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Preparation and In Vitro/In Vivo Characterization of Mixed-Micelles-Loaded Dissolving Microneedles for Sustained Release of Indomethacin.

Pharmaceutics

November 2024

Department of Pharmaceutics, School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou Higher Education Mega Center, 280 East Waihuan Road, Guangzhou 510006, China.

Indomethacin (IDM) is commonly used to treat chronic inflammatory diseases such as rheumatoid arthritis and osteoarthritis. However, long-term oral IDM treatment can harm the gastrointestinal tract. This study presents a design for encapsulating IDM within mixed micelles (MMs)-loaded dissolving microneedles (DMNs) to improve and sustain transdermal drug delivery.

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Co-delivering dual-drug systems have proven to be effective in, for example, anticancer therapy or HIV prophylaxis due to a higher target selectivity and therapeutic efficacy from compound synergism. However, various challenges regarding physical stability can arise during the formulation definition when multiple drug compounds are included in the same formulation. In this work, the focus was on aqueous suspensions, which could be applied as long-acting injectable formulations to release the drug compounds over weeks to months after administration.

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Nonsteroidal anti-inflammatory drugs (NSAIDs) can induce serious adverse effects in gastrointestinal (GI) mucosa, increasing intestinal permeability and leading to mitochondrial dysfunction, oxidative stress, apoptosis and inflammation. As proton pump inhibitors are effective in protecting against NSAID-induced gastropathy but not NSAID-induced enteropathy, current research is focused on natural products as protective substances for therapy and prevention of intestinal injury. Herein, through the use of an in vitro model based on intestinal epithelial cell (Caco-2) damage caused by indomethacin (INDO), we examined the protective activity of a commercially available standardized extract (OFI+OE) from (L.

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Background: Yoghurt, a fermented dairy product consumed by diverse cultures for centuries, has garnered significant attention from the scientific community due to its potential health benefits and remarkable versatility. This study investigated the anti-inflammatory and anti-oxidative effects of pre-treatment with pasteurized yoghurt in indomethacin induced gastric ulceration.

Method: Thirty male Wistar rats were randomly assigned into five groups.

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Formulation, Characterization, and Cytotoxic Effect of Indomethacin-Loaded Nanoparticles.

Antiinflamm Antiallergy Agents Med Chem

December 2024

Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey.

Background: Indomethacin (IND), classified as class 2 in the Biopharmaceutical Classification System (BCS), has emerged as an anti-inflammatory agent with low solubility and high permeability. Widely used in the treatment of various diseases, such as rheumatoid arthritis and ankylosing spondylitis, this drug is well-known for its adverse effects, particularly in the stomach, and a short biological half-life, which is around 1.5-2 hours.

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