PEGylated Eudragit L100 (ELP)-containing proliponiosomes (PLNs) were developed for improved oral delivery of celecoxib (CXB). The successful introduction of PEG 2000 or 5000 to Eudragit L100 (EL) was confirmed via proton nuclear magnetic resonance analysis of which calculated molar substitution ratio of PEG to EL was 36.0 or 36.7, respectively. CXB, ELP, phospholipid, and non-ionic surfactants were dissolved in dimethyl sulfoxide and lyophilized to produce CXB-loaded PLNs (). The physical state of [email protected] was evaluated using differential scanning calorimetry and powder X-ray diffractometry, which revealed that crystalline CXB was transformed into amorphous form after the fabrication procedure. The reconstitution of [email protected] in aqueous media generated CXB-loaded liponiosomes with nano-sized mean diameters and spherical morphology. [email protected] displayed enhanced dissolution rate and permeability compared to CXB suspension. In vivo pharmacokinetic studies performed on rats demonstrated the improved oral bioavailability of [email protected] compared to that of CXB suspension. No serious systemic toxicity was observed in the blood biochemistry tests performed on rats. These results suggest that the developed PLNs could be promising oral delivery systems for improving the bioavailability of poorly water-soluble drugs, such as CXB.

中文翻译：

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Eudragit L100-PEG脂质体的制备和评价，用于增强塞来昔布的口服给药。

开发了含聚乙二醇化Eudragit L100（ELP）的脂质体（PLN），用于改善塞来昔布（CXB）的口服给药。通过质子核磁共振分析证实了将PEG 2000或5000成功引入Eudragit L100（EL），其质子核算的PEG与EL的摩尔取代比分别为36.0或36.7。将CXB，ELP，磷脂和非离子型表面活性剂溶解在二甲基亚砜中并冻干，以制得负载CXB的PLN（）。使用差示扫描量热法和粉末X射线衍射法评估[电子邮件保护的]物理状态，这表明在制备过程之后结晶的CXB转变为非晶形式。[电子邮件保护]在水性介质中的重建产生了CXB负载的脂质体，具有纳米级的平均直径和球形形态。[受电子邮件保护]与CXB悬浮液相比，显示出更高的溶出度和渗透性。在大鼠上进行的体内药代动力学研究表明，与CXB悬浮液相比，[受电子邮件保护的]口服生物利用度得到改善。在对大鼠进行的血液生化试验中未观察到严重的全身毒性。这些结果表明，已开发的PLN有望成为改善水溶性差的药物（如CXB）生物利用度的有希望的口服给药系统。