Methotrexate delivering microneedle patches for improved therapeutic efficacy in treatment of rheumatoid arthritis

Rajendran, Kayalvizhi; Pahal, Suman; Badnikar, Kedar; Nayak, M. M.; Dinesh, N. S.; Vemula, Praveen Kumar; Krishnan, Uma Maheswari

doi:10.1016/j.ijpharm.2023.123184

Cited by 6 publications

(1 citation statement)

References 31 publications

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“…The needles were reported to successfully penetrate porcine and psoriatic mouse skin, detaching and embedding the drugloaded tips deeply in the skin, thus enabling more prolonged and sustained drug release (over 96 h) compared to subcutaneous injection and dissolving microneedles [19]. Rajendran et al developed a biodegradable microneedle patch to deliver MTX sustainably and locally to arthritic joints of guinea pigs and found that MTX-loaded microneedles induced minimal immune response and provided sustained drug release for the rapid restoration of mobility and a significant decrease in inflammatory and rheumatoid markers at the affected joints compared to hypodermic injection [42]. Zhao and coworkers fabricated dissolving microneedles from hyaluronic acid and polyvinyl pyrrolidone K90 to deliver MTX transdermally.…”

Section: Introductionmentioning

confidence: 99%

Polymeric Microneedles Enhance Transdermal Delivery of Therapeutics

Nguyen,

Kipping,

Banga

2024

Pharmaceutics

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This research presents the efficacy of polymeric microneedles in improving the transdermal permeation of methotrexate across human skin. These microneedles were fabricated from PLGA Expansorb® 50-2A and 50-8A and subjected to comprehensive characterization via scanning electron microscopy, Fourier-transform infrared spectroscopy, and mechanical analysis. We developed and assessed a methotrexate hydrogel for physicochemical and rheological properties. Dye binding, histological examinations, and assessments of skin integrity demonstrated the effective microporation of the skin by PLGA microneedles. We measured the dimensions of microchannels in the skin using scanning electron microscopy, pore uniformity analysis, and confocal microscopy. The skin permeation and disposition of methotrexate were researched in vitro. PLGA 50-8A microneedles appeared significantly longer, sharper, and more mechanically uniform than PLGA 50-2A needles. PLGA 50-8A needles generated substantially more microchannels, as well as deeper, larger, and more uniform channels in the skin than PLGA 50-2A needles. Microneedle insertion substantially reduced skin electrical resistance, accompanied by an elevation in transepidermal water loss values. PLGA 50-8A microneedle treatment provided a significantly higher cumulative delivery, flux, diffusion coefficient, permeability coefficient, and predicted steady-state plasma concentration; however, there was a shorter lag time than for PLGA 50-2A needles, base-treated, and untreated groups (p < 0.05). Conclusively, skin microporation using polymeric microneedles significantly improved the transdermal delivery of methotrexate.

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Section: Introductionmentioning

confidence: 99%

Polymeric Microneedles Enhance Transdermal Delivery of Therapeutics

Nguyen,

Kipping,

Banga

2024

Pharmaceutics

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A Novel Methacryloyl Chitosan Hydrogel Microneedles Patch with Sustainable Drug Release Property for Effective Treatment of Psoriasis

Dai

Sun

et al. 2023

Macromolecular Bioscience

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Psoriasis is a chronic and recurrent skin disease that often requires long‐term treatment, and topical transdermal drug delivery can reduce systemic side effects. However, it is still a challenge in efficient transdermal drug delivery for psoriasis treatment due to low penetration efficiency of most drugs and the abnormal skin conditions of psoriasis patients. Here, a safe and effective methacryloyl chitosan hydrogel microneedles (CSMA hMNs) patch is developed and served as a sustained drug release platform for the treatment of psoriasis. By systematically optimizing the CSMA preparation, CSMA hMNs with excellent morphological characteristics and strong mechanical properties (0.7 N needle−1) are prepared with a concentration of only 3% (w/v) CSMA. As a proof‐of‐concept, methotrexate (MTX) and nicotinamide (NIC) are loaded into CSMA hMNs patch, which can produce a sustained drug release of 80% within 24 h in vitro. In vivo experiments demonstrated that the CSMA hMNs patch can effectively inhibit the skin thickening and spleen enlargement of psoriatic mice and has a good biosafety profile at sufficient therapeutic doses. This study provides a new idea for the preparation of hMN systems using modified CS or other biocompatible materials and offers an effective therapeutic option for psoriasis treatment.This article is protected by copyright. All rights reserved

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Resveratrol nanocrystals based dissolving microneedles with highly efficient for rheumatoid arthritis

Diao,

Liu,

Wang

et al. 2024

Drug Deliv. and Transl. Res.

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Rheumatoid arthritis (RA) is a chronic destructive in ammatory synovitis that is associated with a wide range of clinical consequences, including comorbidities affecting systemic bone, vasculature, metabolic function, and cognition. Although Resveratrol (Res) has been shown to have pharmacological bene ts in the treatment of RA, its limited bioavailability and poor water solubility have prevented clinical usage of this substance. Therefore, changing the crystalline form of Res to boost its solubility and bioavailability can thus signi cantly improve its therapeutic effect for RA. Based on this, in this study, the crystalline form of Res was milled into nanocrystals by media milling and loaded into soluble microneedles (MNs) prepared from high molecular weight hyaluronic acid by vacuum casting for the treatment of RA. This study addressed the shortcomings of poor water solubility and low bioavailability of Res, and meanwhile, the transdermal drug delivery system mediated by soluble MNs improved patient compliance and extended the duration of drug action in vivo, which provided a novel research idea for the treatment of RA.

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Methotrexate delivering microneedle patches for improved therapeutic efficacy in treatment of rheumatoid arthritis

Cited by 6 publications

References 31 publications

Polymeric Microneedles Enhance Transdermal Delivery of Therapeutics

Polymeric Microneedles Enhance Transdermal Delivery of Therapeutics

A Novel Methacryloyl Chitosan Hydrogel Microneedles Patch with Sustainable Drug Release Property for Effective Treatment of Psoriasis

Resveratrol nanocrystals based dissolving microneedles with highly efficient for rheumatoid arthritis

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