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.
摘要：
本研究的目的是制备美洛昔康（MX）包埋的混合颗粒（HP）以增强肠道渗透和抗炎活性。通过纳米沉淀法使用脂质制备MX-HP，壳聚糖,泊洛沙姆,和TPGS。评价制剂(MX-HPs1、MX-HPs2、MX-HPs3)的粒度,截留效率，和药物释放，以选择优化的组合物，并进一步评估渗透研究，稳定性研究，形态学,互动研究，并通过角叉菜胶诱导大鼠爪水肿的抗炎活性试验。制备的MX-HP显示出纳米级颗粒（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），包封效率高（75.1±4.7至88.5±3.9%）。通过透射电子显微镜评估表面形态并显示非聚集颗粒。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射线衍射证实了晶体MX转化为无定形形式。释放研究数据显示，MX释放时间延长了24小时。选定的优化杂化颗粒（MX-HPs2）比游离MX的增强率提高了2.3倍。储存稳定性和胃肠稳定性数据证明了在SIF以及SGF中的稳定制剂。抗炎活性显示出比纯MX分散体更好的治疗作用。从研究中，可以得出结论，制备的MX-HP可能是MX治疗炎症性疾病的有前途的递送系统。
