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

Abstract

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.

Wu-Teng-Gao External Treatment Improves Th17/Treg Balance in Rheumatoid Arthritis

“…For example, Qing-Feng-Teng (Sinomenium Acutum), Lei-Gong-Teng (Tripterygium Wilfordii), and Hei-Gu-Teng (Periploca Forrestii Schltr.) are effective in anti-inflammation and RA treatment [18,35,36]. Despite several clinical studies that have been conducted, the molecular mechanism by which WTG alleviates RA progression remains poorly understood.…”

Transdermal delivery of inflammatory factors regulated drugs for rheumatoid arthritis

“…The GH patch can continuously penetrate for 48 h, which solved the problem of frequent medication caused by oral GH (twice daily), and significantly reduce the side effects of diarrhea and weight loss caused by oral GH. In summary, the GH patch is a safe and efficient transdermal dosage form for the treatment of RA (Kandil et al., 2020 ). Vaidya prepared MTX patch by solvent casting method.…”

Recent advances on transdermal delivery systems for the treatment of arthritic injuries: From classical treatment to nanomedicines

“…Sinomenine hydrochloride‐loaded dissolving MNp (SH‐MN) were fabricated using PVP and chondroitin sulfate via a casting method. In percutaneous permeation studies in vitro, the cumulative permeation and permeation rate of SH‐MN were 5.31 and 5.06 times higher than that of Sinomenine hydrochloride (SH)‐gel (SH‐G; Shu et al, 2020). Amodwala et al (2017) fabricated PVA and PVP‐based MNp to enhance the delivery of Meloxicam for arthritis treatment.…”