Ascorbyl Palmitate Research Articles

Microencapsulation of Chia Seed Oil by Spray‐Drying: Influence of the Antioxidant Addition

AbstractChia seed oil has a high content of polyunsaturated fatty acids, giving it nutritionally beneficial qualities, although determining its high susceptibility to oxidative deterioration. Microencapsulation and natural antioxidants are alternatives to protect this oil during its processing and storage. This work aims to study the physicochemical characteristics and the oxidative stability of chia seed oil microencapsulated with different antioxidants (rosemary extract, blend of rosemary and chamomile extracts, ascorbyl palmitate) by spray‐drying using sodium caseinate and lactose as wall material. The microencapsulation efficiency and the moisture content are >97% and <3% d.b., respectively. Scanning electron microscopy shows that the microcapsules are spherical, with diameters ranging between 11.3 and 14.8 µm. At t = 0, the microencapsulated oil recorded a ti = 12.7 h, seven times greater than that of the bulk‐oil. The addition of the antioxidants increases the ti of the microencapsulated oil. The addition of ascorbyl palmitate maintains the peroxide value under the acceptable limit after 60 d of storage (25 °C, darkness, HR 33%). Thus, microencapsulation by spray drying of chia oil with ascorbyl palmitate addition will be the most appropriate studied system to obtain microparticles with high efficiency and oxidative stability during the processing and storage.Practical Application: This study contributes to investigating the microencapsulation of omega‐3 fatty acids n‐3 fatty acids (FAs) from a novel oilseed (chia oil), applying different antioxidants, including those from vegetable sources such as rosemary and chamomile extracts, to confer additional protection to microencapsulated oil. Thus, the application of these techniques will enable the delivery of this vegetable oil for the development of functional foods.

Potential use of nanoformulated ascorbyl palmitate as a promising anticancer agent: First comparative assessment between nano and free forms

The aim of the present study is to evaluate, for the first time, the anticancer activity of a stable nanoformulation of ascorbyl palmitate (APnp) and investigate its therapeutic action as well as its mechanism against Ehrlich ascites carcinoma (EAC)-bearing mice in comparison with native AP. AP was loaded into pluronic nanoparticles, fully characterized and then studied as an anticancer agent using EAC model. The APnp were spherical and attained a small size of 220 ± 9 nm and a zetapotential of −41.16 ± 2 mV. The release profile of the AP from the nanoparticles was around 72% within the first 2 h and the rest of the drug amount was released sustainably within 9 days. The results of the present study demonstrated that APnp treatment destroyed tumors with inhibition of proliferation by inhibiting signal transducer and activator of transcription 3 (STAT3) pathway leading to induction of apoptosis and cell cycle arrest at G2/M phase as well as preventing metastasis and invasion. Moreover, APnp significantly elevated antioxidant levels [superoxide dismutase (SOD), catalase (CAT) and reduced glutathione (GSH)], and significantly decreased the levels of oxidative stress biomarkers [malondialdehyde (MDA) and nitric oxide (NO)]. Besides, mitochondrial and nuclear degeneration in cancer cells was demonstrated by an electron microscope to be more severe in the case of using our newly-developed APnp. The present study revealed the superiority of APnp as a potent anticancer agent over free AP via increasing its bioavailability and specificity towards cancer cells.

Ascorbyl Palmitate-Vitamin C Effective Friction Modifier and Wear Inhibitor for Steel in a PAO Base Oil

Ascorbyl palmitate (AP), known as a nutrition pill, and an antioxidant agent in food, has demonstrated excellent lubricity as an additive in PAO4. Adding one wt% AP in PAO4 drastically decreases friction Coefficient (CoF) up to 66% and protects the steel surface from wear. Meanwhile, it shows a more vital friction reduction ability than conventional Mo-based additives and fatty acids, especially palmitic acid. Ascorbic acid core on AP optimises palmitic acid lubricity by forming robust chemical C-O-Fe bond on steel, increasing surface coverage rate. Masked by AP self-assembled layers, steel surfaces can also handle extreme pressure (up to 2.34 GPa) and temperature (150 °C) with unmeasurable wear. This work broadens human-friendly AP vitamin C application for industrial use and introduces a new pathway for optimizing fatty acids lubricity.

Changes of molecular mobility of ascorbyl palmitate and α-tocopherol by phospholipid and their effects on antioxidant properties in bulk oil

Molecular mobility of ascorbyl palmitate and α-tocopherol in the presence of 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) were determined by NMR relaxation technique. Synergistic effects of DOPC on the antioxidative capacities of ascorbyl palmitate were evaluated in DPPH radical scavenging assay and bulk oil matrix. NMR relaxation technique can provide information on the mobility of protons. Molecular mobility of two protons in hydroxyl group of ascorbyl palmitate decreased by 85 and 78% in the presence of DOPC compared to those without DOPC. However, proton mobility of α-tocopherol increased by 41% when DOPC was present. DOPC significantly enhanced the DPPH reactivity in medium chain triacylglycerol, while this effect was not observed in α-tocopherol. Mixture of ascorbyl palmitate with DOPC showed synergistic antioxidant properties in corn oil at 60 °C. DOPC may make protons of ascorbyl palmitate in more rigid state, which can enhance hydrogen donating ability and antioxidant properties of ascorbyl palmitate in bulk oils.

Development of hemp seed oil nanoemulsions loaded with ascorbyl palmitate: Effect of operational parameters, emulsifiers, and wall materials

The perceived health properties of hemp seed oil, as one of the few plant-basedsources of omega-3 and omega-6 fatty acids with an ideal ratio of 1:3, suggest its incorporation in food-grade emulsions to improve its water solubility and oxidative stability. The current research's main aim was nanoemulsification of hemp seed oil using the oil-in-water emulsification method followed by ultrasonication. The entrapment efficiency of the nanoemulsions for antioxidant ascorbyl palmitate and its impact on oxidative stability of the oil was also evaluated. Gum arabic: maltodextrin in 75:25 ratio could result in nanoemulsion with entrapment efficiency of 97.10 % for ascorbyl palmitate and radical scavenging activity of oil-soluble bioactives of 92.13 %. Moreover, incorporation of ascorbyl palmitate could effectively retard the oxidation, specifically in nanoemulsions containing gum Arabic. The optimum formulation of nanoemulsion having an average droplet size of 293 nm can be applied as an ideal vegetarian source of omega-3 fatty acids.

Tocopherol Content in Peanuts after gamma-Irradiation: Effect of Ascorbyl Palmitate Addition on Oil Stability

Food irradiation has a number of advantages over the other conventional preservation technologies like canning, freezing, pasteurization and addition of chemical preservatives. It is a fast and inexpensive treatment which can be performed in the original packaging eliminating the risk of re-pollution. Unfortunately, changes as a result of irradiation may occur in biologically active compounds, especially lipids and antioxidants, thus decreasing the oil oxidative stability. So, this study is focused on the evaluation of changes in the content of tocopherols in oil, extracted from peanuts subjected to gamma-irradiation with a dose of 10 kGy. The effect of ascorbyl palmitate added to the oil in different proportions has been studied as well. The results showed decreasing of tocopherols in the oil from irradiated peanuts. On the other hand, addition of ascorbyl palmitate in 1:1 ratio to the native γ-tocopherol indicated synergistic effect which not only compensated the negative effect of irradiation but decreased twice the oxidation rate compared to that of non-irradiated oil.

Impact of glucose syrup and antioxidants on properties and oxidative stability of microcapsules loaded with skipjack tuna eyeball oil

Effects of glucose syrup (GS) at different ratios as wall materials on encapsulation efficiency (EE) and properties of micro-encapsulated skipjack tuna eyeball oil (ME-STEO) were determined. Highest EE (90.45-90.61%) was obtained when the mixtures of fish gelatin (FG), sodium caseinate (SC) and GS at ratios of 1:1:1 and 1:1:2 (w/w/w) were used. Moisture content, water activity and lightness (L*) of ME-STEO were declined when the amount of GS was augmented, but redness (a*), yellowness (b*), total difference in color (∆E*) and surface shrinkage of ME-STEO were increased. When α-tocopherol (AT) in combination of ascorbyl palmitate (AP) were incorporated in STEO, lower peroxide and thiobarbituric acid substances were found in ME-STEO than others (P < 0.05). Mixtures of wall material (FG:SC:GS=1:1:2) and the addition of 200 ppm AT in combination with 200 ppm AP yielded STEO as a core with higher oxidative stability during 30 days of storage at room temperature.

Encapsulation of ascorbyl palmitate in corn starch matrix by extrusion cooking: Release behavior and antioxidant activity

The main limitation associated with the oral delivery of ascorbyl palmitate, a potent food antioxidant, is its susceptibility to oxidative deterioration. The main objective of the current research was to encapsulate ascorbyl palmitate into corn starch matrix using extrusion cooking and evaluate its release behavior and oxidative stability. Results showed that ascorbyl palmitate was efficiently encapsulated (96.06–99.28%) in the starch matrix using the extrusion technique. The release behavior of ascorbyl palmitate from the extruded starch matrix during simulated upper gastrointestinal tract conditions was slow but steady (18.92–28.32% after 180 min) and presented a sustainable antioxidant activity. Acid treatment (pH 2.0) increased the release rate of ascorbyl palmitate from the extruded starch matrix. Furthermore, the antioxidant capacity of ascorbyl palmitate released from the extruded samples stored in both darkness and under UV radiation at 40 °C was found to be remarkably retained (p > 0.05) for up to three months.

Effect of Lipid Vehicles on Solubility, Stability, and Topical Permeation of Delta-9-Tetrahydrocannabinol.

Delta-9-tetrahydrocannabinol (THC) is one of the most effective antinociceptive agents used in the treatment of peripheral neuropathy. THC is highly lipophilic and susceptible to thermal and oxidative degradation. Identifying appropriate solvents in which THC is stable as well as adequately solubilized is crucial in developing topical dosage forms. Lipid solvent systems are of utmost utility and relevance for formulating highly lipophilic drugs. Hence, the objective of this project was to screen the solubility of THC in lipidic excipients, monitor THC content in the selected vehicles during stability, and study the influence of these excipients on permeation of THC across skin. The solubility of THC in liquid lipid excipients was in the range of 421 to 500mg/g. The solubility of THC in solid lipid excipients was in the range of 250 to 750mg/g. THC in its neat form was poorly stable, but when dissolved in lipid-based excipients, its stability improved significantly. THC in lipid excipients was more stable at 4 ± 3°C compared to samples stored at 25 ± 2°C. The antioxidants (butylated hydroxytoluene and ascorbyl palmitate) used in the excipients further improved the stability of THC. The results demonstrated that the liquid and solid lipid excipients used in the study could solubilize THC freely and mitigate the degradation of THC significantly. The binary combination of lipid excipients enhanced THC skin permeation and retention, demonstrating the potential for topical formulation development of THC.

Mechanism Study on Nanoparticle Negative Surface Charge Modification by Ascorbyl Palmitate and Its Improvement of Tumor Targeting Ability.

Surface charge polarity and density influence the immune clearance and cellular uptake of intravenously administered lipid nanoparticles (LNPs), thus determining the efficiency of their delivery to the target. Here, we modified the surface charge with ascorbyl palmitate (AsP) used as a negatively charged lipid. AsP-PC-LNPs were prepared by dispersion and ultrasonication of AsP and phosphatidylcholine (PC) composite films at various ratios. AsP inserted into the PC film with its polar head outward. The pKa for AsP was 4.34, and its ion form conferred the LNPs with negative surface charge. Zeta potentials were correlated with the amount and distribution of AsP on the LNPs surface. DSC, Raman and FTIR spectra, and molecular dynamics simulations disclosed that AsP distributed homogeneously in PC at 1–8% (w/w), and there were strong hydrogen bonds between the polar heads of AsP and PC (PO2−), which favored LNPs’ stability. But at AsP:PC > 8% (w/w), the excessive AsP changed the interaction modes between AsP and PC. The AsP–PC composite films became inhomogeneous, and their phase transition behaviors and Raman and FTIR spectra were altered. Our results clarified the mechanism of surface charge modification by AsP and provided a rational use of AsP as a charged lipid to modify LNP surface properties in targeted drug delivery systems. Furthermore, AsP–PC composites were used as phospholipid-based biological membranes to prepare paclitaxel-loaded LNPs, which had stable surface negative charge, better tumor targeting and tumor inhibitory effects.

Improving the oxidation stability of high-oleic sunflower oil with composite antioxidants

This study aimed to search for the optimum antioxidant mixture for improvement of the stability of high-oleic sunflower oil. Seven antioxidants including vitamin E, phytic acid, antioxidant of bamboo leaves, rosemary extract, tea polyphenols, ascorbyl palmitate (AP) as well as tea polyphenol palmitate (TPP) were used. Peroxide value, free radicals and Rancimat induction time results all proved that TPP was the best single antioxidant. Therefore, TPP was selected to mix with other antioxidants to form composite antioxidants. The combination of TPP and AP revealed the best antioxidant efficiency among the composite antioxidants comprised of two and three constituents in the oil. By optimizing the mixture proportions, the best antioxidant activity could be achieved when combining 480 mg/kg TPP with 40 mg/kg AP. The high-oleic sunflower oil sample (containing 480 mg/kg TPP and 40 mg/kg AP) had 1.96-fold longer shelf life (prediction by Rancimat method) compared with the blank sample.

UV Spectrophotometric Method Development and Validation for the Determination of Ascorbyl Palmitate in Bulk and its Pharmaceutical Dosage Form

A simple, economical, accurate, precise and less time-consuming UV spectrophotometric method has been developed and validated for estimation of Ascorbyl palmitate in bulk and pharmaceutical formulations. In this method, Ascorbyl palmitate exhibits maximum absorbance (λ max) at 261nm. The drug obeys Beer’s law in the concentration range of 2-12μg/ml. The method was validated as per the International Conference on Harmonization (ICH) guidelines. Drug followed the linearity in the concentration range of 2-12μg/ml with correlation coefficient (R2) of 0.998. The validity of the proposed method was assessed by applying the standard addition technique where the percentage recovery of the added standard was found to be 100% -109.7%. The limit of detection and quantification were calculated to be 0.1200µg/ml and 0.363μg/ml respectively. The proposed method is recommended for routine analysis of Ascorbyl palmitate in bulk and dosage forms in quality control testing laboratories. Since it is rapid, simple, accurate, sensitive and economical.

Improving the Oxidation Stability and Shelf-Life of Peanut Oil by Addition of Rosemary Extract Combined with Vitamin C and Ascorbyl Palmitate

Rosemary extracts are natural antioxidants, which can be considered an alternative for synthetic antioxidants in the food industry. The aim of the present study was to evaluate the oxidation stability and shelf-life of rosemary extracts combined with vitamin C (VC) and ascorbyl palmitate (AP) in peanut oil stored at 65°C. Peanut oil with tertbutyl hydroquinone (TBHQ) and without additives served as positive and negative controls, respectively. The peroxide value (POV), thiobarbituric acid reactant (TBARs), conjugated diene (CD), and conjugated triene (CT) values of the peanut oil samples were evaluated during accelerated storage every 48 h. Among them, 0.23 g/kg rosemary extracts combined with 0.13 g/kg VC and 0.07 mg/kg AP exhibited the best oxidative stability. Additionally, the oxidation kinetics model predicated that the rosemary extracts combined with VC and AP could effectively prolong the shelf-life of peanut oil. In accelerated storage, the rosemary extracts combined with VC and AP not only inhibited peanut oil oxidation like chemical antioxidants, but also were safer than chemical antioxidants. Therefore, the rosemary extracts combined with VC and AP were an effective alternative to chemical antioxidants, which could improve the oxidation stability and shelf-life of peanut oil.

Synthesis and In Vitro Characterization of Ascorbyl Palmitate-Loaded Solid Lipid Nanoparticles.

Antitumor applications of ascorbic acid (AA) and its oxidized form dehydroascorbic acid (DHA) can be quite challenging due to their instability and sensitivity to degradation in aqueous media. To overcome this obstacle, we have synthesized solid lipid nanoparticles loaded with ascorbyl palmitate (SLN-AP) with variations in proportions of the polymer Pluronic F-68. SLNs were synthesized using the hot homogenization method, characterized by measuring the particle size, polydispersity, zeta potential and visualized by TEM. To investigate the cellular uptake of the SLN, we have incorporated coumarin-6 into the same SLN formulation and followed their successful uptake for 48 h. We have tested the cytotoxicity of the SLN formulations and free ascorbate forms, AA and DHA, on HEK 293 and U2OS cell lines by MTT assay. The SLN-AP in both formulations have a cytotoxic effect at lower concentrations when compared to ascorbate applied the form of AA or DHA. Better selectivity for targeting tumor cell line was observed with 3% Pluronic F-68. The antioxidative effect of the SLN-AP was observed as early as 1 h after the treatment with a small dose of ascorbate applied (5 µM). SLN-AP formulation with 3% Pluronic F-68 needs to be further optimized as an ascorbate carrier due to its intrinsic cytotoxicity.

Development of the emulsion composition and technology based on iron oleate micelles

This paper addresses the problem of drugs for the treatment of iron deficiency anemia (IDA). Iron deficiency anemia is a clinical and hematological syndrome based on a violation of hemoglobin synthesis resulting from iron deficiency. Clinically, IDA is manifested by symptoms of anemia and sideropenia. The aim of the study is to develop new drugs for the treatment of IDA based on lipophilic iron compounds with oleic acid in the form of a microemulsion. Analogues of the developed compounds are presented on the pharmaceutical market, being registered exclusively as biologically active food additives (Lipofer, Sideral Forte). During the study, the following materials and methods were used: iron (III) oleate with an iron ion concentration of 25 mg/g was obtained by mixing 1.1 g (0.03 mol) of iron nitrate with 6.0 g (0.21 mol) of oleic acids. After that, the mixture was heated to 90℃ for 24 hours under constant stirring. To 3 g of the previously obtained iron (III) oleate solution, 0.56 g of ascorbyl palmitate was added in an equimolar ratio to the iron ion. The mixture was stirred for 24 hours at 90℃. The resulting iron (II) oleate emulsion showed the presence of divalent ions at a concentration of 4.77 mg/g. The total concentration of iron ions in the analyzed oleates of both types was the same. Recalculation for the initial solution in oleic acid showed that the concentration was close to the expected values. Solutions for quantifying the concentrations of the active substances of the drugs under development have been presented. The fundamental possibility of carrying out the in situ reduction of the iron ion in oleic acid using a lipophilic reducing agent, ascorbyl palmitate, has been demonstrated.

Comparison in Content of Total Polyphenol, Flavonoid, and Antioxidant Capacity from Different Organs and Extruded Condition of Moringa oleifera Lam

Recently, interest in exploring phytochemicals with health benefits has grown significantly. In this research, we aimed to develop the processing profile and functionality of Moringa oleifera Lam. Here, we implemented biopolymer-mediated extrudate formulations of M. oleifera (leaves, seed, and husk) in order to enhance the phenolic, flavonoid, and antioxidant capacity. The formulation-1 (F1) was prepared for leaves, seed, and husk using biopolymers (10% w/w), namely: whey protein isolate (10% w/w) and lecithin (5% w/w) with vitamin E (2% w/w). The formulation-2 (F2) was composed of lecithin (5% w/w) with ascorbyl palmitate (10% w/w) and vitamin E (2% w/w), processed by hot-melt extrusion (HME). It was observed that the total phenol and flavonoid contents were persistent in the lecithin-mediated F2 formulation of leaves, seed, and husk. Likewise, antioxidant capacity was significantly stayed in the F2 formulation of all organs, compared to the extrudate and control. The IC50 values revealed that the leaves of the F2 formulation showed strong free radical scavenging capacity compared to the F2 formulation of seed and husk. It was concluded that the F2 formulation could be used in the different parts of M. oleifera processing to boost functionality.

A change-prone zwitterionic hyperbranched terpolymer-based diabetic wound dressing

The long inflammation state and susceptibility to infection of a diabetic ulcer impairs wound healing. In this report, an in situ formed hydrogel dressing with antibacterial and anti-inflammatory activities is designed to nurse diabetic wounds. Firstly, a hyperbranched terpolymer (termed as HBPVD) is synthetized by a unique dynamically controllable reversible addition-fragmentation chain transfer (RAFT) polymerization of poly(ethylene glycol) diacrylate (PEGDA), 1-vinylimidazole (VI), and 2-(N-3-sulfopropyl-N,N-dimethyl ammonium) ethyl methacrylate (DMAPS). The resulted HBPVD is equipped with multi-acrylate end group that can be crosslinked with gelatin methacrylate (GelMA) to form a hydrogel in situ under UV light. The imidazole group in VI can chelate metal ions to enhance the mechanical strength of the hydrogels. The introduction of zwitterion DMAPS imparts the hydrogels thermosensitive and anti-fouling capability to get rid of the bacterial debris from wound beds. Meanwhile, the self-assembled ascorbyl palmitate (AP) nanosheet is encapsulated into the hydrogels, affording a strong anti-inflammatory capability and serving as a reservoir of reducing agent. Based on an Ag+-AP in situ-reduction method, Ag+ complexed by VI in the hydrogel can be homogeneously reduced to Ag nanoparticles. The rheological results confirm that a solid HBPVD/GelMA hydrogel is obtained by UV light irradiation within 1 min. The strength of hydrogels is sharply increased by complexation of metal ions. A strong anti-bacterial ability against both gram-positive and gram-negative bacteria is achieved in HBPVD/GelMA/Ag/AP hydrogel. The HBPVD/GelMA/Ag/AP hydrogel dressing is administrated on humanized wound beds in diabetic rats, which can be conveniently changed by spraying 4 °C Cu2+ solution that fleetly triggers both ion-strengthening and thermosensitive responses. The designed dressing presents a faster wound closure ratio with promoting epithelialization and the density of collagen, decreasing the expression level of pro-inflammatory factors (IL-1β, TNF-α), and improving the expression level of anti-inflammatory factor (IL-10). This change-prone hydrogel dressing with antibacterial and anti-inflammatory capability can provide a promising alternative method to repair diabetic wounds.

Multifunctional nanocarrier with self-catalytic production of nitric oxide for photothermal and gas-combined therapy of tumor

Single treatment often faces the problem that it cannot completely eradicate tumor and inhibit the tumor metastasis. In order to overcome this shortcoming, multi-modal tumor treatment has attracted widespread attention. In the present article, based on ascorbyl palmitate (PA) and l-arginine (l-Arg), a multifunctional nanocarrier is designed for synergetic treatment of tumor with photothermal and nitric oxide (NO) gas therapy. Firstly, PA and l-Arg were self-assembled to form novel functional micelles, PL, with high biosafety using electrostatic interaction and hydrogen bonding. The functional micelles could self-catalyze to produce NO at the tumor site. Then, Ag2S quantum dots having fluorescence imaging and photothermal properties were encapsulated to obtain the nanocarrier, A@PL. The results show that A@PL had a hydrated size of around 78 nm and presented good stability within 30 d. Moreover, in vitro studies indicate that it was efficient with regards to NO self-generating capacity, whereas the photothermal conversion efficiency was as high as 34% under near-infrared light irradiation. The cytotoxicity results show that, when the concentration of A@PL was as high as 2 mM, the survival rate of 3 T3 cells was still 78.23%, proving that the probe has good safety characteristics. Fluorescence imaging results show that its maximum enrichment can be achieved at the tumor site after tail vein injection for 3 h, and out of the body after 24 h, indicating good internal circulation. The in vivo studies show that the rate of inhibition of tumor using the nanocarrier was as high as 98%, and almost overcame the problem of tumor recurrence caused by single treatment, thus presenting a significant tumor treatment effect. This new multifunctional nanocarrier with self-catalytic production of NO provides a new idea for the efficient treatment of tumors.

Effects of different antioxidants and their combinations on the oxidative stability of DHA algae oil and walnut oil.

Through monitoring Rancimat induction time (RIT), peroxide value (POV), and thiobarbituric acid‐reactive substances (TBARS) of docosahexaenoic acid (DHA) algae oil and walnut oil during accelerated storage, the effects of the single and the combinations of seven kinds of antioxidants involving ascorbyl palmitate (AP), phytic acid (PA), vitamin E (VE), antioxidant of bamboo leaves (AOB), rosemary extract, tea polyphenols (TP), and tea polyphenol palmitate (TPP) against lipid oxidation were evaluated. RIT, POV, and TBARS results showed that the DHA algae oil sample containing 600 mg/kg TPP revealed the strongest stability and the walnut oil sample containing 450 mg/kg TPP and 100 mg/kg TP revealed the strongest stability. Then, the shelf lives of two oils were predicted from the extrapolation of the linear regression model between Log RIT and temperature. Our results indicated that the optimal antioxidant could prolong the shelf lives of DHA algae oil and walnut oil by 2.31‐ and 7.74‐fold, respectively.

Diversifying the skin cancer-fighting worthwhile frontiers: How relevant are the itraconazole/ascorbyl palmitate nanovectors?

Fighting malignant neoplasms via repurposing existing drugs could be a welcome move for prosperous cancer remediations. In the current work, nanovehiculation and optimization of the repositioned itraconazole (ITZ) utilizing ascorbyl palmitate (AP) aspasomes would be an auspicious approach. Further, the optimized aspasomes were incorporated in a cream and tracked for skin deposition. The in vivo efficacy of aspasomal cream on mice subcutaneous Ehrlich carcinoma model was also assessed. The optimized aspasomes revealed nano size (67.83 ± 6.16 nm), negative charge (-79.40 ± 2.23 mV), > 95% ITZ entrapment and high colloidal stability. AP yielded substantial antioxidant capacity and pushed the ITZ cytotoxicity forward against A431 cells (IC50 = 5.3±0.27 μg/mL). An appealing privilege was the aspasomal cream that corroborated spreadability, contemplated skin permeation and potentiated in vivo anticancer competence, reflected in 62.68% reduction in the tumor weight. Such synergistic tumor probes set the foundation for futuristic clinical translation and commercialization.