Sustained - release microspheric gel of meloxicam: Preparation, evaluation in vitro and in vivo

IF 3.3 4区医学 Q3 ENGINEERING, BIOMEDICAL

Biomedical Microdevices Pub Date : 2025-05-29 DOI:10.1007/s10544-025-00753-2

Peng Zheng, Yongtao Wei, Keren Cao, Chen Xu, Shanshan Yu, Yang Liu, Min Li, Chunyan Zhang, Tao Wang

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引用次数: 0

Abstract

Osteoarthritis (OA) is the common form of chronic joint disease. The disease progression can affect all joints of the body, seriously affecting patients’ quality of life. The most effective clinical treatment for OA at the moment is the oral or intravenous administration of non-steroidal anti-inflammatory drugs, such as meloxicam (MX). However, certain challenges associated with the conventional use of those drugs include long dosing cycles, poor patient compliance, and systemic toxic side effects, primarily gastrointestinal reactions. Joint synovial fluid mainly consists of sodium hyaluronate (HA). In recent years, HA has been developed and used to treat OA with local injections. However, it also faces the limitations of short injection cycle, frequent administration, and increases the risk of exogenous infection. In this study, a microsphere gel formulation containing PL407, HA and meloxicam microspheres was prepared and the MX-MS-Gel system showed good performance, syringeability and stability. The results of in vitro release studies showed that the MX-MS-Gel released 8.6% in vitro at 72 h and 28.0% at 480 h, with a more moderate drug release. By injecting iodoacetic acid into the knee joint of rats to establish an OA model, MX-MS-Gel significantly improved the inflammatory response of OA, while the safety of MX-MS-Gel was superior and evaluated in this study, which was safe. The results showed that MX-MS-Gel could realize the purpose of delaying the drug release rate and reducing the frequency of administration, thus improving patient compliance and medication safety.

AbstractSection Graphical Abstract

Abstract Image

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美洛昔康缓释微球凝胶的制备及体外、体内评价。

骨关节炎是一种常见的慢性关节疾病。病情进展可影响全身所有关节，严重影响患者的生活质量。目前OA最有效的临床治疗方法是口服或静脉注射非甾体抗炎药，如美洛昔康（MX）。然而，与常规使用这些药物相关的某些挑战包括给药周期长，患者依从性差，以及全身毒副作用，主要是胃肠道反应。关节滑液主要由透明质酸钠（HA）组成。近年来，HA已发展并用于局部注射治疗OA。但也面临注射周期短、给药频繁、外源性感染风险增加等局限性。本研究制备了一种含有PL407、HA和美洛昔康微球的微球凝胶配方，其MX-MS-Gel体系具有良好的性能、注射性和稳定性。体外释放研究结果表明，MX-MS-Gel在体外72 h释放8.6%，480 h释放28.0%，释药较为温和。通过在大鼠膝关节内注射碘乙酸建立OA模型，MX-MS-Gel明显改善OA的炎症反应，同时MX-MS-Gel的安全性优越，本研究对其进行了评价，是安全的。结果表明，MX-MS-Gel能够达到延缓药物释放速度、减少给药频率的目的，从而提高患者的依从性和用药安全性。摘要节图形摘要

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Biomedical Microdevices 工程技术-工程：生物医学

CiteScore

6.90

自引率

3.60%

发文量

审稿时长

6 months

期刊介绍： Biomedical Microdevices: BioMEMS and Biomedical Nanotechnology is an interdisciplinary periodical devoted to all aspects of research in the medical diagnostic and therapeutic applications of Micro-Electro-Mechanical Systems (BioMEMS) and nanotechnology for medicine and biology. General subjects of interest include the design, characterization, testing, modeling and clinical validation of microfabricated systems, and their integration on-chip and in larger functional units. The specific interests of the Journal include systems for neural stimulation and recording, bioseparation technologies such as nanofilters and electrophoretic equipment, miniaturized analytic and DNA identification systems, biosensors, and micro/nanotechnologies for cell and tissue research, tissue engineering, cell transplantation, and the controlled release of drugs and biological molecules. Contributions reporting on fundamental and applied investigations of the material science, biochemistry, and physics of biomedical microdevices and nanotechnology are encouraged. A non-exhaustive list of fields of interest includes: nanoparticle synthesis, characterization, and validation of therapeutic or imaging efficacy in animal models; biocompatibility; biochemical modification of microfabricated devices, with reference to non-specific protein adsorption, and the active immobilization and patterning of proteins on micro/nanofabricated surfaces; the dynamics of fluids in micro-and-nano-fabricated channels; the electromechanical and structural response of micro/nanofabricated systems; the interactions of microdevices with cells and tissues, including biocompatibility and biodegradation studies; variations in the characteristics of the systems as a function of the micro/nanofabrication parameters.