EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
·
2024
·
IF 4.4
Peng Sun,Hui Li,Kaihua Gong,Yang Zhang,Yu Cai,Chao Liu,Liang Fang
Tandospirone(Tan) is a commonly used drug for anxiety treatment. However, it has a significant first-pass effect and needs to be taken three times a day. To increase the bioavailability of the drug and reduce the number of administrations, this work amid to prepare a Tan patch that can be administered once a day by using the strategy of therapeutic deep eutectic solvent(THEDES) in cooperation with chemical permeation enhancer(CPE). In this study, four organic acids and five permeation enhancers were selected, and the optimized formulation was obtained by single-factor investigation and Box-Behnken design. The optimized formulation could significantly enhance drug loading by 2.5-fold and skin permeation up to 586.6 ± 17 μg/cm 2 in rats. Based on pharmacokinetic results, compared to oral administration, the drug exhibited a substantially elevated bioavailability, registering a 17-fold increase(from 3.01 % to 52.17 %), alongside a 10-fold rise in the mean residence time(MRT). Meanwhile, the patch was not irritating. The results of the mechanistic study showed that levulinic acid(LeA) acted as a bridge to increase the interaction between the Tan and the matrix and inhibited the crystallization of the drug in the patch, and THEDES together with CPE improved the matrix fluidity and skin permeability. This study provides a reference for the joint application of THEDES and CPEs in patch development.
研究领域:
药剂学
·
药物递送系统
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULAR PHARMACEUTICS
·
2024
·
IF 4.5
Shuai Zhang,Jiaxu Wu,Peng Sun,Liang Fang
Novel hydroxyphenyl adhesives (HP-PSAs) could significantly increase drug solubility and control drug release through a doubly ionic hydrogen bond (DIH bond) in the patch. However, chemical penetration enhancers (CPEs) always destroy the performance of most adhesives. As a result, this work investigated the stability of both the HP-PSA features and the DIH bond under the interference of the CPEs. Donepezil (DON) was chosen as the model drug, and CPEs with hydroxyl, carboxyl, amido, and ester groups were selected as model CPEs. Unlike the commonly used neutral H-bond, the DIH bond between DON and the HP-PSA was still stable under the interference of the CPEs, resulting in the 2–3-fold drug solubility in the HP-PSA, which was higher than that in the nonfunctional PSA, which reduced the drug crystallization risk and the difficulty of formulation design. FT-IR, 1H NMR, XPS, dynamic simulation, and molecular docking revealed the mechanism of the stability feature of both the DIH bond and the high drug solubility of the HP-PSA, which was that the formed neutral H-bond interaction caused by CPEs is weaker than that of the DIH bond between DON and the HP-PSA. Furthermore, the drug release, skin permeation, and CPE release study showed that the newly formed weak H-bond and strong ionic H-bond interaction promoted or controlled both DON and CPE release, respectively, thereby influencing drug skin permeation, which provided a theoretical basis for drug release regulation. To summarize, besides the reversible, strong features of the DIH bond in our previous study, the stability of the interaction made the HP-PSA’s high drug solubility potential to be applied in the TDDS.
研究领域:
药学
·
材料科学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PEST MANAGEMENT SCIENCE
·
2024
·
IF 3.8
Shuning Chen,Ao Yuan,Huafeng Wang,Daibin Yang,Li Cui,Fengjiao Hao,Xiaojing Yan,Huizhu Yuan
BACKGROUND Citrus huanglongbing (HLB) is a devastating disease in citrus, caused by Candidatus Liberibacter asiaticus (CLas), which primarily resides in the phloem where chemicals cannot effectively reach, posing a significant challenge in controlling HLB. To address these challenges, plant essential oils (EOs), widely used as transdermal enhancers and known for their benefits for plant tissues, were investigated for their potential to enhance chemical permeation. RESULTS In this study, seven EOs – eugenol, carvacrol, eucalyptol, geraniol, linalool, cinnamaldehyde, and d -limonene – were evaluated for their potential to enhance chemical penetration into citrus leaves. Preliminary screening with tracer methods revealed that geraniol provided the greatest enhancement of permeation, achieving the deepest and broadest distribution into the spongy tissue of the citrus leaf. The permeation levels of rhodamine B and crystal violet through the cuticular layer were elevated from 0.55 mg L −1 and 0.11 mg L −1 to 20.04 mg L −1 and 7.14 mg L −1 , respectively, by the addition of geraniol. Further validation through high-performance liquid chromatography–mass spectrometry (HPLC–MS) confirmed that the penetration of fludioxonil and tetracycline into citrus leaf tissues was enhanced by 15.07-fold and 20.43-fold, respectively. In planta experiments confirmed that adding geraniol to tetracycline and oxytetracycline via foliar application eliminated CLas bacteria in HLB-affected citrus more efficiently than controls. CONCLUSION Our study underscores the potential of geraniol as an effective EO-based permeation enhancer for combating HLB. By significantly improving the delivery and efficacy of bactericidal treatments, geraniol offers a promising strategy for managing this catastrophic citrus disease, potentially transforming the approach to controlling HLB. © 2024 Society of Chemical Industry.
研究领域:
植物病理学
·
农业化学
·
植物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Coatings
·
2025
·Vol. 15
·期 5
·518
·
IF 2.8
Ke Cai,Bailing Jiang
How to solve hydrogen embrittlement (HE) is a key issue that urgently needs to be addressed in the hydrogen energy industry. The use of hydrogen barrier coatings can effectively reduce the occurrence of HE. In this article, we utilized the epoxy resin (ER) as the base coating and the graphene (GN) and the silicon carbide (SiC) as the additives to prepare the (GN-ER)/(SiC-ER)/(GN-ER) sandwich structure composite hydrogen barrier coatings by the spin coating method and investigated the effect of coating composite ways on the hydrogen barrier performance. The GN-ER and the SiC-ER are used as the hydrogen barrier layer and the hydrogen capture layer, respectively, in order to improve the hydrogen barrier performances jointly. The XRD and the SEM were used to characterize their phase compositions and microstructures, and the hydrogen barrier performances were analyzed by the electrochemical hydrogen permeation curves. The adhesive strength was characterized through the pull-out method. Compared to the single-layer and the double-layer structures, sandwich structures can effectively enhance the hydrogen barrier performance of the coatings, such as the relatively low electrochemical hydrogen diffusion coefficient (Dt, 3.88 × 10−8cm2·s−1), the relatively high permeation reduction factor (PRF, 59) and adhesive strength (10.9 MPa). This research may provide a theoretical basis for improving the hydrogen barrier performance of coatings. The (GN-ER)/(SiC ER)/(GN-ER) sandwich structures composite hydrogen barrier coatings can be expected to be used in the field of safe hydrogen storage and transportation.
研究领域:
材料科学
·
表面工程
·
氢能技术
·
腐蚀防护
·
高分子复合材料
✓ 已验证
DOI
高影响因子
AAPS PHARMSCITECH
·
2021
·Vol. 22
·期 5
·1-14
·
IF 3.246
Luo Zheng,Liu Chao,Quan Peng,Zhang Yimeng,Fang Liang
Chemical penetration enhancers (CPEs) are commonly added into transdermal patches to impart improved skin permeation of drug. However, significant unexplained variability in drug release kinetics in transdermal patches is possible as a result of the addition of CPEs; investigations into the underlying mechanisms are still limited. In the present study, a diverse set of CPEs was employed to draw broad conclusions. Solubility parameters of CPEs and acrylate pressure-sensitive adhesive were calculated by molecular dynamics simulation and Fedors group contribution method to evaluate drug-adhesive miscibility. CPE-adhesive interaction was characterized by FT-IR study, 13 C NMR spectroscopy, and molecular docking simulation. Results showed that release enhancement ratio ( ER R ) of CPEs for zolmitriptan was rank ordered as isopropyl myristate > azone > Plurol Oleique ® CC497 > Span ® 80 > N -methylpyrrolidone > Transcutol ® P. It was found that solubility parameter difference (Δ δ ) between CPE and adhesive was negatively related with ER R . It was proved that hydrogen bonding between CPE and adhesive would increase drug release rate, but only if the CPE showed good miscibility with adhesive. CPE like isopropyl myristate, which had good miscibility with adhesive, could decrease drug-adhesive interaction leading to the release of drug from adhesive.
研究领域:
药剂学
·
药学化学
·
生物物理学
·
材料科学
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）