Design of self-polymerized insulin loaded poly(n-butylcyanoacrylate) nanoparticles for tunable oral delivery.,Journal of Controlled Release

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Design of self-polymerized insulin loaded poly(n-butylcyanoacrylate) nanoparticles for tunable oral delivery.
Journal of Controlled Release ( IF 10.5 ) Pub Date : 2020-02-22 , DOI: 10.1016/j.jconrel.2020.02.034
Hongbo Cheng ₁ , Xin Zhang ₁ , Lu Qin ₁ , Yingnan Huo ₁ , Zhixiang Cui ₁ , Chang Liu ₁ , Yujiao Sun ₁ , Jian Guan ₁ , Shirui Mao ₁

Affiliation

Macromolecular drugs, characterized by low stability and large molecular weight, still faced various difficulties by oral administration. And controlling drugs' release rate to reach the physiological concentration in the blood was recognized as one of the main challenges in this field but no studies are available so far. Thus, the objective of this study was to investigate the effect of insulin release rate on its in vitro and in vivo behavior when other obstacles (drug stability, mucus penetration and retention in gastrointestinal tract) was firstly overcome. Using n-butylcyanoacrylate (BCA) as the carrier, insulin-loaded Poly (n-butylcyanoacrylate) nanoparticles (Ins/PBCA NPs) were prepared by self-polymerization and the release rate of insulin was controlled by adjusting the mass ratio of Insulin/BCA. The NPs exhibited good stability in gastric fluid with controlled release in intestine and the release rate increased with the increase of Insulin/BCA mass ratio. All the Ins/PBCA NPs with different release rate showed excellent mucus penetration (>60%, 10 min) and strong gastrointestinal retention (~70%, 12 h). Especially, all the NPs showed promising hypoglycemic effect with the extent depending on drug release rate. Ins/BCA = 2/10 NPs exhibited fast hypoglycemic effect, while Ins/BCA = 2/15 NPs showed slow and outstanding performance. In conclusion, Ins/PBCA NPs could not only overcome the oral barriers of insulin delivery but also provide desired hypoglycemic effect by controlling insulin release rate.

中文翻译：

自聚合胰岛素负载型聚（氰基丙烯酸正丁酯）纳米粒子的设计，用于可调口服给药。

具有低稳定性和大分子量的大分子药物，通过口服给药仍然面临各种困难。控制药物的释放速率以达到血液中的生理浓度已被认为是该领域的主要挑战之一，但迄今为止尚无研究。因此，本研究的目的是研究在首次克服其他障碍（药物稳定性，粘液渗透性和在胃肠道中的保留）时胰岛素释放速率对其体外和体内行为的影响。以氰基丙烯酸正丁酯（BCA）为载体，通过自聚合制备了载有胰岛素的聚（氰基丙烯酸正丁酯）纳米颗粒（Ins / PBCA NPs），并通过调节胰岛素/ BCA的质量比来控制胰岛素的释放速率。。NPs在胃液中表现出良好的稳定性，并在肠道内受控释放，且释放速率随胰岛素/ BCA质量比的增加而增加。具有不同释放速率的所有Ins / PBCA NPs均具有出色的粘液渗透性（> 60％，10分钟）和强大的胃肠道保留（〜70％，12 h）。特别是，所有NPs显示出有希望的降血糖作用，其程度取决于药物释放速率。Ins / BCA = 2/10 NPs表现出快速降血糖作用，而Ins / BCA = 2/15 NPs表现出缓慢而出色的表现。总之，Ins / PBCA NPs不仅可以克服口服胰岛素传递的障碍，而且可以通过控制胰岛素释放速率来提供所需的降血糖作用。具有不同释放速率的所有Ins / PBCA NPs均具有出色的粘液渗透性（> 60％，10分钟）和强大的胃肠道保留（〜70％，12 h）。特别是，所有NPs显示出有希望的降血糖作用，其程度取决于药物释放速率。Ins / BCA = 2/10 NPs表现出快速降血糖作用，而Ins / BCA = 2/15 NPs表现出缓慢而出色的表现。总之，Ins / PBCA NPs不仅可以克服口服胰岛素传递的障碍，而且可以通过控制胰岛素释放速率来提供所需的降血糖作用。具有不同释放速率的所有Ins / PBCA NPs均具有出色的粘液渗透性（> 60％，10分钟）和强大的胃肠道保留（〜70％，12 h）。特别是，所有NPs显示出有希望的降血糖作用，其程度取决于药物释放速率。Ins / BCA = 2/10 NPs表现出快速降血糖作用，而Ins / BCA = 2/15 NPs表现出缓慢而出色的表现。总之，Ins / PBCA NPs不仅可以克服口服胰岛素传递的障碍，而且可以通过控制胰岛素释放速率来提供所需的降血糖作用。而Ins / BCA = 2/15 NP表现出缓慢而出色的性能。总之，Ins / PBCA NPs不仅可以克服口服胰岛素传递的障碍，而且可以通过控制胰岛素释放速率来提供所需的降血糖作用。而Ins / BCA = 2/15 NP表现出缓慢而出色的性能。总之，Ins / PBCA NPs不仅可以克服口服胰岛素传递的障碍，而且可以通过控制胰岛素释放速率来提供所需的降血糖作用。

更新日期：2020-02-23

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