ACS Applied Bio Materials
·
2025
·
IF 4.7
Beibei Lu,Bo Ruan,Jianglin Zhang,Jiaheng Zhang,Yanzhen Liang
Astaxanthin is an antioxidant with extremely high antioxidant activity. However, the stability and solubility of free astaxanthin are poor. Therefore, we prepared astaxanthin-betaine (ASTA-Bet) ionic liquid liposomes through a combination of theoretical calculations and experimental research and studied their physicochemical properties and biological effects. This liposome has good stability and skin permeability. The cumulative permeability of the ASTA-Bet ionic liquid liposome is 22.95 times that of free astaxanthin and 2.41 times that of the ASTA-Bet ionic liquid. The particle size of astaxanthin liposomes was 117.2 nm, and the particle size did not change significantly after 28 days of storage, indicating good stability. Compared with free astaxanthin, the ASTA-Bet ionic liquid liposome has good antioxidant activity and can exert antioxidant and anti-inflammatory effects by regulating the TGF-β1/smad2/smad3 pathway damaged by ultraviolet radiation, which may contribute to the resistance to ultraviolet radiation damage. Therefore, it can be used as a raw material to develop cosmetics with antiaging and anti-inflammatory functions.
研究领域:
药剂学
·
生物化学
·
皮肤科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2025
·Vol. 26
·期 11
·5249
·
IF 4.9
Lijun Ding,Xiao Luo,Weijia Wen
Obesity and associated metabolic disorders pose significant health challenges. Fucoxanthin, a lipophilic compound, has shown promising anti-obesity potential, but its poor solubility and bioavailability limit therapeutic efficacy. The successful formulation of solid lipid nanoparticles (SLNs) amplified fucoxanthin’s efficacy in mitigating obesity and the associated metabolic dysregulation. High-fat diet (HFD)-induced obese mice were treated with free fucoxanthin, lyophilized SLNs (L-SLN), and dispersed SLNs (D-SLN) loaded with fucoxanthin. The intervention with D-SLN demonstrated the most significant reduction in body weight gain (29.94%) and fat mass gain (61.80%) compared to the HFD group (p< 0.05), alongside notable improvements in metabolic indicators including fasting blood glucose, liver enzymes, lipid profile, and inflammatory markers such as leptin and monocyte chemoattractant protein 1 (MCP-1) levels. Histopathological evaluation corroborated these findings, showing highly reduced hepatic lipid droplet accumulation and improved adipocyte and testicular morphology. This advancement paved the way for translating fucoxanthin into a clinically effective anti-obesity agent.
研究领域:
药理学
·
营养学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2018
·
IF 3.862
Qilong Wang,Qiuxuan Yang,Xia Cao,Qiuyu Wei,Caleb K. Firempong,Min Guo,Feng Shi,Ximing Xu,Wenwen Deng,Jiangnan Yu
[6]-Shogaol, an alkylphenol compound purified from the root and stem of ginger ( Zingiber officinale ), has attracted considerable interest due to its potential anticancer, antioxidative and antirheumatic properties. However, the oral bioavailability of [6]-shogaol has been severely limited because of its poor solubility. In this study, a significant quantity of high-purity [6]-shogaol (yield: 3.6%; purity: 98.65%) was extracted and encapsulated in solid lipid nanoparticles (SLNs) via high-pressure homogenization (encapsulation efficiency: 87.67%) to improve its solubility and oral bioavailability. The resulting [6]-shogaol-loaded solid lipid nanoparticles (SSLNs) were stable, homogeneous and well-dispersed. Its mean particle size and zeta potential were 73.56 ± 5.62 nm and −15.2 ± 1.3 mV, respectively. Importantly, the in vitro release profile and in vivo oral bioavailability of SSLNs were significantly improved compared with the free drug. Furthermore, the SSLNs could remarkably lower the uric acid level via inhibiting the activity of xanthine oxidase and reduce the production of interleukin-1β (IL-1β) and tumor necrosis factor (TNF-α) in the hyperuricemia/gouty arthritis rat model, when compared to the free [6]-shogaol. Collectively, SLNs could serve as a promising drug delivery system to improve the oral bioavailability of [6]-shogaol for effective treatment of gouty arthritis.
研究领域:
药剂学
·
生物化学
·
纳米医学
✓ 已验证
DOI
高影响因子
Artificial Cells Nanomedicine and Biotechnology
·
2018
·
IF 3.026
Dawei Guo,Dandan Dou,Xinyu Li,Qian Zhang,Zohaib Ahmed Bhutto,Liping Wang
To avoid potential systematical toxicity, solid lipid nanoparticles (SLNs) were prepared as a vehicle for transdermal delivery of ivermectin (IVM) using hot homogenisation followed by ultrasonic method. The as-prepared SLNs were approximately spherical shape with good stability. IVM was encapsulated in amorphous form within SLNs and displayed prolonged release from SLNs without burst release due to high encapsulation efficiency (EE). The cumulative permeation of IVM across excised rat skin from SLNs was significantly increased compared to the ivermection suspension. These results indicated that the proposed SLNs can be considered as an efficient carrier for dermal delivery of IVM to effectively treat scabies.
研究领域:
药剂学
·
皮肤病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF LIPID SCIENCE AND TECHNOLOGY
·
2017
·Vol. 119
·期 9
·1600364
·
IF 2.145
Zhen Wen,Jing Lin,Junqing Su,ZongKun Zheng,Qing Chen,Lidi Chen
The aim of the present work is to evaluate influences of doping trehalose into solid lipid nanoparticles (SLNs) on drug loading. SLNs were prepared by the emulsion-evaporation and low temperature-solidification method, using glyceryl monostearate as a lipid, phosphatidylcholine as a surfactant, trehalose as a modifier and resveratrol as a model drug. As the SLNs were doped by trehalose at a low amount [ m (trehalose): m (lipids) = 1:5], entrapment efficiency and loading capacity were enhanced to (81.37 ± 1.50) and (8.71 ± 0.13)%, respectively. Based on morphology, phase transformation and crystalline structure of SLNs, trehalose was doped into lipid matrix in a non-crystalline state, disrupting the lipid crystallinity and inducing lattice defects.The lipid matrix was crystallized in polymorphic forms composed of α-form and β′-form and β-form, resulting in prevention of drug expulsion from the lipid matrix. The trehalose was interacted with the lipid, facilitating the formation of trehalose/lipid eutectic dopant. The dopant contained lattice defects, allowing for the incorporation of more resveratrol in a amorphous state, contributing to increase of entrapment efficiency and loading capacity. These results confirm stabilizing effects of doping trehalose on improvement of drug loading are attributed to the lipid crystal type and structure of lipid matrix containing lattice defects. Practical applications: Trehalose-doping is an innovative approach to the improvement of loading properties of SLNs. Compared with ordinary SLNs, SLNs doped with trehalose at low amounts exhibit higher drug loading, presenting the potential utility of these nanoparticles as a drug delivery system for hydrophobic drugs. Trehalose modification on improvement of drug loading of SLNs are attributed to the lipid crystal type and structure of lipid matrix containing lattice defects induced by doping trehalose.
研究领域:
药剂学
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
IET Nanobiotechnology
·
2015
·Vol. 9
·期 6
·355-361
·
IF 1.5
Ting Wang,Xiaojin Chen,Mengmeng Lu,Xihe Li,WenZhong Zhou
A florfenicol-loaded solid lipid nanoparticle (FFC-SLN) suspension was prepared by hot homogenisation and ultrasonic technique. The suspension was characterised for its release profile, stability, toxicity, and the physicochemical properties of the nanoparticles. Antibacterial activity of the suspension was evaluated in vitro and in vivo . The results showed that the mean diameter, polydispersity index and zeta potential of the nanoparticles were 253 ± 3 nm, 0.409 ± 0.022 and 47.5 ± 0.21 mV, respectively. In vitro release profile showed the FFC-SLN suspension had sustained release effect. The minimum inhibition concentration values of the FFC-SLN suspension were 6 and 3 µg/mL against Staphylococcus aureus and Escherichia coli respectively, compared with 3.5 and 2 µg/mL of native florfenicol. The suspension was relatively stable at 4°C and less stable at room temperature during 9 months storage. Although the nanoparticle carriers exhibited cytotoxicity in cell cultures, the LD 50 of the lyophilised dry power of the suspension was higher than 5 g/kg body weight. Mortality protection against E. coli lethal infection in mice showed that the nanoparticle suspension had much better efficacy (6/10) than native drug (1/10). These results indicate that FFC-SLN suspension could be a promising formulation in veterinary medicine.
研究领域:
兽医学
·
药剂学
·
微生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
KEY ENGINEERING MATERIALS
·
2020
·
IF 0
Benchawan Chamsai,Wipada Samprasit,Praneet Opanasopit,Pontip Benjasirimongkol,Pornsak Sriamornsak
Resveratrol (Res) loaded nanostructured lipid carriers (NLCs) were prepared by high shear homogenization and ultrasonication technique. Caprylic/capric glyceride (IM) was used as a liquid lipid, while glyceryl monostearate (GMS), beeswax (BW), palmitic acid (PA) and myristic acid (MA) at various concentrations (5, 10, 15, and 20 %w/w) were solid lipids. Polyoxyethylene 20 sorbitan monooleate or polysorbate 80 (Tween® 80) was use as a surfactant. The results showed that all concentration of PA and MA can be prepared the smaller particle NLC than that using GMS and BW according to the small molecule of MA and PA. The zeta potential of Res loaded NLCs were negative charge (-24.30 to -37.80 mV), which could be considered as a stable system. The stability studies revealed that NLCs with MA and PA showed a - high stability in particle size and zeta potential after storage at 40 ± 2°C /75 %RH for 3 months. These results suggested the MA and PA were suitable solid lipids for the NLCs preparation which have potential to be a nanoparticulate carrier for Res delivery.
研究领域:
药剂学
·
生物医学工程
✓ 已验证
DOI
FOOD CHEMISTRY
·
2024
·
IF 8.5
Bowen Yang,Cheng Chen,Weisu Huang,Tian Zhao,Shengyang Ji,Yan Liu,Baiyi Lu
In order to prevent the photooxidation of phytosterols , a new type of Pickering emulsion was developed by regulating the oriented distribution of antioxidants in colloidal lipid particles (CLPs) at the oil-water interface. High-melting-point and low-melting-point lipids were tested to modulate their protective effect against phytosterols photooxidation. Results showed that CLPs could stabilize Pickering emulsion and encapsulate antioxidants, providing a dual functional delivery system for phytosterols protection. The Pickering emulsion formed had a particle size of around 350–820 nm, and the crystallization and melting temperatures of tripalmitin particles were approximately 32 °C and 63.8 °C, respectively. The addition of tributyrin or tricaprylin reduced the crystallization and melting temperatures of Pal CLPs and improved the photooxidation emulsion stability. The prepared Pickering emulsion remained stable for a maximum of 12 days under accelerated light-induced oxidation. Among all formulations, the emulsion primarily composed of tripalmitin CLPs, with added tributyrin and resveratrol , exhibited the highest photooxidation stability.
研究领域:
食品科学
·
生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
·
2021
·
IF 3.133
Zhengwei Huang,Linjing Wu,Wenhao Wang,Wenhua Wang,Fangqin Fu,Xuejuan Zhang,Ying Huang,Xin Pan,Chuanbin Wu
Solid lipid nanoparticles (SLN) have been widely used in a variety of drug delivery routes, which have the outstanding advantage of controlled drug release. The release of SLN is dominated by many factors, among which the particle size of SLN is a critical one. The aim of this project was to explore the relationship between drug release profile and particle size of SLN. SLN were synthesized via the hot high-pressure homogenization (HPH) method, budesonide (BUD) was used as the model drug, and BUD-SLN1–BUD-SLN4 with increasing particle size was obtained, i.e. 120, 240, 360, and 480 nm. The prepared SLN has good encapsulation efficiency, drug loading capacity, and stability. In vitro release behavior studies showed that the cumulative release of BUD-SLN in Tris-Maleate (Tris-M) media was negligible, while that in Tris-M plus pancreatin media or Tris-M-ethanol media obeyed Ritger-Peppas model or first-order kinetic model, respectively. Noticeably, the release behavior of SLN was to some extent related to the average particle size of SLN, but the correlation was insignificant when the intersection degree of particle size distribution was great. This study provides a new idea for the understanding of in vitro release of SLN and has a certain referencing value for the research and development of novel nanomedicines.
研究领域:
药剂学
·
纳米医学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY
·
2022
·Vol. 57
·期 5
·2886-2895
·
IF 3.612
Yunwei Lin,Wenting Yin,Yujie Li,Guoqin Liu
Summary This study aimed to investigate the effect of solid lipids (lauric acid (LAU), myristic acid (MYR), stearic acid (STE), glycerol monostearate (GMS), glycerol 1,3-distearate (GDS), glycerol tristearate (GTS), glycerol trimyristate (GTM) and glycerol trilaurate (GTL)) on the characteristics of novel nanostructured lipid carrier (NLC) containing Antarctic krill oil through ultrasound. The fatty acids (LAU, MYR, STE and GMS) were unsuitable solid lipid materials, as apparent stratification was quickly observed during the NLC preparation. NLCs were successfully prepared using GTS, GTM, GTL and GDS. The zeta potential of all NLCs exceeded −30 mV indicating good uniformity and stability. These NLCs appeared spherical or oval. Differential calorimetry and X-ray diffraction analysis revealed these NLCs formed imperfect crystals. As the carbon chain length of triglycerides increased from C 12 to C 18 , the particle size of NLCs increased from 235.8 ± 2.3 nm to 340.5 ± 2.2 nm, the degree of recrystallisation increased from 39.06% to 49.99%, while the EPA encapsulation efficiency decreased from 88.72 ± 0.47% to 72.86 ± 1.06%. NLC prepared with GDS had the smallest particle size (112.4 ± 0.4 nm), the lowest recrystallisation and the highest EPA encapsulation efficiency (>99%). GDS was the most suitable to prepare high encapsulate efficiency krill oil-loaded NLC.
研究领域:
食品科学
·
药剂学
✓ 已验证
产品关联
DOI
高影响因子
Pharmaceutics
·
2023
·Vol. 15
·期 3
·866
·
IF 5.4
Lei Shu,Wenhua Wang,Chon-iong Ng,Xuejuan Zhang,Ying Huang,Chuanbin Wu,Xin Pan,Zhengwei Huang
Background: Delivery of inhalable nanoparticles through metered-dose inhalers (MDI) is a promising approach to treat lung disease such as asthma and chronic obstructive pulmonary disease. Nanocoating of the inhalable nanoparticles helps in stability and cellular uptake enhancement but complicates the production process. Thus, it is meaningful to accelerate the translation process of MDI encapsulating inhalable nanoparticles with nanocoating structure. Methods: In this study, solid lipid nanoparticles (SLN) are selected as a model inhalable nanoparticle system. An established reverse microemulsion strategy was utilized to explore the industrialization potential of SLN-based MDI. Three categories of nanocoating with the functions of stabilization (by Poloxamer 188, encoded as SLN(0)), cellular uptake enhancement (by cetyltrimethylammonium bromide, encoded as SLN(+)), and targetability (by hyaluronic acid, encoded as SLN(−)) were constructed upon SLN, whose particle size distribution and zeta-potential were characterized. Subsequently, SLN were loaded into MDI, and evaluated for the processing reliability, physicochemical nature, formulation stability, and biocompatibility. Results: The results elucidated that three types of SLN-based MDI were successfully fabricated with good reproducibility and stability. Regarding safety, SLN(0) and SLN(−) showed negligible cytotoxicity on cellular level. Conclusions: This work serves as a pilot study for the scale-up of SLN-based MDI, and could be useful for the future development of inhalable nanoparticles.Keywords:inhalation;solid lipid nanoparticle;metered-dose inhaler;pilot study;nanocoating
研究领域:
药剂学
·
纳米技术
·
肺医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
DRUG DELIVERY
·
2023
·
IF 6
Huamei Li,Fuda Dai,Hanyu Liu,Qi Tao,Jie Hu,Yangrong Zhang,Zhenping Xiao,Ilva D. Rupenthal,Huihui Li,Fan Yang,Wei Li,Huaqing Lin,Dongzhi Hou
Recently, various novel drug delivery systems have been developed to overcome ocular barriers in order to improve drug efficacy. We have previously reported that montmorillonite (MT) microspheres (MPs) and solid lipid nanoparticles (SLNs) loaded with the anti-glaucoma drug betaxolol hydrochloride (BHC) exhibited sustained drug release and thus intraocular pressure (IOP) lowering effects. Here, we investigated the effect of physicochemical particle parameters on the micro-interactions with tear film mucins and corneal epithelial cells. Results showed that the MT-BHC SLNs and MT-BHC MPs eye drops significantly prolonged the precorneal retention time due to their higher viscosity and lower surface tension and contact angle compared with the BHC solution, with MT-BHC MPs exhibiting the longest retention due to their stronger hydrophobic surface. The cumulative release of MT-BHC SLNs and MT-BHC MPs was up to 87.78% and 80.43% after 12 h, respectively. Tear elimination pharmacokinetics study further confirmed that the prolonged precorneal retention time of the formulations was due to the micro-interaction between the positively charged formulations and the negatively charged tear film mucins. Moreover, the area under the IOP reduction curve (AUC) of MT-BHC SLNs and MT-BHC MPs was 1.4 and 2.5 times that of the BHC solution. Accordingly, the MT-BHC MPs also exhibit the most consistent and long-lasting IOP-lowering effect. Ocular irritation experiments showed no significant toxicity of either. Taken together, MT MPs may have the potential for more effective glaucoma treatment.
研究领域:
药剂学
·
眼科医学
✓ 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）