Preparation and Characterization of Self Nano-Emulsifying Drug Delivery System Loaded with Citraland Its Antiproliferative Effect on Colorectal Cells In Vitro

Abstract

Citral is an active compound naturally found in lemongrass, lemon, and lime. Although this pale-yellow liquid confers low water solubility, the compound has been reported to possess good therapeutic features including antiproliferative and anticancer modalities. The self nano-emulsifying drug delivery system (SNEDDS) is a type of liquid-lipid nanocarrier that is suitable for the loading of insolubilized oil-based compound such as Citral. This study reports the design and optimization of a SNEDDS formulation, synthesis and characterization as well as loading with Citral (CIT-SNEDDS). Further assessment of theantiproliferative effects of CIT-SNEDDS towards colorectal cancer cells was also conducted. SNEDDS composed of coconut oil, dimethyl sulfoxide (DMSO) and Tween 80. CIT-SNEDDS was prepared via gentle agitation of SNEDDS with 0.5% Citral for 72 h at room temperature. Physicochemical characterization was performed using several physicochemical analyses. The average particle size of CIT-SNEDDS was16.86 ± 0.15 nm, zeta potential of 0.58 ± 0.19 mV, and polydispersity index (PDI) of 0.23 ± 0.01. In vitro drug release of Citral from CIT-SNEDDS was 79.25% of release, and for Citral the release percentage was 93.56% over 72 h. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was done to determine the cytotoxicity effect of CIT-SNEDDS in human colorectal cancer cell lines HT29 and SW620. The half maximal inhibitory concentrations (IC50) for 72 hof CIT-SNEDDS and Citral on SW620 were 16.50 ± 0.87 µg/mL and 22.50 ± 2.50 µg/mL, respectively. The IC50 values of CIT-SNEDDS and Citral after 72 h of treatment on HT29 were 34.10 ± 0.30 µg/mL and 21.77 ± 0.23 µg/mL, respectively. This study strongly suggests that CIT-SNEDDS has permitted the sustained release of Citral and that CIT-SNEDDS constitutes a potential soluble drug nanocarrier that is effective against colorectal cancer cells.

Preparation a core‐shell lipid/polymer nanoparticle containing Isotretinoin drug with pH sensitive property: A response surface methodology study

“…In fact, the negatively charged groups of hydroxyl and ester in the GMS molecules are the reasons for negative zeta potential of lipid coated CNPs 18 . The zeta potential value of more than ±30 mV confirms the sufficient stability of NPs 56,57 …”

Characterization and Cellular Internalization of Spherical Cellulose Nanocrystals (CNC) into Normal and Cancerous Fibroblasts

“…Also, based on the UV-Vis spectrometry analysis (not shown), it was deduced that 0.073 mmol of FITC moieties were covalently mounted per gram CNC which was more than the amount reported in previous literature [24,45]. In terms of surface charge, as presented in Table 1, it was found that conjugation of FITC had altered the zeta potential of CNC from −38.6 mV to −17.7 mV while the Ð improved from 0.703 to 0.371, which was considered acceptable for the delivery application [46].…”

The Evaluation of Drug Delivery Nanocarrier Development and Pharmacological Briefing for Metabolic-Associated Fatty Liver Disease (MAFLD): An Update

“…Self-emulsifying drug delivery systems (SEDDs) ( Figure 9 ) have sparked profound interest from pharmaceutical researchers and industries through mainly antibiotic and antiviral SEDDs products in the market [ 186 ]; this micro/nanosystem offers droplet sizes of 5 µm to 200 nm [ 187 ] and <100 nm as well [ 188 ]. It can enhance the oral delivery of various therapeutic agents with different physicochemical properties [ 189 , 190 ], with either initial in vitro burst release, followed by a gradual-release phase or a sustained release profile [ 191 , 192 , 193 , 194 ]. SEDDs exist as liquid and solid formulations, where the solid form is suggested to provide better stability, reproducibility, and patient compliance, in addition to ease of process control, and various pharmaceutical dosage forms production (powders, capsules, tablets, or pellets) with the possibility of developing a controlled in vitro release attitude by mixing these dosage forms with suitable polymers or coating with polymeric films [ 193 , 195 ].…”