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Oral nanoemulsions of candesartan cilexetil: formulation, characterization and in vitro drug release studies
AAPS Open Pub Date : 2017-06-02 , DOI: 10.1186/s41120-017-0016-7
Halah Hussein Ali , Ahmed Abbas Hussein

Nanoemulsion is considered to be a new and exciting field of research that seeks to exploit the attractive properties of components to improve oral delivery of drugs like candesartan cilexetil used in the management of chronic diseases. Candesartan cilexetil is a lipophilic acidic drug with a half-life of about (5–10) hour and absolute bioavailability of (14–40%). For this reason, the study target was to formulate and characterize candesartan cilexetil nanoemulsions that could improve solubility, dissolution and stability of the lipophilic drug candesartan cilexetil. The solubility of candesartan cilexetil was checked in various vehicles in order to choose the best solubilizing components for building up an efficient nanoemulsion based on regulating hydrophilic/lipophilic balance (HLB) value above 10, and then pseudo-ternary phase diagram was used as a useful tool to evaluate the nanoemulsion domain. The nanoemulsion formulations were prepared using various concentrations of cinnamon oil, tween 80 with poloxamer mixture and transcutol HP as oil, surfactant mixture and co-surfactant respectively by aqueous titration method at surfactant/co-surfactant ratios of 3:1 and 4:1 and varying the type of poloxamer in each ratio. The prepared nanoemulsions were tested for nanodispersion stability studies, droplet size distribution, polydispersity index, zeta potential, viscosity, filter paper spreadability, dye miscibility, electroconductivity, pH, percent transmittance, surface tension, refractive index, morphology and drug dissolution. It was found that release rate and extent for all prepared nanoformulations were significantly higher (p < 0.05) than marketed tablet formulation as well as plain drug powder. The results demonstrated that, the potential use of this system is a perfect technique for improving solubility and dissolution of candesartan cilexetil.

中文翻译:

坎地沙坦cilexetil口服纳米乳剂:制剂,表征和体外药物释放研究

纳米乳剂被认为是新的令人兴奋的研究领域,其试图利用组分的吸引人的性质来改善用于治疗慢性病的药物如坎地沙坦西酯的口服递送。Candesartan cilexetil是一种亲脂性酸性药物,半衰期约为(5-10)小时,绝对生物利用度为(14-40%)。因此,本研究的目的是配制和表征坎地沙坦西奈克司特纳米乳剂,该乳液可以改善亲脂性药物坎地沙坦西奈克司特的溶解性,溶解性和稳定性。检查坎地沙坦酯在各种媒介物中的溶解度,以便基于将亲水性/亲脂性平衡(HLB)值控制在10以上,从而选择最佳的增溶组分来构建有效的纳米乳液,然后使用伪三元相图作为评估纳米乳液域的有用工具。通过水滴定法,以3:1和4:1的表面活性剂/助表面活性剂的比例通过水滴定法分别使用不同浓度的肉桂油,吐温80与泊洛沙姆混合物和transcutol HP作为油,表面活性剂混合物和助表面活性剂来制备纳米乳剂。在每个比例中改变泊洛沙姆的类型。测试了制备的纳米乳剂的纳米分散稳定性,液滴尺寸分布,多分散指数,ζ电势,粘度,滤纸铺展性,染料混溶性,电导率,pH,透射率百分比,表面张力,折射率,形态和药物溶解性。发现所有制备的纳米制剂的释放速率和程度均显着更高(p <0。05)比市售的片剂以及普通药物粉末更便宜。结果表明,该系统的潜在用途是改善坎地沙坦酯的溶解度和溶解度的理想技术。
更新日期:2017-06-02
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