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Coadministration of Polypeptide-k and Curcumin Through Solid Self-Nanoemulsifying Drug Delivery System for Better Therapeutic Effect Against Diabetes Mellitus: Formulation, Optimization, Biopharmaceutical Characterization, and Pharmacodynamic Assessment.
ASSAY and Drug Development Technologies ( IF 1.6 ) Pub Date : 2019-05-17 , DOI: 10.1089/adt.2018.902
Varun Garg 1 , Puneet Kaur 2 , Monica Gulati 1 , Sachin Kumar Singh 1 , Bimlesh Kumar 1 , Narendra Kumar Pandey 1 , Ankit Kumar Yadav 1 , Rajesh Kumar 1 , Gowthamarajan Kuppusamy 3 , Anindita De 3 , Nethravathi Puttappa 3 , Sheetu Wadhwa 1
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An attempt has been made to prepare solid self-nanoemulsifying drug delivery system (SNEDDS) of polypeptide-k (PPK) and curcumin (CRM) using Labrafil M1944 CS as oil, Tween-80 as surfactant, Transcutol P as cosurfactant and Aerosil-200 (A-200) as porous hydrophobic carrier for improving their antidiabetic potential through oral delivery. Box-Behnken Design was used to optimize the liquid formulation based on the results of the mean droplet size, polydispersity index, percentage drug loading, and zeta potential. The formulation was adsorbed on Aerosil-200 through spray drying. The formulation showed desirable micromeritic, disintegration, and dissolution properties. About fivefold rise in the dissolution and permeation rate for drugs was observed from formulations vis a vis their unprocessed forms. The formulation was found to be stable with variation in pH, dilution, and temperature. The individual solid SNEDDS formulation of PPK and CRM and their combination were evaluated for antidiabetic potential and the results were compared with their naive forms on streptozotocin-induced diabetic rats. The results revealed better control of serum glucose level and other biochemical tests, such as liver parameters, lipid profiles, and antioxidant levels, as well as histological evaluation of pancreatic tissues in all the solid SNEDDS formulation as compared with their naive forms.

中文翻译:

多肽-k和姜黄素通过固体自纳米乳化药物递送系统共同给药,对糖尿病具有更好的治疗作用:配方,优化,生物药物表征和药效学评估。

尝试使用Labrafil M1944 CS作为油,Tween-80作为表面活性剂,Transcutol P作为辅助表面活性剂和Aerosil-200,制备多肽-k(PPK)和姜黄素(CRM)的固体自纳米乳化药物递送系统(SNEDDS) (A-200)作为多孔疏水载体,可通过口服给药改善其抗糖尿病的潜力。基于平均液滴尺寸,多分散指数,载药量百分比和zeta电位的结果,使用Box-Behnken设计来优化液体制剂。通过喷雾干燥将该制剂吸附在Aerosil-200上。该制剂显示出所需的微团,崩解和溶解性质。从制剂相对于其未加工形式观察到药物的溶解和渗透速率提高约五倍。发现该制剂在pH,稀释度和温度的变化下是稳定的。评估了PPK和CRM各自的固体SNEDDS配方及其组合的抗糖尿病潜力,并将其结果与链脲佐菌素诱导的糖尿病大鼠的幼稚形式进行了比较。结果显示,与所有天然SNEDDS制剂相比,所有固体SNEDDS制剂均能更好地控制血清葡萄糖水平和其他生化测试,例如肝脏参数,脂质谱和抗氧化剂水平,以及胰腺组织的组织学评估。
更新日期:2019-11-01
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