Sinomenine hydrochloride-loaded dissolving microneedles enhanced its absorption in rabbits

Wu, Xiaoyan; Chen, Y; Shen, Guanghui; Chen, L; Cao, Yongtong; Yin, Daqiang; Ma, Ping

doi:10.3109/10837450.2015.1055766

Cited by 15 publications

(12 citation statements)

References 59 publications

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“…However, oral SH can cause adverse reactions such as gastrointestinal irritation and a first-pass effect. Injections are more expensive and require professional training for administration (Wu et al, 2016;Arya et al, 2017). Transdermal drug delivery is an attractive alternative to oral administration or injection, and early studies confirmed that it could overcome the above-mentioned problems (Prausnitz & Langer, 2008;Romgens et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

Polyvinylpyrrolidone microneedles for localized delivery of sinomenine hydrochloride: preparation, release behavior of in vitro & in vivo, and penetration mechanism

et al. 2020

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Sinomenine (SIN) is an anti-inflammatory alkaloid derived from Sinomenium acutum, and the products sinomenine hydrochloride (SH) tablets and injections have been marketed in China to treat rheumatoid arthritis (RA). Oral administration of SH has shortcomings of gastrointestinal irritation and low bioavailability. The injection may require professional training and higher cost. It is of interest to develop an alternative form that is easier to administer and avoids the first-pass metabolism. In this study, SHloaded dissolving microneedles (SH-MN) were fabricated using polyvinyl pyrrolidone and chondroitin sulfate with a casting method. In percutaneous permeation studies of In vitro, the cumulative permeation and permeation rate of SH-MN were 5.31 and 5.06 times higher than that of SH-gel (SH-G). In percutaneous pharmacokinetic studies, the values of the area under the curve after administration of SH-MN in the skin and blood were 1.43-and 1.63-fold higher than that of SH-G, respectively. In percutaneous absorption studies, SH-MN could absorb into tissue fluid; and dissolve after skin penetration. The drug was released along the channel and spread to surrounding skin tissue. After 4 h, the needle tip was almost completely dissolved, and the drug could penetrate to a depth of 200 lm under the skin. These results demonstrate that the SH-MN is an effective, safe, and simple strategy for transdermal SH delivery.

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Section: Introductionmentioning

confidence: 99%

Polyvinylpyrrolidone microneedles for localized delivery of sinomenine hydrochloride: preparation, release behavior of in vitro & in vivo, and penetration mechanism

et al. 2020

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“…This also eliminates any potential risk of biohazardous sharp waste. Sustained delivery from the MN baseplates is also possible for small molecules (Wu et al, ). DMN has been widely used to deliver hydrophilic drugs, as such molecules are easy to mix with water‐soluble polymers used for DMN preparation (Donnelly et al, ).…”

Section: Introductionmentioning

confidence: 99%

Novel nanosuspension‐based dissolving microneedle arrays for transdermal delivery of a hydrophobic drug

Vora

Vavia

Larrañeta

et al. 2018

J of Interdiscip Nanomed

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A nanosuspension (NS) was formulated from the lipophilic molecule cholecalciferol (CL) for enhanced transdermal delivery by embedding this NS into hydrophilic polymer‐based dissolving microneedles (DMNs). First, the NS was prepared by sonoprecpitation with different molecular weights of poly (vinyl alcohol) and poly (vinyl pyrrolidone) as stabilizers and using two different solvents for particle size and zeta potential optimization. DMN arrays were then prepared by centrifugation‐assisted micromoulding and subsequently dried. Poly (vinyl alcohol) (10 kDa) produced a NS with the lowest particle size ( ~ 300 nm). These particles yielded DMN with good mechanical properties when combined with aqueous blends of high molecular weight poly (vinyl pyrrolidone) (360 kDa). The particle size remained similar before and after MN preparation, as confirmed by scanning electron microscope. The CL was in the amorphous state in the free particles as well as in the DMN and, hence, no characteristic CL peak was observed in differential scanning calorimetry or X‐ray diffraction. DMN arrays were found to be strong enough to bear a 32 N force, showed efficient skin insertion, and penetrated down to the third layer (depth ≈ 375 μm) of the validated skin model Parafilm M®. An ex vivo porcine skin permeation study using Franz diffusion cells compared the permeation of CL from CL‐NS‐loaded DMN arrays and MN‐free CL‐NS patches. It was observed that CL‐NS‐loaded DMN arrays showed significantly higher (498.19 μg ± 89.3 μg) ex vivo skin permeation compared with MN‐free CL‐NS patches (73.2 μg ± 26.5 μg) over 24 h. This is the first time a NS of a hydrophobic drug has been successfully incorporated into dissolving MN and suggest that NS‐containing DMN systems could be a promising strategy for transdermal delivery of hydrophobic drugs.

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“…However, the control of morphine was very strict, accordingly, it is difficult to be obtained. It was reported by Wu et al, that the external standard method was used to determine the plasma concentration of sinomenine hydrochloride 19. The representative chromatograms of blank rabbit plasma, and blank rabbit plasma spiked with sinomenine hydrochloride were shown in Figure 2A.…”

Section: Resultsmentioning

confidence: 99%

<p>Enhanced transdermal permeability and drug deposition of rheumatoid arthritis via sinomenine hydrochloride-loaded antioxidant surface transethosome</p>

Song¹,

Wen

et al. 2019

IJN

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Background: Transdermal drug delivery system (TDDS) curing rheumatoid arthritis (RA) for long-term treatment can improve patients’ compliance and reduce the accumulation of drug side effects. However, TDDS is constrained by the tight junction of the stratum corneum and low permeation efficiency. It is necessary to adopt proper permeation methods to ensure the therapeutic effect. The transethosome (TE), which is derived from transfersome and ethosome (E), containing a high content of ethanol along with an edge activator or permeation enhancer, has superior deformability and higher permeation efficiency. Methods and Results: In this study, sinomenine hydrochloride-loaded TE was decorated with ascorbic acid to form antioxidant surface transethosome (AS-TE). It was revealed that TE and AS-TE containing sodium deoxycholate can effectively increase the entrapment efficiency of hydrophilic drug, and has superior deformability and higher permeation efficiency than E group. The plasma pharmacokinetics of rabbits showed that TE group and AS-TE group had similar blood concentration and bioavailability; however, micro-dialysis on synovial fluid demonstrated that AS-TE group had higher drug concentration. In RA rat models, the alleviation of the joint swell of AS-TE group was more obvious in the course of 3 weeks of treatment. The inflammatory cytokines and erythrocyte sedimentation rate were significantly lower than those in the negative control group and TE1 group. Conclusion: AS-TE, which can enhance transdermal permeability and drug deposition for the oxidant stress of RA, had further research potential to serve as a TDDS of RA.

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Sinomenine hydrochloride-loaded dissolving microneedles enhanced its absorption in rabbits

Cited by 15 publications

References 59 publications

Polyvinylpyrrolidone microneedles for localized delivery of sinomenine hydrochloride: preparation, release behavior of in vitro & in vivo, and penetration mechanism

Polyvinylpyrrolidone microneedles for localized delivery of sinomenine hydrochloride: preparation, release behavior of in vitro & in vivo, and penetration mechanism

Novel nanosuspension‐based dissolving microneedle arrays for transdermal delivery of a hydrophobic drug

<p>Enhanced transdermal permeability and drug deposition of rheumatoid arthritis via sinomenine hydrochloride-loaded antioxidant surface transethosome</p>

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