Design of hydrogels of 5-hydroxymethyl tolterodine and their studies on pharmacokinetics, pharmacodynamics and transdermal mechanism

Liu, Wenhua; Teng, Lirong; Yu, Kongtong; Sun, Xiangshi; Fan, Chunyu; long, Chaoxing; Liu, Na; Li, Shuang; Wu, Bing; Xu, Qingji; Sun, Fengying; Li, Youxin

doi:10.1016/j.ejps.2016.10.024

Cited by 31 publications

(9 citation statements)

References 31 publications

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“…The skin was observed for any response, including redness and erythema, after the application of LN-NLC-R11 gels. In the skin irritation test, we referred to the scoring criteria in the literatures 33,34. The scores of erythema and edema were recorded (ranging from 0 to 4), and the scores were called as the irritation index.…”

Section: Methodsmentioning

confidence: 99%

<p>Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema</p>

Gao¹,

Tian²,

Han³

et al. 2019

IJN

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Background: Nanostructured lipid carriers (NLCs) are emerging as attractive drug carriers in transdermal drug delivery. The surface modification of NLCs with cell-penetrating peptides (CPPs) can enhance the skin permeation of drugs. Purpose: The objective of the current study was to evaluate the ability of the cell-penetrating peptide (CPP) polyarginine to translocate NLCs loaded with lornoxicam (LN) into the skin layers and to evaluate its anti-inflammatory effect. Methods: The NLCs were prepared using an emulsion evaporation and low temperature solidification technique using glyceryl monostearates, triglycerides, DOGS-NTA-Ni lipids and surfactants, and then six histidine-tagged polyarginine containing 11 arginine (R11) peptides was modified on the surface of NLCs. Results: The developed NLCs formulated with LN and R11 (LN-NLC-R11) were incorporated into 2% HPMC gels. NLCs were prepared with a particle size of (121.81±3.61)–(145.72±4.78) nm, and the zeta potential decreased from (−30.30±2.07) to (−14.66±0.74) mV after the modification of R11 peptides. The encapsulation efficiency and drug loading were (74.61±1.13) % and (7.92±0.33) %, respectively, regardless of the surface modification. Cellular uptake assays using HaCaT cells suggested that the NLC modified with R11 (0.02%, w/w) significantly enhanced the cell internalization of nanoparticles relative to unmodified NLCs ( P <0.05 or P <0.01). An in vitro skin permeation study showed better permeation-enhancing ability of R11 (0.02%, w/w) than that of other content (0.01% or 0.04%). In carrageenan-induced rat paw edema models, LN-NLC-R11 gels inhibited rat paw edema and the production of inflammatory cytokines compared with LN-NLC gels and LN gels ( P <0.01). Conclusion: In our investigation, it was strongly demonstrated that the surface modification of NLC with R11 enhanced the translocation of LN across the skin, thereby alleviating inflammation.

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Section: Methodsmentioning

confidence: 99%

<p>Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema</p>

Gao¹,

Tian²,

Han³

et al. 2019

IJN

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“…The shift in T m to lower temperature is interpreted as disruption of the lipid bilayer while reduction in ΔH is ascribed to fluidization of lipid bilayers. Studies have shown that the T m and △H of human skin after treated by lauramide was significantly reduced and skin permeability was increased (Liu et al, 2017). It was worth noting that the T m of human skin, pig skin, mouse skin and rabbit skin was significantly different (Kaushik and Michniak-Kohn, 2010).…”

Section: Resultsmentioning

confidence: 99%

“…At present, the main techniques to study the transdermal mechanism include Attenuated Total Reflectance Fourier Transform Infrared Spectroscopy (ATR-FTIR) (Wang et al, 2018), Confocal Laser Scanning Microscopy (CLSM) (Zhao et al, 2017), Differential Scanning Calorimeter (DSC) (Liu et al, 2017), Raman (Melot et al, 2009), Scanning Electronic Microscopy (SEM) (Park et al, 2018), Transmission Electron Microscope (TEM) (Yin et al, 2017), X-ray Photoelectron Spectroscopy (XPS) (Mandal et al, 2017) and Electron Spin Resonance (ESR) (Moll et al, 2008). These techniques have facilitated the research on transdermal mechanism.…”

Section: Introductionmentioning

confidence: 99%

Mechanism investigation of ethosomes transdermal permeation

Niu

Zhang

Bian

et al. 2019

International Journal of Pharmaceutics: X

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“…Notably, the CCAT1 expression levels in adjacent normal tissues from GC cases were higher compared with a negative control group, and recurrent GC tissues demonstrated the highest expression levels among these groups (57). Furthermore, CCAT1 overexpression is positively associated with metastasis, TNM grade, OS and RFS in patients with GC (58–60).…”

Section: Lncrna Ccat1 In Human Cancermentioning

confidence: 98%

Pivotal prognostic and diagnostic role of the long non‑coding RNA colon cancer‑associated transcript 1 expression in human cancer (Review)

Wang

et al. 2018

Mol Med Report

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Long non-coding RNAs (lncRNAs) have been classically defined as regulatory RNA members >200 nucleotides in length, without detectable open-reading frames to encode proteins. Previous studies have demonstrated that lncRNAs serve critical roles in multiple cancer types. Colon cancer-associated transcript 1 (CCAT1), a novel cancer-associated lncRNA, is significantly overexpressed in a number of malignancies. Functionally, as an oncogenic lncRNA, CCAT1 is involved in proliferation, migration, cell cycle progression, apoptosis, chemoresistance and other biological processes of cancer cells through complex regulation mechanisms in the cytoplasm or nucleus. In clinical applications, CCAT1 is additionally positively associated with histological differentiation, tumour node metastasis stage, vascular invasion, overall survival and recurrence-free survival, which demonstrates its important role as a diagnostic and prognostic marker in cancer. The present review summarises the current research progress of the oncogenic potential and clinical uses of CCAT1 in various human cancer types.

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Design of hydrogels of 5-hydroxymethyl tolterodine and their studies on pharmacokinetics, pharmacodynamics and transdermal mechanism

Cited by 31 publications

References 31 publications

<p>Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema</p>

<p>Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema</p>

Mechanism investigation of ethosomes transdermal permeation

Pivotal prognostic and diagnostic role of the long non‑coding RNA colon cancer‑associated transcript 1 expression in human cancer (Review)

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