格列汀高分子纳米胶束的制备与评价

Q2 Pharmacology, Toxicology and Pharmaceutics Drug Delivery Letters Pub Date : 2019-05-31 DOI:10.2174/2210303109666190212112505
Deep Kumar
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引用次数: 1

摘要

本研究的主要目的是用直接溶出法制备负载格列汀的聚合物纳米胶束。通过对比评价研究聚合物浓度对配方粒径、包封效率、载药量和释药量的影响。采用直接溶出法制备了负载格列汀的高分子纳米胶束。通过改变聚合物的浓度来制备配方,所有配方中药物浓度保持不变。在配方F-1、F-2、F-3中,聚合物(普鲁兰)的浓度分别保持在0.1%、0.5% ~ 1%。考察了聚合物浓度对平均粒径、zeta电位、包封率、载药量和体外释药量的影响。优化后的普兰兰纳米配方浓度为0.1%,平均粒径为368.2nm, zeta电位值为-7.96mV,稳定性较好。因此,F-1被认为是制备格列汀负载聚合物纳米胶束的最佳配方。综上所述,聚合物纳米胶束可以改善格列汀等III类药物的生物利用度和渗透性差的问题,是一种更好的药物控制递送方法。
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Formulation and Evaluation of Polymeric Nanomicelles of Gliptin for Controlled Drug Delivery
The main objective of the study was to develop gliptin loaded polymeric nanomicelles by direct dissolution method. The comparative evaluation studies were performed to study the effect of polymer concentration on particle size, entrapment efficiency, loading capacity and drug release of the formulation. Gliptin loaded polymeric nanomicelles were prepared by the direct dissolution method. The formulations were prepared by varying the concentration of polymer and drug concentration was kept constant in all the formulations. The concentration of polymer (pullulan) was maintained 0.1%, 0.5% 1% in formulation F-1, F-2 and F-3, respectively. The effect of polymer concentration on mean particle size, zeta potential, % entrapment efficiency, % loading capacity and in vitro drug release was studied. The optimized nanoformulation was obtained with pullulan 0.1% concentration with a mean particle diameter of 368.2nm and zeta potential value (-7.96mV) indicating greater stability. Hence F-1 was considered to be the best formulation for the preparation of gliptin loaded polymeric nanomicelles. Hence, it can be concluded that polymeric nanomicellar approach can be beneficial to improve the bioavailability and poor permeability of class III drugs like gliptins and thus can be a better approach for controlled drug delivery.
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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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