Department of Pharmaceutics, College of Pharmacy, AL-Qassim University, Qassim, KSA.
Department of Quality Control & Quality Assurance, Holding Company for Biological Products and Vaccines, Cairo, Egypt.
Drug Deliv. 2022 Dec;29(1):1836-1847. doi: 10.1080/10717544.2022.2083723.
Development of new approaches for oral delivery of an existing antiviral drug aimed to enhance its permeability and hence bioavailability. Ganciclovir (GC) is an antiviral drug that belongs to class III in biopharmaceutical classification. The encapsulation of poorly absorbed drugs within nanosized particles offers several characteristics to drug due to their acquired surface properties. In the following study, the solvent evaporation technique was used to incorporate GC, within elegant nanosize particles using cyclodextrin and shellac polymers for enhancing its permeability and release pattern. Formulation variables were optimized using 2 full factorial design. The prepared formulations were assessed for yield, particle size, content, and micromeritics behavior. The optimized formula (F6) was identified through differential scanning calorimetry and Fourier transform infrared. release and stability were also assessed. Pharmacokinetic parameters of optimized nano GC solid dispersion particles (NGCSD-F6) were finally evaluated. The optimized formula (F6) showed a mean particle size of 288.5±20.7nm, a zeta potential of about 23.87±2.27, and drug content 95.77±2.1%. The drug release pattern of F6 showed an initial burst release followed by a sustained release over the next 12h. The optimized formula showed accepted stability upon storage at room and refrigerator temperatures for 6months with good flowing properties (Carr's index=18.28±0.44). pharmacokinetic study in rabbits revealed 2.2 fold increases in the bioavailability of GC compared with commercial convention tablets. The study affords evidence for the success of the solid dispersion technique under specified conditions in improvement of bioavailability of GC.
开发新方法用于口服现有抗病毒药物,旨在提高其通透性和生物利用度。更昔洛韦(GC)是一种属于生物药剂学分类法 III 类的抗病毒药物。将吸收不良的药物包封在纳米级颗粒内,由于其获得的表面特性,可为药物提供多种特性。在接下来的研究中,使用溶剂蒸发技术将 GC 包封在使用环糊精和紫胶聚合物的优雅纳米级颗粒内,以增强其通透性和释放模式。使用 2 因子完全设计优化制剂变量。评估了制剂的收率、粒径、含量和微粉学特性。通过差示扫描量热法和傅里叶变换红外法鉴定了优化的配方(F6)。还评估了释放和稳定性。最后评估了优化的纳米 GC 固体分散颗粒(NGCSD-F6)的药代动力学参数。优化的配方(F6)的平均粒径为 288.5±20.7nm,zeta 电位约为 23.87±2.27,药物含量为 95.77±2.1%。F6 的药物释放模式显示初始突释,随后在接下来的 12 小时内持续释放。优化的配方在室温下和冰箱中储存 6 个月后表现出良好的稳定性,具有良好的流动性(Carr 指数=18.28±0.44)。在兔子中的药代动力学研究表明,与商业常规片剂相比,GC 的生物利用度增加了 2.2 倍。该研究证明了在特定条件下固体分散技术在提高 GC 生物利用度方面的成功。