木麻黄提取物载磷脂体:Wistar大鼠抗糖尿病和降血脂活性的优化、表征和体内评价

Q2 Pharmacology, Toxicology and Pharmaceutics Drug Delivery Letters Pub Date : 2019-05-31 DOI:10.2174/2210303109666190118162157
A. Rani, Sunil Kumar, R. Khar
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引用次数: 3

摘要

草药提取物具有良好的体外活性,但由于其大分子大小和较差的脂溶性,其体内活性较低,吸收差,生物利用度低。这些问题可以通过设计新的给药系统来纠正。与传统的草药提取物相比,磷脂体提供更好的吸收和生物利用度。本文对植物提取物中磷脂复合物的制备、优化、表征及体内抗糖尿病、降血脂活性进行了研究,以提高具有足够稳定性的治疗效果。初步采用了不同的制备工艺,并选择了抗溶剂沉淀法。以全因子设计为指导,研究了自变量对各种因变量的影响,得到了最优制剂。为每个响应因子生成响应轮廓图,以预测产生具有最小粒径和最大捕获效率的光复体配方的光复体组成。平均粒径为295±0.53nm,捕获效率为82.43±1.65%,Span值为0.34±0.14。Zeta电位为19.35mv,表明形成了稳定的配方。体外释放研究表明,该药物的释放符合Korsmeyer- Peppas动力学模型。结果表明,与木麻黄粗提物相比,木麻黄粗提物具有更强的抗糖尿病和降血脂活性。成功配制了木麻黄提取物的光敏体,其包封效率和理化性质均较好,确定了稳定的配方。体内抗糖尿病活性证实了优化制剂的更好潜力。因此,木麻黄提取物的磷脂体可能是一种有用的新型药物传递系统,具有比传统植物提取物更好的治疗效果。
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Casuarina equisetifoliaExtract Loaded Phytosomes: Optimization, Characterization andIn vivoEvaluation of Antidiabetic and Antihyperlipidemic Activities in Wistar Rats
Herbal extracts have brilliant in-vitro activity but less in-vivo action in light of their macromolecular size and poor lipid solubility bringing about poor absorption and low bioavailability. These issues can be corrected by designing novel drug delivery systems. Phytosomes provide better absorption and bioavailability when compared to conventional herbal extract.This paper deals with the preparation, optimization and characterization of Phytosome of plant extract and in vivo assessment of antidiabetic and antihyperlipidemic activity for improved therapeutic efficacy having sufficient stability.Preliminary distinctive strategies were utilized to get ready Phytosome and antisolvent precipitation method was chosen. The formulation was guided by a full factorial design to study the effect of Independent variable on various dependent variables and resulted in an optimised product. Response contour plots were generated for each response factor to predict a phytosomal composition that yields phytosome formulation having least particle size and maximum entrapment efficiency.Mean particle size, entrapment efficiency and Span value were found to be 295 ± 0.53nm, 82.43 ± 1.65% and 0.34 ± 0.14 respectively. Zeta potential was found to be 19.35mv, indicating the formation of stable formulation. In vitro release study described that the drug release follows the Korsmeyer- Peppas kinetic model. The results proved that Phytosomes of Casuarina equisetifolia extract exhibited more antidiabetic potential and antihyperlipidemic properties as compared to crude Casuarina extract.Phytosomes of Casuarina equestifolia extract was successfully formulated having good entrapment efficiency and physico-chemical characterization of the optimized product, confirming the formation of stable formulation. In vivo antidiabetic activity confirmed better potential of the optimised formulation. Consequently, it has been presumed that Phytosomes of Casuarina equisetifolia extract serve as a useful novel drug delivery system and provide more therapeutic efficacy than conventional plant extracts.
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来源期刊
Drug Delivery Letters
Drug Delivery Letters Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
CiteScore
1.70
自引率
0.00%
发文量
30
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