Bhandari Jyoti, Mishra Harshita, Mishra Pawan Kumar, Wimmer Rupert, Ahmad Farhan J, Talegaonkar Sushama
Department of Pharmaceutics, Jamia Hamdard, New Delhi, India.
Department of Wood Science, Mendel University in Brno, Brno, Czech Republic.
Int J Nanomedicine. 2017 Mar 14;12:2021-2031. doi: 10.2147/IJN.S124318. eCollection 2017.
Cellulose nanofiber (CNF) aerogels with favorable floatability and mucoadhesive properties prepared by the freeze-drying method have been introduced as new possible carriers for oral controlled drug delivery system. Bendamustine hydrochloride is considered as the model drug. Drug loading was carried out by the physical adsorption method, and optimization of drug-loaded formulation was done using central composite design. A very lightweight-aerogel-with-matrix system was produced with drug loading of 18.98%±1.57%. The produced aerogel was characterized for morphology, tensile strength, swelling tendency in media with different pH values, floating behavior, mucoadhesive detachment force and drug release profiles under different pH conditions. The results showed that the type of matrix was porous and woven with excellent mechanical properties. The drug release was assessed by dialysis, which was fitted with suitable mathematical models. Approximately 69.205%±2.5% of the drug was released in 24 hours in medium of pH 1.2, whereas ~78%±2.28% of drug was released in medium of pH 7.4, with floating behavior for ~7.5 hours. The results of in vivo study showed a 3.25-fold increase in bioavailability. Thus, we concluded that CNF aerogels offer a great possibility for a gastroretentive drug delivery system with improved bioavailability.
通过冷冻干燥法制备的具有良好漂浮性和粘膜粘附特性的纤维素纳米纤维(CNF)气凝胶已被引入作为口服控释给药系统的新型潜在载体。盐酸苯达莫司汀被视为模型药物。采用物理吸附法进行载药,并使用中心复合设计对载药制剂进行优化。制备出了一种载药量为18.98%±1.57%的超轻质气凝胶-基质系统。对所制备的气凝胶进行了形态学、拉伸强度、在不同pH值介质中的溶胀趋势、漂浮行为、粘膜粘附脱离力以及不同pH条件下的药物释放曲线等表征。结果表明,基质类型为多孔且编织状,具有优异的机械性能。通过透析评估药物释放情况,并拟合了合适的数学模型。在pH 1.2的介质中,约69.205%±2.5%的药物在24小时内释放,而在pH 7.4的介质中,约78%±2.28%的药物释放,且具有约7.5小时的漂浮行为。体内研究结果表明生物利用度提高了3.25倍。因此,我们得出结论,CNF气凝胶为具有提高生物利用度的胃滞留给药系统提供了巨大可能性。