Abstract
The current study inspects the screening of the formulation components further, evaluates the physicochemical properties of the nanostructured lipid carriers (NLCs) for the antihypertensive drug as Candesartan Cilexetil (CC). The sequence screening of all excipients required for the preparation of NLCs should be performed. Firstly, the solubility of CC in different solid and liquid lipids is the major parameter for the selection of the best one. Precirol® ATO 5, Compritol ® 888 ATO and Glyceryl Monostearate (GMS) were showed the maximum solubility of the CC (1000±4.12 mg, 1500±4.15 mg and 1750±3.16 mg), respectively. Hence, they were selected as the solid lipids for the development of NLCs. Liquid lipids Transcutol® HP (30±2.21 mg/ml), Labrasol® ALF (25±1.32 mg/ml) and CapryolTM 90 (18±1.34 mg/ml) were observed to have good affinity for the drug on systematic screening of different liquid lipids. However, Precirol® ATO 5 was found to has good physical compatibility with Transcutol® HP, Compritol ATO 888 was found to has high physical miscibility with Labrasol® ALF and last GMS was appeared in good affinity and compatibly with CapryolTM 90. Hence, the following binary lipid mixtures (Precirol® ATO 5 - Labrasol® ALF), (Compritol® 888 ATO-Transcutol® HP) and (GMS - CapryolTM 90) were selected for the preparation of NLCs. The liquid–solid lipid mixture in the ratio up to 30:70 was observed to have sufficient melting point (55-59 0C). Lutrol F-68, Lutrol F-127, Cremophore EL and Cremophore® RH. In addition to, the combination of (Lutrol® F68:Cremophore® EL) and (Lutrol® F127: Cremophore® RH) were selected as the main surfactants for the preparation of NLCs formulations because of its good emulsification efficacy and homogeneity for the solid-liquid lipid mix. The prepared formulations were investigated for the different quality issues. All designed formulations observed in nanometer size of particles ranged from (408.9±11.5 to 114.6±8.3 nm) with high encapsulation efficiency around 99%. Also, the obtained results revealed that the ZP of the various formulations was consistently negative surface charge in between ((-13 ±2.3 to27.3±3.7 mV). Finally, formula number nine of CC (CC-NLC9) which composed of GMS (solid lipid), CapryolTM 90 (liquid lipid) and Lutrol® F127: Cremophore® RH (surfactants combination) was selected as the best formulation after the rank order for further investigations in the next work. 
 Peer Review History: 
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 Received file 
 
 Average Peer review marks at initial stage: 5.0/10
 Average Peer review marks at publication stage: 7.5/10
 Reviewer(s) detail:
 Name: Dr. Mohammed Abdel-Wahab Sayed Abourehab
 Affiliation: Umm Al-Qura University; Makkah Al-Mukarramah, Saudi Arabia
 E-mail: maabourehab@uqu.edu.sa
 
 Name: Dr. Maha Khalifa Ahmed Khalifa 
 Affiliation: Al-Azhar Universit - Cairo, Egypt
 E-mail: mahakhalifa.ahmed@hotmail.com
 
 Name: Dr. Evren Alğin Yapar
 Affiliation: Turkish Medicines and Medical Devices Agency, Turkiye
 E-mail: evren.yapar@yahoo.com
 Comments of reviewer(s): 
 
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Highlights
Selection of Solid Lipid The efficient solubility of the drug in the solid lipid reflects the capacity of Nanostructured lipid carriers (NLCs) formulations to accommodate high amount of specific drug[17]
Candesartan Cilexetil (CC) solubility in various solid lipids should be performed to select the appropriate ones, which allowed accommodation of high amount of the drug leading to maximizing an essential qualification of a carrier system as the loading capacity and encapsulation efficiency of the prepared NLC formulations
The experiments with solid lipids demonstrated that the affinity of CC to solid lipid was in order of Gelucire® 44/14
Summary
Candesartan Cilexetil (CC) is prodrug of candesartan, angiotensin II type 1 (AT1) receptor antagonist, widely used in the management of hypertension and heart failure[1]. Candesartan Cilexetil own great drawbacks which influence on its oral efficacy and therapeutic application such as very low aqueous solubility and first pass metabolism. To repair previously mentioned drawbacks and to enhance oral bioavailability, lipid–based drug delivery systems like nanostructured lipid carrier (NLCs) second type of lipid nanoparticles system can be employed. Lipid nanoparticles systems (LNs) which have to generation’s first, solid lipid nanoparticles (SLN) and second, nanostructured lipid carrier (NLCs) can improve the lymphatic transport of the lipophilic drugs as CC and increase its oral bioavailability[4]. Nanostructured lipid carriers (NLCs) composed of both solid and liquid lipids in certain proportion. They offer various advantages over solid lipid nanoparticles (SLN) such as higher encapsulation efficiency, smaller size and low polymorphic changes[8]. This study can offer the sequence steps for the development of NLCs and evaluation of their quality characteristics
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