of OXY frequently cause skin irritation and low permeation efficiency arising discontinued medication. Here, oxybutynin nanosuspension (OXY-NS) and its gel preparation (OXY-NG) were constructed to resolve these issues. In vitro permeation test and in vivo pharmacokinetics study confirmed that OXY-NG significantly enhanced the transdermal permeation of OXY, about 4-fold and 3-fold higher than oxybutynin coarse suspension (OXY-CG), respectively, and in vitro retention test certified that OXY-NG increased OXY concentration especially in viable epidermis (VE) and Dermis (about 3 times that of OXY-CG), consequently improving the bioavailability. Skin irritation assay demonstrated that OXY-NG would not trigger skin adverse effects. In addition, selectively blocking hair follicles test evidenced that hair follicles pathway played an important role in OXY-NS transdermal delivery. In general, by virtue of excellent drug loading, low toxicity and ease of scale-up, OXY-NG is a promising strategy to ameliorate skin permeation of insoluble OXY for better transdermal treatment for OAB, hence increasing its bioavailability, reducing adverse effects, and achieving good patient compliance.
研究领域:
药剂学
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药物递送系统
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药理学
✓ 已验证
DOI
PubMed
高影响因子
DRUG DELIVERY
·
2022
·
IF 6.819
Yang Liu,Xiaoruo Zhu,Shiliang Ji,Zhen Huang,Yuhui Zang,Ying Ding,Junfeng Zhang,Zhi Ding
Colchicine (Col) is used to prevent and treat acute gout flare; however, its therapeutic use is strictly limited owing to severe gastrointestinal side effects after oral administration. Therefore, we developed a dissolvable Col-loaded microneedle (MN) with hyaluronic acid to deliver Col via the transdermal route. We studied the preparation, mechanical properties, skin insertion, skin irritation, drug content, and transdermal release of the Col-loaded MN. The pharmacokinetics of Col after Col-loaded MN application were compared with those of Col solution gavage over 24 h. Knee joint edema evaluation and the hindfoot mechanical threshold test were conducted to determine the pharmacodynamic profile. The dissolvable Col-loaded MN possessed sufficient mechanical strength to penetrate the skin and release the loaded drug. No skin irritation was observed for 3 days after application. We found that 3.36-fold more Col contained in MNs was delivered through the skin compared with that in gel in vitro, and moderate relative bioavailability in vivo. The Col-loaded MN significantly relieved swollen knee joints and mechanical hypernociception in an acute gout model in rats. The dissolvable Col-loaded MN array reduced inflammation and pain via topical administration when acute gout occurred. Reducing the gastrointestinal side effects of Col-loaded MNs is expected to optimize the therapeutic effects of Col and improve patient compliance.
研究领域:
药剂学
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药物递送系统
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药理学
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生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2020
·
IF 4.845
Danping Zhang,Qiong Bian,Junjun Li,Qiaoling Huang,Jianqing Gao
Topical administration is a promising clinical strategy to avoid serious gastrointestinal adverse reactions of loxoprofen sodium (LOX), a new non-steroidal anti-inflammatory drug. Small molecule organic acids had been reported with the ability of promoting transdermal rate of several drugs. In this article, the effect of small molecule organic acids on the transdermal delivery of LOX was studied, and the possible mechanism was also explored by Fourier infrared spectroscopy , differential scanning calorimetry , tape stripping, etc. The results showed that lactic acid and fumaric acid could significantly increase the penetration rate of LOX and reduce time lag even without the help of acidic environment. The preliminary mechanism investigation inferred that fumaric acid could increase LOX’s distribution in stratum corneum and might change its complexation state, but had little effect on the drug structure and skin’s lipids and proteins configuration. The topical LOX gel using fumaric acid as penetration enhancer had higher transdermal rate, significant anti-inflammatory effect and no obvious skin irritation . This study proved the promising application of small molecule organic acids in transdermal enhancing and provided a potential strategy for transdermal delivery of LOX combined with fumaric acid.
研究领域:
药剂学
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药理学
·
药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）