Kaity Santanu, Ghosh Animesh
Int J Biol Macromol. 2015 Jan;72:883-93. doi: 10.1016/j.ijbiomac.2014.09.036.
Strategically developed natural polymer-based controlled release multiparticulate drug delivery systems have gained special interest for “spatial placement” and “temporal delivery” of drug molecules. In our earlier study, locust bean gum-poly(vinyl alcohol) interpenetrating polymer network (LBG-PVA IPN), carboxymethylated locust bean gum-poly(vinyl alcohol) interpenetrating polymer network (CMLBG-PVA IPN) and acrylamide grafted locust bean gum-poly(vinyl alcohol) interpenetrating polymer network (Am-g-LBG-PVA IPN) were prepared and characterized. The present study deals with accelerating stability testing, comparative bio-safety and single dose in vivo pharmacokinetic study of all three IPN microspheres for controlled oral delivery of buflomedil hydrochloride (BH). From the stability study, it was observed that the particles were stable throughout the study period. From toxicity and biodegradability study it was proved that the microspheres were safe for internal use and complied with bio-safety criterion. From the in vivo pharmacokinetic study in rabbits, it was observed that the CMLBG-PVA IPN microspheres possessed almost similar Tmax value with BH oral suspension. However, in comparison between the LBG-PVA and Am-g-LBG-PVA IPN microspheres, the later showed well controlled release property than the first in biological condition. Thus, this type of delivery system might be useful to achieve the lofty goals of the controlled release drug delivery.
经过战略开发的基于天然聚合物的控释多颗粒药物递送系统,因药物分子的“空间定位”和“定时递送”而备受关注。在我们早期的研究中,制备并表征了刺槐豆胶 - 聚乙烯醇互穿聚合物网络(LBG - PVA IPN)、羧甲基化刺槐豆胶 - 聚乙烯醇互穿聚合物网络(CMLBG - PVA IPN)和丙烯酰胺接枝刺槐豆胶 - 聚乙烯醇互穿聚合物网络(Am - g - LBG - PVA IPN)。本研究涉及对所有三种IPN微球进行加速稳定性测试、比较生物安全性以及单次给药体内药代动力学研究,以实现盐酸丁咯地尔(BH)的口服控释。从稳定性研究中观察到,在整个研究期间颗粒都是稳定的。从毒性和生物降解性研究证明,微球可安全内服并符合生物安全性标准。从兔体内药代动力学研究中观察到,CMLBG - PVA IPN微球与BH口服混悬液的Tmax值几乎相似。然而,在LBG - PVA和Am - g - LBG - PVA IPN微球之间进行比较时,后者在生物学条件下显示出比前者更好的控释性能。因此,这种类型的递送系统可能有助于实现控释药物递送的崇高目标。