Ascorbic Acid Formulation Research Articles

Formulation of Ascorbic Acid and Betaine-based Therapeutic Deep Eutectic System for Enhanced Transdermal Delivery of Ascorbic Acid.

L-ascorbic acid (AA), a potent antioxidant, is commonly used topically in the pharmaceutical and cosmetic fields. However, the incorporation of AA into topical formulations is difficult because of its highly unstable nature and relatively poor skin permeability. In this study, we propose an alternative strategy for improving the solubility and topical delivery of AA through its conversion to a therapeutic deep eutectic system (THEDES). AA and betaine (Bet)-based THEDESs were prepared at certain molar ratios and characterized using polarized optical microscopy, Fourier transform infrared spectroscopy, and differential scanning calorimetry. Solubility tests showed that AA in the form of THEDES was readily soluble in various polyols (glycerin, 1,3-butylene glycol, dipropylene glycol, and 1,3-propanediol) at a high concentration (approximately 40%). Furthermore, compared to AA alone or the physical mixture of AA and Bet, AA-based THEDES significantly enhanced AA delivery through porcine skin. In an in vivo human study, THEDES-containing serum reduced the markers of aging and induced an even skin tone. These findings indicate the utility of AA and Bet-based THEDES as novel transdermal delivery systems for AA. Furthermore, our approach also showed good extension to developing gluconolactone, a well-known natural antioxidant, and Bet-based THEDES, showing potential application in transdermal delivery systems.

Formulation of Ascorbic Acid and Skim Milk in Feed for Salinity Stress in Artemia sp.

Artemia sp. is recognized for its abundant and comprehensive nutritional profile, yet it lacks the inherent ability to produce vital elements such as vitamins, Eicosapentaenoic Acid (EPA), and Docosahexaenoic Acid (DHA), necessitating their acquisition from external sources. To augment the nutritional quality of Artemia sp., enrichment becomes imperative. This research aimed to evaluate the toxicity of ascorbic acid when used as a feed for Artemia sp. and investigate the influence of ascorbic acid enrichment and the addition of skim milk to the feed on Artemia sp.'s response to salinity stress. The study employed a Completely Randomized Design (CRD). The toxicity assessment of ascorbic acid utilized the Brine Shrimp Lethality Test (BSLT) method, yielding an LC50 value of 200.84 (> 1000 ppm), indicating toxicity to Artemia sp. Salinity stress resistance exhibited variability across treatments, with the longest survival times observed sequentially in Artemia sp. subjected to AS treatment 3 (20 hours), AS 2, and the control (16 hours), SM, AS 3, and C 1 (12 hours), and C 2 (8 hours). The enrichment of Artemia sp. feed with ascorbic acid and skim milk significantly influenced (sig. = 0.002) its resistance to salinity stress, with the optimal formulation identified at 200 ppm of ascorbic acid.

Orally disintegrating films based on sodium alginate as a carrier vehicle for vitamin C

SummaryOrally disintegrating films (ODFs) have been studied for their innovative way of delivering active compounds into the oral cavity. The study aimed to develop and evaluate ODFs using sodium alginate and different concentrations of vitamin C. Four formulations were evaluated for barrier, mechanical, thermal, microstructural properties, surface pH, disintegration time and concentration of vitamins. The ODFs produced showed high solubility, pH close to oral and disintegration time ranging from 24.66 s for the control formulation to 56.28 s for the 1% ascorbic acid formulation. The release of vitamin C occurred after 1 min of reaction for all formulations with the lowest concentration (0.25%) releasing a volume of 80.46 mg g−1. Thermal analyses demonstrated the presence of sodium alginate and vitamin C, and an interaction between them, confirmed by FTIR spectra. This interaction was interesting for ODFs since it can affect the properties and release of the active compound from the polymeric matrix. The results positively demonstrated that sodium alginate can be a promising polymer in the production of ODFs and for use in the delivery of vitamin C.

Effect of liposomal formulation of ascorbic acid on corneal permeability

Ascorbic acid (AA) has a pivotal role in corneal wound healing via stimulating the biosynthesis of highly organized extracellular matrix components, but its rapid degradation and low corneal permeability limits its therapeutic effects. In this paper, we present the pharmacokinetic properties of a liposomal-based formulation of AA in terms of corneal permeation. Chemical stability, shelf-life, and drug release rate of lyophilized liposome (AA-LLipo) formulation was determined in comparison to free-form of AA solution using high-performance liquid chromatography (HPLC) and rapid equilibrium dialysis. In vitro transcorneal permeability was studied using a parallel artificial membrane permeability assay (PAMPA). Ex vivo permeation was examined on AA-LLipo-treated porcine cornea by determining the AA content on the ocular surface, in the cornea as well as in the aqueous humor using HPLC, and by Raman-mapping visualizing the AA-distribution. Our results showed that the liposomal formulation improved the chemical stability of AA, while drug release was observed with the same kinetic efficiency as from the free-form of AA solution. Both corneal-PAMPA and porcine corneal permeability studies showed that AA-LLipo markedly improved the corneal absorption kinetics of AA, thus, increasing the AA content in the cornea and aqueous humor. AA-LLipo formulation could potentially increase the bioavailability of AA in corneal tissues.

Combined Antioxidant Formulation of Ascorbic Acid with Resveratrol Ameliorates Isoproterenol-Induced Myocardial Infarction in Rats

The current investigation was proposed to assess the effectiveness of the combination of resveratrol and ascorbic acid against Isoproterenol (ISO)-induced myocardial infarction in rats. The experimental model was divided into six groups (n = 6 in each group). Group I: control, Group 2: isoproterenol (ISO)-100 mg/kg b.wt, Group 3: ISO+Resveratrol (RES) (20 mg/kg b.wt) treated, Group 4: ISO+ Ascorbic acid (AA) (80 mg/kg b.wt) treated, Group 5: ISO+RES (20 mg/kg b.wt)+AA (80 mg/kg b.wt) treated and Group 6 : RES (20 mg/kg b.wt)+ AA (80 mg/kg b.wt) alone treated. The study showed an increase in lipid peroxides and cardiac markers in the serum samples of experimental animals administered with ISO. Treatment with RES and AA individually and a combinational formulation brought a significant decrease in lipid peroxides and cardiac markers. They increased the level of enzymatic antioxidants and non-enzymatic antioxidant levels. Histopathological results showed the distortion of heart architecture among the experimental groups administered with ISO and significant recovery when treated with RES and AA individually and in their combination. The study presents the effective combination of RES and AA in combating ISO-induced myocardial infarction and protection against ROS-mediated oxidative stress.

Ascorbic Acid as an Adjuvant to Unbleached Cotton Promotes Antimicrobial Activity in Spunlace Nonwovens.

The development of affordable, effective, and environmentally friendly barrier fabrics is a current goal in antimicrobial textile development. The discovery of new routes to achieve non-toxic naturally occurring molecules with antimicrobial activity is of interest in the development of materials that promote wound healing, improve hygiene, and offer protection against nosocomial infection. Highly cleaned and sterile unbleached cotton has constituents that produce hydrogen peroxide at levels commensurate with those that favor cell signaling in wound healing. Here, we show the antimicrobial and antiviral properties of spunlaced griege cotton-containing nonwovens treated with ascorbic acid formulations. The mechanism of action occurs through the promotion of enhanced hydrogen peroxide activity. The levels of hydrogen peroxide activity afford antimicrobial activity against Gram-negative and Gram-positive bacteria and antiviral activity against MS2 bacteriophages. Spun-bond nonwoven unbleached cotton was treated with ascorbic acid using traditional pad-dry-cure methods. An assessment of antibacterial and antiviral activity against Staphylococcus aureus, Klebsiella pneumoniae, and MS2 bacteriophages with the AATCC 100 test method showed a 99.99% inhibitory activity. An approach to the covalent attachment of ascorbic to cellulose through citric acid crosslinking chemistry is also discussed. Thus, a simple, low-cost approach to antimicrobial and antiviral cotton-based nonwovens applicable to dressings, nosocomial barrier fabrics, and face masks can be adopted by combining ascorbic acid with spunlace greige cotton nonwoven fabrics.

Ascorbic acid formulation for survivability and diazotrophic efficacy of Azotobacter chroococcum Avi2 (MCC 3432) under hydrogen peroxide stress and its role in plant-growth promotion in rice (Oryza sativa L.)

Oxidative stress generates reactive oxygen species which causes cell damage of living organisms and are normally detoxified by antioxidants. Indirect reports signify the damages caused by reactive oxygen species and neutralized by antioxidant, but the direct evidence to confirm this hypothesis is still unclear. To validate our hypothesis, an attempt was made in a diazotrophic bacterium (Azotobacter chroococcum Avi2) as a biological system, and hydrogen peroxide (H2O2) and ascorbic acid were used as oxidative stress and antioxidant supplement, respectively. Additionally, rice plant-growth attributes by Avi2 was also assessed under H2O2 and ascorbic acid. Results indicated that higher concentration of H2O2 (2.5 mM-4.5 mM) showed the complete mortality of Avi2, whereas one ppm ascorbic acid neutralized the effect of H2O2. Turbidity, colony forming unit, DNA quantity, nifH gene abundance, indole acetic acid and ammonia productions were significantly (p < 0.5) increased by 11.93%, 17.29%, 19.80%, 74.77%, 71.89%, and 42.53%, respectively in Avi2-treated with 1.5 mM H2O2 plus ascorbic acid compared to 1.5 mM H2O2 alone. Superoxide dismutase was significantly (p < 0.5) increased by 60.85%, whereas catalase and ascorbate peroxidase activities were significantly (p < 0.05) decreased by 64.28% and 68.88% in Avi2-treated with 1.5 mM H2O2 plus ascorbic acid compared to 1.5 mM H2O2 alone. Germination percentage of three rice cultivars (FR13a, Naveen and Sahbhagi dhan) were significantly (p < 0.5) increased by 20%, 13.33%, and 4%, respectively in Avi2-treated with 0.6 mM H2O2 plus ascorbic acid compared with uninoculated control. Overall, this study indicated that ascorbic acid formulation neutralizes the H2O2-oxidative stress and enhances the survivability and plant growth-promoting efficacy of A. chroococcum Avi2 and therefore, it may be used as an effective formulation of bio-inoculants in rice under oxidative stress.

Pentafluorophenyl bonded phase separation: the assay of Australian antioxidant formulation of ascorbic acid, rutin and hesperidin

This work describes two novel validated HPLC methods for the separation and determination of potent antioxidant formulation.

Meta-analysis of ascorbic acid for prevention of postoperative atrial fibrillation after cardiac surgery.

Results of a systematic review and meta-analysis of published data on use of ascorbic acid to prevent postoperative atrial fibrillation (POAF) after cardiac surgery are presented. MEDLINE and other sources were searched for reports on trials evaluating the effects of preoperative and/or postoperative use of ascorbic acid in patients undergoing cardiac surgery. For each study selected for meta-analysis, an assessment for risks of methodological bias was performed. Data on POAF frequency and length of stay (LOS) outcomes were pooled and analyzed via random-effects modeling. The 11 identified studies involved patients receiving coronary artery bypass grafts with or without valve replacement; both i.v. and oral ascorbic acid formulations were used. Analysis of pooled outcomes data on treatment and control groups indicated that ascorbic acid prophylaxis was associated with reductions in POAF frequency (odds ratio, 0.44; 95% confidence interval [CI], 0.32 to 0.61), intensive care unit (ICU) LOS (difference in means, -0.24 day; 95% CI, -0.45 to -0.03 day), and total hospital LOS (difference in means, -0.94 day; 95% CI, -1.65 to -0.23 day). Significant statistical, methodological, and clinical heterogeneity were observed. A meta-analysis revealed that, compared with use of a placebo or a nonplacebo control, perioperative administration of ascorbic acid to patients undergoing cardiac surgery was associated with a reduced frequency of POAF and a shorter ICU LOS and total hospital LOS.

Niosomes of ascorbic acid and α-tocopherol in the cerebral ischemia-reperfusion model in male rats.

The objective of the present study was to prepare a stable iv injectable formulation of ascorbic acid and α-tocopherol in preventing the cerebral ischemia. Different niosomal formulations were prepared by Span and Tween mixed with cholesterol. The physicochemical characteristics of niosomal formulations were evaluated in vitro. For in vivo evaluation, the rats were made ischemic by middle cerebral artery occlusion model for 30 min and the selected formulation was used for determining its neuroprotective effect against cerebral ischemia. Neuronal damage was evaluated by optical microscopy and transmission electron microscopy. The encapsulation efficiency of ascorbic acid was increased to more than 84% by remote loading method. The cholesterol content of the niosomes, the hydrophilicity potential of the encapsulated compounds, and the preparation method of niosomes were the main factors affecting the mean volume diameter of the prepared vesicles. High physical stability of the niosomes prepared from Span 40 and Span 60 was demonstrated due to negligible size change of vesicles during 6 months storage at 4–8°C. In vivo studies showed that ST60/Chol 35 : 35 : 30 niosomes had more neuroprotective effects against cerebral ischemic injuries in male rats than free ascorbic acid.

Assessment of clinical efficacy of different concentrations of topical ascorbic acid formulations in the treatment of melasma

Assessment of clinical efficacy of different concentrations of topical ascorbic acid formulations in the treatment of melasma

Formulation of ascorbic acid microemulsions with alkyl polyglycosides

Ascorbic acid microemulsions for topical application were developed. In this study, microemulsions were prepared using HLD (hydrophilic lipophilic deviation) concept to optimise the formulation. From this optimal formulation, the realisation of dilution ternary diagrams leads to obtain microemulsion zones. In addition, the effects of composition variable on the physicochemical characteristics of each system were investigated. After optimisation of the microemulsion systems, ascorbic acid was loaded in the formulations. Surface tension and small angle neutron scattering were used to characterise the surface properties and the structure of the microemulsions. Bicontinuous structure microemulsions were identified, and the influence of ascorbic acid localisation at the interface leading to modifications of the microemulsion structure was pointed out. The solubilisation of ascorbic acid, the stabilisation and in vitro transdermal penetration “Frantz cells” of ascorbic acid microemulsions were studied. Three different microemulsions were envisaged. The results confirmed that these microemulsion systems present a real interest for formulation and protection of ascorbic acid. Regarding their transcutaneous penetration behaviour, the different microemulsions studied could be useful for different topical applications. A major location of ascorbic acid found in the epidermis where the decomposition of melanin occurred indicates that microemulsion could be considered as a suitable carrier system for application of ascorbic acid as a whitening agent. In addition, a good passage of the drug in the dermis could be interesting for the relative oxygen matrix damage.

Ascorbic acid: useful as a buffer agent and radiolytic stabilizer for metalloradiopharmaceuticals.

The goal of this study is to explore the use of ascorbic acid (AA) as a buffer agent and a radiolytic stabilizer for preparation and stabilization of radiolabeled DOTA-biomolecule conjugates. Results from a titration experiment show that 0.1 M AA solution has sufficient buffer capacity at pH 5.0 while 0.5 M AA solution is useful even at pH 6.0. The radiolabeling experiment using TA138, a DOTA-conjugated nonpeptide integrin alpha(v)beta(3) receptor antagonist, clearly demonstrates that AA is a good buffer agent for pH control and an excellent antioxidant for stabilization of metal-labeled diagnostic ((111)In) and therapeutic ((90)Y and (177)Lu) radiopharmaceuticals if the radiolabeling is performed at pH 5-6. There is no need for the additional stabilizer (e.g., gentisic acid) and buffer agent such as ammonium acetate. The anaerobic AA formulation described in this study is particularly useful for radiolabeling of small biomolecules, which are sensitive to the radiolytic degradation during radiolabeling.

Drug Adjuvant Interaction Study Using DSC Supported by Isothermal Method

Extensive work has been done in the field of drug adjuvant interaction studies using differential scanning calorimetry (DSC), but conclusive interpretive techniques could not be reached since very few workers supplemented their work by conventional isothermal stability testing methods. This work compared the drug adjuvant thermogram with results obtained from isothermal stability studies and used it to reiterate the results of the drug adjuvant thermograms. In the formulation of ascorbic acid in a cosmetic preparation, the various adjuvants were tested for interactions first by the isothermal stability testing technique, which was followed by DSC scanning of the drug adjuvant. The results of the two methods were compared and correlated.

Granulation of Acetaminophen by a Rotating Fluidized-Bed Granulator

The purpose of this research was to evaluate the use of a rotating fluidized-bed granulator to produce acetaminophen granules with sufficient binding force between particles and good plasticity in tablets. Ethenzamide and ascorbic acid were used to compare the relationship between granulation and the sample wetness. It was revealed that a blade rotation rate of 300 rpm, inlet air flow rate of 42 m3/hr, and spraying pressure of 1.5 kg/cm3 produced tablets with the best properties. The granule and tablet properties of ethenzamide and ascorbic acid were compared to those of acetaminophen. These compounds showed different wetting behaviors with water and different compression behaviors. With an increase in medicament content, tablet hardness increased except for the ascorbic acid formulation. Capping and sticking were observed in acetaminophen and in ascorbic acid, respectively, and acetaminophen and ethenzamide showed prolonged disintegration time.

Bioequivalence Study of Three Ascorbic Acid Tablet Formulations in Healthy Male Volunteers

This study compares the bioequivalence of three ascorbic acid formulations (test: Celong 500 mg prolonged release tablets from Whitehall; standard: Cewin 500 mg prolonged release tablets from Winth...

Oral administration of different formulations of ascorbic acid to the horse

Summary The absorption of crystalline ascorbic acid, ascorbyl palmitate, ascorbyl stearate and a formulation of ascorbic acid was investigated in six mature Thoroughbred horses following oral administration. It was found that ascorbyl palmitate gave both highest plasma concentrations and greatest area under the curve (AUC) for ascorbic acid. Least variation between animals also occured for this preparation. No apparent absorption was seen in some animals given ascorbic acid or ascorbyl stearate.

Polyethylene glycol as a binder for tablets.

Polyethylene glycol 6000 was evaluated as a binder for the direct compression of 11 tablet formulations. Six formulations compressed quite well, and the resulting tablets were satisfactory in all respects. To evaluate stability, actual shelflife studies were considered more appropriate than the accelerated studies. After a shelflife of 3 years, five of the six formulations were stable. The ascorbic acid formulation was stable for up to 18 months.

A Study of the Chemical and Physical Stability of Ascorbic Acid, Folic Acid, and Thiamine Hydrochloride Tablets Formulated with Emcompress Standard

Tablets which were prepared from separate formulations of Emcompress StandardR, a commercially available directly compressible granulation, with ascorbic acid, folic acid, and thiamine hydrochloride were subjected to accelerated aging conditions and studied for chemical stability and such physical parameters as hardness, friability, and disintegration time. Other physical factors which could affect the interpretation of the data, such as moisture content, particle size distribution, angle of repose, weight variation, and hardness were also studied using fresh samples.Accelerated aging showed that the ascorbic acid formulation was chemically unstable; the tablets became soft, the frability increased markedly, and the disintegration time decreased. The folic acid formulation was chemically stable, but the tablets became soft, the friability increased, and disintegration time increased. The thiamine hydrochloride formulation was also chemically stable—the tablets became soft, the disintegration time decreased, and the friability increased.

A Note On The Use Of Sorbitol Solution In Pharmaceutical Formulations

Evidence is presented to indicate the significance of the shipping containers for commercial sorbitol solutions used in the formulation of liquid dosage forms. Some inconsistency in stability data of ascorbic acid formulations is attributed to the relatively high trace metal content of the sorbitol solution used. This solution was supplied in a poorly protected metal container.