Penetration effect of Ostrich Oil as a Promising Vehicle on Transdermal Delivery of Sinomenine

Liu, Xin; Chen, Teng; Liu, Xuesong; Chen, Yong; Wang, Longhu

doi:10.5650/jos.62.657

Cited by 8 publications

(5 citation statements)

References 17 publications

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“…Concurrently, transdermal drug delivery might enable the drug to bypass the first pass effect (oral administration) and might provide relatively steady drug concentration in SF for long periods of time 21. Although transdermal delivery of SH has been reported, the application of the transdermal delivery system is often limited due to the stratum corneum (SC) layer, which is the primary barrier of the outermost skin layer 22. The transdermal delivery did not enable the passive diffusion of SH into the skin, thereby reducing SH efficacy.…”

Section: Introductionmentioning

confidence: 99%

Controlled release of optimized electroporation enhances the transdermal efficiency of sinomenine hydrochloride for treating arthritis in vitro and in clinic

Feng¹,

Zhu²,

Huang³

et al. 2017

DDDT

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Sinomenine hydrochloride (SH) is an ideal drug for the treatment of rheumatoid arthritis and osteoarthritis. However, high plasma concentration of systemically administered SH can release histamine, which can cause rash and gastrointestinal side effects. Topical delivery can increase SH concentration in the synovial fluid without high plasma level, thus minimizing systemic side effects. However, passive diffusion of SH was found to be inefficient because of the presence of the stratum corneum layer. Therefore, an effective method is required to compensate for the low efficiency of SH passive diffusion. In this study, transdermal experiments in vitro and clinical tests were utilized to explore the optimized parameters for electroporation of topical delivery for SH. Fluorescence experiment and hematoxylin and eosin staining analysis were performed to reveal the mechanism by which electroporation promoted permeation. In vitro, optimized electroporation parameters were 3 KHz, exponential waveform, and intensity 10. Using these parameters, transdermal permeation of SH was increased by 1.9–10.1 fold in mice skin and by 1.6–47.1 fold in miniature pig skin compared with passive diffusion. After the electroporation stimulation, the intercellular intervals and epidermal cracks in the skin increased. In clinical tests, SH concentration in synovial fluid was 20.84 ng/mL after treatment with electroporation. Therefore, electroporation with optimized parameters could significantly enhance transdermal permeation of SH. The mechanism by which electroporation promoted permeation was that the electronic pulses made the skin structure looser. To summarize, electroporation may be an effective complementary method for transdermal permeation of SH. The controlled release of electroporation may be a promising clinical method for transdermal drug administration.

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Section: Introductionmentioning

confidence: 99%

Controlled release of optimized electroporation enhances the transdermal efficiency of sinomenine hydrochloride for treating arthritis in vitro and in clinic

Feng¹,

Zhu²,

Huang³

et al. 2017

DDDT

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“…A quantitative determination method of ginsenoside Rb1 through ultra-performance liquid chromatography (UPLC) was devised and validated as per Pharmacopoeia of the People's Republic of China (2010 Edition) by using an ACQUITY UPLC System (Waters, Milford, MA) equipped with DAD detector and ACQUITY UPL® BEH C18 column (1.7 μm, 2.1 mm×50 mm, Waters). The mobile phase was a mixture of Acetonitrile and Millipore water at a ratio of 28/72 (v/v) (17)(18)(19). Different concentration of ginsenoside Rb1 was solved in PBS (pH 7.4) and aliquots of 10 μL from each sample were injected and eluted at a flow rate of 0.3 mL/min.…”

Section: Uplc Determination Of Ginsenoside Rb1mentioning

confidence: 99%

“…This ensures that the exposed surface area of the skin samples were similar between the two devices. An aliquot of receiver medium (300 μL) was collected every 30 min from the receptor chamber for 4 h, followed by the replenishment of the same volume of fresh, preheated receiver medium after each sampling interval (17,22). Three replicates were performed for each diffusion experiment.…”

Section: Rate Of In Vitro Percutaneous Permeation: Measurement and Chmentioning

confidence: 99%

The Melanogenesis-Inhibitory Effect and the Percutaneous Formulation of Ginsenoside Rb1

Wang

Lü

et al. 2014

AAPS PharmSciTech

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Ginsenoside Rb1 (Rb1) is the most predominant ginsenoside isolated from the roots of ginseng (Panax ginseng C. A. Meyer). This compound is active in various human biological pathways that are involved in human collagen synthesis and inhibition of cell apoptosis. In this study, the skin-whitening effects of Rb1 were investigated in B16 melanoma cells. Our results showed that Rb1 inhibited melanogenesis in α-melanocyte-stimulating hormone (α-MSH)-stimulated B16 cells in a dose-dependent manner, which collectively indicated that Rb1 may have skin-whitening effects and may be formulated into skin-whitening products for skin care. Accordingly, a ginsenoside collagen transdermal patch was developed as a vehicle to topically deliver Rb1 into pig skin. The percutaneous permeation, retention within skin, and release in vitro of Rb1 from seven transdermal patch formulas were studied. It was determined that the best formula for ginsenoside collagen transdermal patch is made of protein collagen hydrolysate powder (PCHP) 2.0% (w/w), methyl cellulose (MC) 0.5% (w/w), polyethyleneglycol 6000 (PEG6000) 0.5% (w/w), ginsenoside 0.036% (w/w), azone 0.4% (v/w), menthol 0.20% (w/w), and water.

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“…For example, chemical enhancers, such as membrane-penetrating peptides, usually show inefficient transdermal delivery efficiency. [25,26] Meanwhile, physical enhancement devices usually depend on large equipment to open the epithelial barrier through pulses with high energy, which may be inconvenient, expensive, and invasive. [27,28] Moreover, although microneedles have shown great potential for vaccine delivery, they could still induce slight damage to the skin with many small needles, which also has the risk of infection.…”

Section: Introductionmentioning

confidence: 99%

Noninvasive Needle‐Free Cancer Vaccine Cream Patch Based on Fluorinated Chitosan

Xiao,

Li,

Deng

et al. 2023

Adv Funct Materials

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In recent years, cancer vaccines that intend to specifically initiate host immune responses against cancer have achieved some clinical success. Delivery of vaccines with traditional needles is usually associated with the risk of infection and poor patient compliance. The development of needle‐free vaccines may overcome these limitations. In this work, a needle‐free patch is designed for effective cancer vaccination using a fluorine chain‐modified cationic polymer, fluorinated chitosan (FCS), which is able to transdermatically deliver the antigen to antigen‐presenting cells in the skin. Specifically, a transdermal carrier, FCS, and model antigen ovalbumin (OVA) can self‐assemble into nanoparticles, which can reversibly open the tight junction‐associated proteins of epithelial cells and penetrate across the epidermis. The needle‐free cancer vaccine patch is fabricated by mixing FCS‐OVA nanoparticles with the US Food and Drug Administration‐approved immune adjuvant imiquimod (R837) in blank cream. Such a needle‐free cancer vaccine can generate robust immune responses to protect mice against ovalbumin‐expressing melanoma (B16‐OVA). Compared to traditional intradermal injection, needle‐free cancer vaccines achieved an even more efficient protection effect against B16‐OVA cancer cells. This work indicated that the novel needle‐free cancer vaccine may provide a compelling technology for simple and safe vaccination, which may help to increase vaccination coverage.

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Penetration effect of Ostrich Oil as a Promising Vehicle on Transdermal Delivery of Sinomenine

Cited by 8 publications

References 17 publications

Controlled release of optimized electroporation enhances the transdermal efficiency of sinomenine hydrochloride for treating arthritis in vitro and in clinic

Controlled release of optimized electroporation enhances the transdermal efficiency of sinomenine hydrochloride for treating arthritis in vitro and in clinic

The Melanogenesis-Inhibitory Effect and the Percutaneous Formulation of Ginsenoside Rb1

Noninvasive Needle‐Free Cancer Vaccine Cream Patch Based on Fluorinated Chitosan

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