Candesartan cilexetil is an ester prodrug antagonist to angiotensin II receptor type 1 (AT1) used in management of many cardiovascular diseases. The absolute bioavailability of candesartan cilexetil is about (14–40%). Therefore, the paper aim was to prepare and evaluate solid self-nanoemulsifying drug delivery systems for candesartan cilexetil in order to improve its solubility, dissolution and stability. Solubility study was run in different vehicles to select the best excipients for dissolving candesartan cilexetil. Pseudo-ternary phase diagrams were constructed at 1:1, 2:1, 3:1 and 4:1 ratios and four formulations were prepared using various concentrations of cinnamon oil, tween 80 with poloxamer 407 mixture and transcutol HP as oil, surfactant mixture and co-surfactant, respectively. After this step about (0.2 milliliter) of each formulation was adsorbed on to two different adsorbent mixtures set which were: avicel 101 with aerosil 200 and avicel 101 with dibasic calcium phosphate anhydrous resulted in eight solid nanoformulations. All prepared formulations were evaluated for particle size distribution, polydispersity index, zeta potential, scanning probe microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray powder diffractometry and in vitro drug dissolution. It was found that release rate and extent for all prepared formulations were significantly higher (p < 0.05) than marketed tablet as well as plain drug powder. It could be concluded from the study that self-nanoemulsifying drug delivery system is a promising approach to improve solubility, wettability, dissolution and stability of candesartan cilexetil.

中文翻译：

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坎地沙坦citexetil口服固体自纳米乳化药物递送系统：制剂，表征和体外药物释放研究

Candesartan cilexetil是一种用于治疗许多心血管疾病的1型血管紧张素II受体（AT1）的酯类前药拮抗剂。坎地沙坦酯的绝对生物利用度约为（14–40％）。因此，本文的目的是制备和评价坎地沙坦西酯的固体自纳米乳化药物递送系统，以提高其溶解度，溶解性和稳定性。在不同的载体中进行了溶解度研究，以选择最佳的赋形剂来溶解坎地沙坦酯。伪三元相图以1：1、2：1、3：1和4：1的比例构建，并使用不同浓度的肉桂油，吐温80与泊洛沙姆407混合物和反式角豆酚HP作为油，表面活性剂混合物制备了四种配方和辅助表面活性剂。在大约（0。将每种配方2毫升吸附到两种不同的吸附剂混合物上，这两种混合物是：带aerosil 200的avicel 101和带无水磷酸氢钙的avicel 101，产生了8个固体纳米制剂。评价所有制备的制剂的粒度分布，多分散指数，ζ电势，扫描探针显微镜，傅里叶变换红外光谱，差示扫描量热法，X射线粉末衍射法和体外药物溶解。发现所有制备的制剂的释放速率和程度均显着高于市售片剂和普通药物粉末（p <0.05）。从研究中可以得出结论，自纳米乳化的药物递送系统是提高坎地沙坦酯的溶解度，润湿性，溶解性和稳定性的一种有前途的方法。