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Mung bean (Vigna radiata) porous starch for solubility and dissolution enhancement of poorly soluble drug by solid dispersion
International Journal of Biological Macromolecules ( IF 7.7 ) Pub Date : 2020-11-27 , DOI: 10.1016/j.ijbiomac.2020.11.172
Sameer Nadaf , Amrita Jadhav , Suresh Killedar

In this study, a novel Vigna radiata based porous starch (PS) is prepared by solvent exchange technique and explored as a solubilizer for model drug albendazole (ABZ). PS carrier was investigated for different chemical, functional, and micromeritic properties. Solubilizing potential of PS is evaluated by formulating ABZ-PS solid dispersion (1:0.5–1:2) based tablets (SDT). ABZ-PS solid dispersions were evaluated for micromeritic properties, dissolution studies, and anthelmintic activity. Direct compression suitability and susceptibility of mung bean starch were studied by SeDem diagram, Heckel, and Kawakita analysis respectively. PS had an A-type crystallinity pattern and evinced functional properties similar to other legume starches. PS was determined to be suitable for direct compression (good compressibility index = 5.50). SD (1:2) manifested 36.18 fold and 1.6–3.04 fold improvement in the % dissolution and anthelmintic activity of ABZ respectively. All SD batches (R2 = 0.949–0.996) and ABZ (R2 = 0.168) followed the Higuchi-matrix release kinetic model. DSC and P-XRD analysis corroborated the amorphous form of ABZ. SDT showed ≈ a 1.90 fold improvement in dissolution rate than the marketed formulation. Conclusively, Vigna radiata PS could be explored as an alternative to reduce the large burden on the established starches.



中文翻译:

绿豆(Vigna radiata)多孔淀粉通过固体分散促进难溶性药物的溶解度和溶出度。

在这项研究中,一种新颖的Vigna radiata基多孔淀粉(PS)是通过溶剂交换技术制备的,并被用作模型药物阿苯达唑(ABZ)的增溶剂。研究了PS载体的不同化学,功能和微链性能。PS的增溶潜力通过配制基于ABZ-PS固体分散体(1:0.5-1:2)的片剂(SDT)进行评估。评估了ABZ-PS固体分散体的微链性能,溶出度研究和驱虫活性。分别通过SeDem图,Heckel和Kawakita分析研究了绿豆淀粉的直接压缩适应性和敏感性。PS具有A型结晶模式,并具有类似于其他豆类淀粉的功能特性。确定PS适合直接压缩(良好的压缩指数= 5.50)。SD(1:2)表现为36.18倍和1.6–3。ABZ的%溶出度和驱虫活性分别提高04倍。所有SD批次(R2  = 0.949–0.996)和ABZ(R 2  = 0.168)遵循Higuchi-矩阵释放动力学模型。DSC和P-XRD分析证实了ABZ的无定形形式。SDT的溶出度比市售配方提高了约1.90倍。结论是,可以探索Vigna radiata PS作为替代方法,以减轻已建立淀粉的大量负担。

更新日期:2020-12-05
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