Faculty of Pharmacy, Lachoo Memorial College of Science and Technology, Shastri Nagar, Sector A, Jodhpur, 342001, Rajasthan, India.
Department of Pharmacology, Faculty of Pharmacy, Maulana Azad University, Jodhpur, 342802, Rajasthan, India.
AAPS PharmSciTech. 2024 Jul 24;25(6):172. doi: 10.1208/s12249-024-02878-8.
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.
本研究的目的是制备美洛昔康（MX）包封的混合粒子（HPs），以增强肠道渗透和抗炎活性。MX-HPs 通过纳米沉淀法使用脂质、壳聚糖、泊洛沙姆和 TPGS 制备。对制剂（MX-HPs1、MX-HPs2、MX-HPs3）进行粒径、包封效率和药物释放评估，以选择优化的组成，并进一步进行渗透研究、稳定性研究、形态学研究、相互作用研究和抗炎活性研究，通过角叉菜胶诱导的大鼠足肿胀试验。所制备的 MX-HPs 表现出纳米级颗粒（198.5 ± 3.7 至 223.8 ± 2.1nm）和 PDI（<0.3）、zeta 电位（16.5 ± 2.7 至 29.1 ± 3.6mV）和高包封效率（75.1 ± 4.7 至 88.5 ± 3.9%）。通过透射电子显微镜评估表面形态，显示出无聚集的颗粒。纯 MX 以及制剂的红外（IR）光谱显示没有药物-聚合物相互作用，X 射线衍射证实了结晶 MX 转化为无定形形式。释放研究数据显示 24 小时内 MX 释放时间延长。所选优化的混合粒子（MX-HPs2）显示出比游离 MX 提高 2.3 倍的增强比。储存稳定性和胃肠道稳定性数据表明在 SIF 和 SGF 中均具有稳定的配方。抗炎活性表明，与纯 MX 分散体相比，具有更好的治疗作用。从研究中可以得出结论，制备的 MX-HPs 可能是治疗炎症性疾病的 MX 有前途的递药系统。
