Formulation and Evaluation of Meloxicam Hybrid nano Particles

IF 3.4 4区医学 Q2 PHARMACOLOGY & PHARMACY

AAPS PharmSciTech Pub Date : 2024-07-24 DOI:10.1208/s12249-024-02878-8

Mohammed Asif, Kaneez Fatima, Syed Sarim Imam, Sultan Alshehri, Wael A. Mahdi

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Abstract

The goal of the present study was to prepare meloxicam (MX) entrapped hybrid particles (HPs) to enhance intestinal permeation and anti-inflammatory activity. MX-HPs were prepared by nanoprecipitation method using lipid, chitosan, poloxamer, and TPGS. The formulations (MX-HPs1, MX-HPs2, MX-HPs3) were evaluated for particle size, entrapment efficiency, and drug release to select the optimized composition and further evaluated for permeation study, stability study, morphology, interaction study, and anti-inflammatory activity by carrageenan-induced rat paw edema test. The prepared MX-HPs showed nano sized particles (198.5 ± 3.7 to 223.8 ± 2.1 nm) and PDI (<0.3), zeta potential (16.5 ± 2.7 to 29.1 ± 3.6 mV), and high entrapment efficiency (75.1 ± 4.7 to 88.5 ± 3.9%). The surface morphology was assessed by transmission electron microscopy and showed non-aggregated particles. Infra-red (IR) spectroscopy of pure MX as well as formulation revealed no drug-polymer interaction and X-ray diffraction confirmed the conversion of crystalline MX into amorphous form. The release study data revealed prolonged MX release for 24 h. The selected optimized hybrid particles (MX-HPs2) revealed a 2.3-fold improved enhancement ratio than free MX. The storage stability and gastrointestinal stability data demonstrated a stable formulation in SIF as well as SGF. The anti-inflammatory activity showed better therapeutic action than pure MX dispersion. From the study, it can be concluded that the prepared MX-HPs may be a promising delivery system for MX in treating inflammatory disorders.

Graphical Abstract

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美洛昔康混合纳米粒子的制备与评估

本研究的目的是制备美洛昔康（MX）夹带混合颗粒（HPs），以增强其肠道渗透性和抗炎活性。本研究使用脂质、壳聚糖、聚氧乙烯醚和 TPGS 通过纳米沉淀法制备了 MX-HPs。对制备的制剂（MX-HPs1、MX-HPs2、MX-HPs3）进行了粒度、包埋效率和药物释放评估，以选出最优化的成分，并通过卡拉胶诱导的大鼠爪水肿试验进一步评估了渗透研究、稳定性研究、形态学研究、相互作用研究和抗炎活性。制备的 MX-HPs 显示出纳米尺寸的颗粒（198.5 ± 3.7 至 223.8 ± 2.1 nm）和 PDI (

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来源期刊

AAPS PharmSciTech 医学-药学

CiteScore

6.80

自引率

3.00%

发文量

264

审稿时长

2.4 months

期刊介绍： AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.