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Formulation, In Vitro Evaluation, and Toxicity Studies of A. vulgaris-co-AAm Carrier for Vildagliptin
Advances in Polymer Technology ( IF 2.0 ) Pub Date : 2021-07-23 , DOI: 10.1155/2021/6634780
Samia Kausar 1 , Alia Erum 1 , Ume Ruqia Tulain 1 , Muhammad Ajaz Hussain 2 , Muhammad Farid-ul-Haq 2 , Nadia Shamshad Malik 3 , Ayesha Rashid 4
Affiliation  

This study investigated the use of Artemisia vulgaris L. seed mucilage as a new excipient for sustained delivery of Vildagliptin. Copolymeric carrier of A. vulgaris seed mucilage-co-AAm was devised by using acrylamide (AAm) as a monomer, methylene-bis-acrylamide (MBA) as a crosslinker, and potassium persulfate (KPS) as an initiator through free radical polymerization. Different formulations of A. vulgaris-co-AAm were devised by varying contents of polymer, monomer, crosslinking agent, initiator, and reaction temperature. Copolymeric structures were characterized through XRD analysis, Fourier transform infrared (FTIR) spectroscopy, TGA and DSC analysis, and scanning electron microscopy. Porosity, gel fraction, and Vildagliptin loading capacity of copolymers were also established. Swelling and in vitro drug release studies were conducted. XRD evaluation showed the alteration of the crystalline structure of Vildagliptin into an amorphous form. FTIR analysis confirmed the successful grafting of AAm to A. vulgaris seed mucilage backbone. Porosity was increased with increasing polymer concentration and reaction temperature while it was decreased with an increasing amount of AAm, MBA, and KPS. Gel content was decreased with increasing polymer concentration and reaction temperature while it was increased with an increasing amount of AAm, MBA, and KPS. Acute oral toxicity of copolymeric network was done in animal models to evaluate the safety. Copolymers showed the same swelling behavior at all pH 1.2, 4.5, 6.8, and 7.4. Vildagliptin release from copolymer showed a cumulative trend by increasing polymer content and reaction temperature, while a declining trend was observed with increasing contents of monomer, crosslinking agent, and initiator. Sustained release of Vildagliptin was observed from copolymers and release followed the Korsmeyer-Peppas model. From the acute oral toxicity studies, it is evident that newly synthesized copolymeric carriers are potentially safe for eyes, skin, and vital organs.

中文翻译:

维格列汀的 A. vulgaris-co-AAm 载体的制剂、体外评价和毒性研究

本研究调查了使用青蒿种子粘液作为持续递送维格列汀的新赋形剂的用途。的共聚载体A.寻常子粘液-共- AAM通过使用丙烯酰胺(AAM)作为单体,亚甲基-双-丙烯酰胺(MBA)作为交联剂设计,和过硫酸钾(KPS)通过自由基聚合引发剂。不同配方的A. vulgaris-co-AAm 是通过改变聚合物、单体、交联剂、引发剂和反应温度的含量而设计的。通过 XRD 分析、傅里叶变换红外 (FTIR) 光谱、TGA 和 DSC 分析以及扫描电子显微镜对共聚物结构进行了表征。还确定了共聚物的孔隙率、凝胶分数和维格列汀负载能力。进行了溶胀和体外药物释放研究。XRD 评估显示维格列汀的晶体结构改变为无定形形式。FTIR 分析证实 AAm 成功嫁接至A. vulgaris种子粘液骨架。孔隙率随着聚合物浓度和反应温度的增加而增加,而随着 AAm、MBA 和 KPS 量的增加而降低。凝胶含量随着聚合物浓度和反应温度的增加而降低,而随着 AAm、MBA 和 KPS 量的增加而增加。共聚网络的急性口服毒性在动物模型中进行以评估安全性。共聚物在所有 pH 值 1.2、4.5、6.8 和 7.4 下都表现出相同的溶胀行为。随着聚合物含量和反应温度的增加,维格列汀从共聚物中的释放呈累积趋势,而随着单体、交联剂和引发剂含量的增加,维格列汀的释放呈下降趋势。从共聚物中观察到维格列汀的持续释放,释放遵循 Korsmeyer-Peppas 模型。
更新日期:2021-07-23
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