Madan Jyotsana R, Ansari Izharahemad N, Dua Kamal, Awasthi Rajendra
Department of Pharmaceutics, Smt. Kashibai Navale College of Pharmacy, Savitribai Phule Pune University, Pune 411048, Maharashtra, India.
Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Ultimo NSW 2007, Australia.
Adv Pharm Bull. 2020 Jul;10(3):408-417. doi: 10.34172/apb.2020.049. Epub 2020 May 11.
The objective of this work was to formulate casein (CAS) nanocarriers for the dissolution enhancement of poorly water soluble drug celecoxib (CLXB). The CLXB loaded CAS nanocarriers ., nanoparticles, reassembled CAS micelles and nanocapsules were prepared using sodium caseinate (SOD-CAS) as a carrier to enhance the solubility of CLXB. The prepared formulations were characterized for particle size, polydispersity index, zeta potential, percentage entrapment efficiency, and surface morphology for the selection of best formulation. Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray powder diffraction study was used to for the confirmation of encapsulation of CLXB. Further, drug dissolution, permeation studies on chicken ileum and stability studies were carried out. The CLXB loaded casein nanoparticles (CNP) (batch A2) showed a particle size diameter 216.1 nm, polydispersity index 0.422 with percentage entrapment efficiency of 90.71% and zeta potential of -24.6 mV. Scanning electron microscopy of suspension confirmed globular shape of CNP. The release data of optimized batch followed non Fickian diffusion mechanism. The permeation studies on chicken ileum of CLXB loaded CNP showed permeation through mucous membrane as compared to pure CLXB. The apparent permeability of best selected freeze dried CLXB loaded CNP (batch A2) was higher and gradually increased from 0.90 mg/cm after 10 min to a maximum of 1.95 mg/cm over the subsequent 90 min. A higher permeation was recorded at each time point than that of the pure CLXB. The study explored the potential of CAS as a carrier for solubility enhancement of poorly water soluble drugs.
这项工作的目的是制备酪蛋白（CAS）纳米载体，以提高难溶性药物塞来昔布（CLXB）的溶解度。以酪蛋白酸钠（SOD-CAS）为载体，制备了负载CLXB的CAS纳米载体，即纳米颗粒、重组CAS胶束和纳米胶囊，以提高CLXB的溶解度。对制备的制剂进行粒度、多分散指数、zeta电位、包封率百分比和表面形态表征，以选择最佳制剂。采用傅里叶变换红外光谱、差示扫描量热法和X射线粉末衍射研究来确认CLXB的包封情况。此外，还进行了药物溶解、鸡回肠渗透研究和稳定性研究。负载CLXB的酪蛋白纳米颗粒（CNP）（批次A2）的粒径为216.1 nm，多分散指数为0.422，包封率为90.71%，zeta电位为-24.6 mV。悬浮液的扫描电子显微镜证实了CNP为球形。优化批次的释放数据遵循非Fickian扩散机制。负载CLXB的CNP在鸡回肠的渗透研究表明，与纯CLXB相比，其能够透过黏膜。最佳选择的冻干负载CLXB的CNP（批次A2）的表观渗透率较高，在10分钟后从0.90 mg/cm逐渐增加，在随后的90分钟内最高达到1.95 mg/cm。在每个时间点记录的渗透率均高于纯CLXB。该研究探索了CAS作为难溶性药物溶解度增强载体的潜力。
