Department of Rheumatology of Traditional Chinese and Western Medicine, Xinxiang Central Hospital, Xinxiang 453000, People's Republic of China.
Faculty of Pharmaceutical Sciences, Dow College of Pharmacy, Dow University of Health Sciences, Karachi 74200, Pakistan.
Int J Nanomedicine. 2020 Nov 10;15:8819-8828. doi: 10.2147/IJN.S271938. eCollection 2020.
Piroxicam exhibits low oral bioavailability, due to its meager solubility in water. The intent of this study was to ameliorate the bioavailability of the drug by employing a solubility-enhancing encapsulation technique.
Seven samples were formulated with piroxicam and gelatin using both solvent evaporation and electrospraying together. Evaluation of solubility and release rate in water and assessment of bioavailability in rats were carried out in comparison with piroxicam plain drug powder (PPDP). Other in vitro explorations were accomplished using powder X-ray diffraction analysis, differential scanning calorimetry, thermogravimetric analysis, scanning electron microscopy, and Fourier-transform infrared spectroscopy.
All piroxicam-loaded gelatinnanocontainers (PLGNs) enhanced solubility and release of the payload in water. In particular, a PLGN formulation consisting of piroxicam and gelatin at a 1:8 (w:w) ratio presented about 600-fold the drug solubility of that shown by PPDP. Moreover, 85.12%±10.96% of the payload was released from this formulation in 10 minutes which was significantly higher than that dissolved from PPDP in 10 minutes (11.81%±5.34%). Drug content, drug loading, and encapsulation efficiency of this formulation were 93.41%±0.56%, 10.45%±0.06%, and 66.74%±6.87%, respectively. The drug loaded in PLGNs existed in the amorphous state, as confirmed by X-ray diffraction and differential scanning-calorimetry analyses, and was more stable when analyzed by thermogravimetric analysis. Moreover, Fourier-transform infrared spectroscopy analysis suggested nonexistence of any piroxicam-gelatin interaction in the formulation. In the scanning electron-microscopy image, PLGNs appeared as round, smooth particles, with particle size of <1,000 nm. Amelioration in bioavailability of piroxicam with the aforementioned PLGN formulation was fourfold that of PPDP.
The PLGN formulation fabricated with piroxicam and gelatin at 1:8 (w:w) might be a promising system for enhanced biopharmaceutical performance of the drug.
吡罗昔康在水中的溶解度很低，因此口服生物利用度也较低。本研究旨在通过使用增溶包封技术来改善药物的生物利用度。
采用溶剂蒸发法和电喷雾法，将吡罗昔康与明胶共制成 7 种样品。与普通吡罗昔康药物粉末（PPDP）相比，对其在水中的溶解度和释放速率进行评估，并进行大鼠体内生物利用度评价。采用粉末 X 射线衍射分析、差示扫描量热法、热重分析、扫描电子显微镜和傅里叶变换红外光谱对其他体外探索进行研究。
所有载吡罗昔康明胶纳米容器（PLGN）均能提高药物在水中的溶解度和释放度。特别是，由吡罗昔康和明胶以 1:8（w:w）比例组成的 PLGN 制剂，其药物溶解度约为 PPDP 的 600 倍。此外，该制剂在 10 分钟内释放了 85.12%±10.96%的载药量，明显高于 PPDP 在 10 分钟内溶解的 11.81%±5.34%。该制剂的药物含量、药物载量和包封效率分别为 93.41%±0.56%、10.45%±0.06%和 66.74%±6.87%。X 射线衍射和差示扫描量热分析证实，载药 PLGN 中的药物呈无定形态，热重分析表明其更为稳定。此外，傅里叶变换红外光谱分析表明，该制剂中不存在吡罗昔康-明胶相互作用。在扫描电子显微镜图像中，PLGN 呈圆形、光滑的颗粒状，粒径<1000nm。上述 PLGN 制剂可使吡罗昔康的生物利用度提高 4 倍。
由吡罗昔康和明胶以 1:8（w:w）制成的 PLGN 制剂可能是一种有前途的系统，可提高药物的生物药剂学性能。
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