DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
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2019
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IF 2.367
Li Zhengguang,Huang Jie,Zhang Yong,Cao Jiaojiao,Wang Xingqi,Chu Xiaoqin
Objective: The purpose of this study was to research the mechanism of percutaneous penetration of Ibuprofen (IBU) nanoemulsion.Method: Transdermal penetration mechanism of IBU nanoemulsion was investigated by using Fourier transform infra-red spectral analysis (FTIR), differential scanning calorimeter thermogram (DSC), and activation energy (Ea) measurement. The in vivo skin penetration test of rats was carried out using Rhodamine B nanoemulsion to simulate the process of drug penetration into the skin, and the frozen section of the skin was observed by confocal laser scanning microscopy (CLSM).Result: FTIR spectra and DSC thermogram of rat skin treated with IBU nanoemulsion showed that infiltration occurred due to disruption of the stratum corneum (SC) protein–lipid structure and increasing of fluidity, hydration, and disruption of the lipid bilayer structure of the SC. The significant reduce in Ea (1.255 kcal/mol) for IBU permeating rat skin suggested crucial disruption of the SC lipid bilayers (P < 0.05), which is speculated that nanoemulsion may create new pathways to promote drug penetration. CLSM revealed that Rhodamine B penetrated into the SC in a shorter period of time and it accumulated around the sebaceous glands.Conclusion: The study of skin penetration mechanism indicated that nanoemulsion can be perfectly well used as the transdermal penetration of poorly soluble drugs.
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
产品关联
DOI
PubMed
高影响因子
JOURNAL OF CONTROLLED RELEASE
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2025
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IF 11.5
Wanting Dai,Xiaoxiao Song,Rui Wang,Weiwei He,Junyi Yin,Shaoping Nie
Selenium deficiency associated with a high risk of many diseases remains a global challenge. Owing to the narrow margin between “nutrition-toxicity” doses of selenium, it is imperative to achieve accurate selenium supplement. Nano‑selenium (SeNPs) is a novel form of selenium supplement with low toxicity, but it could be trapped and removed by intestinal mucus, thus limiting its oral delivery. The mucus penetration of SeNPs is highly associated with interactions between SeNPs and mucin (the structural component of mucus). In this study, we selected four polysaccharides with different functional groups and molecular weights, i.e. chitosan oligosaccharide (COS), chitosan (CS), chitosan quaternary ammonium salt (HACC), and carboxymethyl cellulose (CMC) as templates to modify SeNPs. Then we systematically explored the non-covalent interactions between polysaccharides stabilized nano-Se (PS-SeNPs) and mucin, determined and examined mucus penetration behavior and mechanism of different PS-SeNPs by coarse-grained molecular dynamics simulations, both in vitro and in vivo . It could be observed that penetration of PS-SeNPs depends on their distinct surface properties and mucus pH conditions. COS-SeNPs with short oligosaccharide chains accumulated and bridged with mucin, hindering its mucus penetration at pH 7.4. While HACC-SeNPs with NH 3 + and N + exhibited high binding affinity with mucin, inducing its mucus penetration. The negatively charged CMC-SeNPs diffused freely in mucus due to their electrostatic-repelled interaction and hydrophobic interaction with mucin. This study establishes a theoretical foundation for precise application of SeNPs in oral administration and offers valuable insights into the precise utilization of polysaccharides as tailored carriers of nanoparticles in mucus-covered tissues.
研究领域:
生物医学工程
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药剂学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
WATER RESEARCH
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2024
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IF 11.4
Shideng Yuan,Xin Yang,Na Zhang,Jiaojiao Zhang,Shiling Yuan,Zhining Wang
Membrane fouling induced by oily substances significantly constrains membrane distillation performance in treating hypersaline oily wastewater. Overcoming this challenge necessitates a heightened fundamental understanding of the oil fouling phenomenon. Herein, the adsorption and penetration mechanism of oil droplets on hydrophobic membranes in membrane distillation process was investigated at the molecular level. Our results demonstrated that the adsorption and penetration of oil droplets were divided into four stages, including the free stage, contact stage, spreading stage, and equilibrium stage. Due to the extensive non-polar surface distribution of the polytetrafluoroethylene (PTFE) membrane (comprising 95.41 %), the interaction between oil molecules and PTFE was primarily governed by van der Waals interaction. Continuous oil droplet membrane fouling model revealed that the new oil droplet molecules preferred to penetrate into membrane pores where oil droplets already existed. The penetration of resin (a component of medium-quality oil droplets) onto PTFE membrane pores required the “pre-paving” of light crude oil. Finally, the Δ E quantitative structure-activity relationships (QSAR) models were developed to evaluate the penetration mechanism of pollutant molecules on the PTFE membrane. This research provides new insights for improving sustainable membrane distillation technologies in treating saline oily wastewater.
研究领域:
环境科学
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材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
International Journal of Nanomedicine
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2017
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IF 4.3
Xia-Rong Wang,Si-Qian Gao,Xiao-Qian Niu,Long-Jian Li,Xiao-Ying Ying,Zhong-Jie Hu,Jian-Qing Gao
Capsaicin has been used in clinical applications for the treatment of pain disorders and inflammatory diseases. Given the strong pungency and high oil/water partition coefficient of capsaicin, capsaicin-loaded nanolipoidal carriers (NLCs) were designed to increase permeation and achieve the analgesic, anti-inflammatory effect with lower skin irritation. Capsaicin-loaded NLCs were prepared and later optimized by the Box–Behnken design. The physicochemical characterizations, morphology, and encapsulation of the capsaicin-loaded NLCs were subsequently confirmed. Capsaicin-loaded NLCs and capsaicin-loaded NLCs gel exhibited sustained release and no cytotoxicity properties. Also, they could significantly enhance the penetration amount, permeation flux, and skin retention amounts of capsaicin due to the application of NLCs. To study the topical permeation mechanism of capsaicin, 3,3′-dioctadecyloxacarbocyanine perchlorate (Dio) was used as a fluorescent dye. Dio-loaded NLCs and Dio-loaded NLCs gel could effectively deliver Dio up to a skin depth of 260 and 210 μm, respectively, primarily through the appendage route on the basis of version skin sections compared with Dio solution, which only delivered Dio up to 150 μm. In vivo therapeutic experiments demonstrated that capsaicin-loaded NLCs and capsaicin-loaded NLCs gel could improve the pain threshold in a dose-dependent manner and inhibit inflammation, primarily by reducing the prostaglandin E2 levels in the tissue compared with capsaicin cream and capsaicin solution. Meanwhile, skin irritation was reduced, indicating that application of NLCs could decrease the irritation caused by capsaicin. Overall, NLCs may be a potential carrier for topical delivery of capsaicin for useful pain and inflammation therapy.
研究领域:
药剂学
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药学
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药物递送系统
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药理学
✓ 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）