Comparative Stability of Two Anti-Hyperpigmentation Agents: Kojic Acid as a Natural Metabolite and Its Di-Palmitate Ester, Under Oxidative Stress; Application to Pharmaceutical Formulation Design

tazesh, Sahar; Tamizi, Elnaz; Shadbad, Mohammad-Reza Siahi; Mostaghimi, Nazli; Monajjemzadeh, Farnaz

doi:10.34172/apb.2022.031

Cited by 4 publications

(11 citation statements)

References 17 publications

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“…Of note, a decrease in KDP content does not necessarily mean loss of activity, given that KDP can be hydrolyzed to kojic acid. Another possibility for the degradation of KDP and its loss of content is the oxidation of the molecule, which can occur in liquid oxidative stress conditions, as mentioned by Tazesh et al (2021) [ 21 ], leading KDP to suffer oxidative degradation, with the suggested mechanism being ring opening [ 21 ].…”

Section: Resultsmentioning

confidence: 99%

“…KDP content was determined using a high-performance liquid chromatograph coupled to an ultraviolet detector (HPLC–UV) at 250 nm [ 21 ]. Samples were dissolved in THF, acetonitrile, methanol, purified water, and acetic acid (35:30:29:5:1) and kept in an ultrasonic bath for 30 min.…”

Section: Methodsmentioning

confidence: 99%

“…Samples were dissolved in THF, acetonitrile, methanol, purified water, and acetic acid (35:30:29:5:1) and kept in an ultrasonic bath for 30 min. The analysis was performed according to Tazesh et al [ 21 ], with modifications. A Shimadzu chromatograph coupled to a UV detector (SPD-10 AV VP, Shimadzu, Kyoto, Japan), and a Restek C18 column (ROC C18, 5 µm, 4.6 × 250 mm, Restek, Bellefonte, PA, USA) were used.…”

Section: Methodsmentioning

confidence: 99%

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Nanoemulsion Containing Kojic Dipalmitate and Rosehip Oil: A Promising Formulation to Treat Melasma

et al. 2023

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Melasma is a hard-to-treat hyperpigmentation disorder. Combined incorporation of kojic dipalmitate (KDP), the esterified form of kojic acid, and rosehip oil, an oil with antioxidant and skin-regenerating properties, into nanocarrier systems appears to be a suitable strategy to develop high-performance formulations. A high-energy method (Ultra-Turrax®) was used to develop nanoemulsions containing up to 2 mg/mL KDP, 5% rosehip oil, and 7.5% surfactant. Formulations were characterized regarding droplet size, size distribution, pH, density, morphology, KDP content, incorporation efficiency, and stability under different temperature conditions. A scale-up study was conducted. Skin permeation, antioxidant potential, and tyrosinase inhibitory activity were assessed in vitro. Cell viability studies were also performed. Results showed that nanoemulsions containing 1 and 2 mg/mL KDP had incorporation efficiencies greater than 95%, droplet size smaller than 130 nm, suitable size distribution, zeta potential of approximately −10 mV, and good stability over 30 days of refrigerated storage. The nanoemulsion containing 1 mg/mL KDP was chosen for further evaluation because it had lower nanocrystal formation, greater scale-up feasibility and allowed KDP permeation up to the epidermis similarly than observed for 2 mg/mL KDP. This formulation (1 mg/mL KDP) showed antioxidant and depigmenting efficacy, close to that of 1 mM ascorbic acid. No cytotoxicity was observed in formulations concentrations ranging from 0.06% to 1%.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Nanoemulsion Containing Kojic Dipalmitate and Rosehip Oil: A Promising Formulation to Treat Melasma

et al. 2023

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“…HPLC is a versatile technique to evaluate the drug concentration after in transdermal preparations. [21][22][23] A previously validated HPLC method was used for quantitation analyses. 12 To revalidate the method, specificity and linearity parameters were calculated in the same condition as analyzed samples.…”

Section: Resultsmentioning

confidence: 99%

Effects of Transcutol P and Precirol ATO-5 on Percutaneous Absorption of Flutamide from Emulgels

Khalilollah¹,

Shokri²,

Ahmadi³

et al. 2021

Pharm Sci

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Background: Flutamide is a non-steroidal anti-androgenic agent which is not only used in treating prostate cancer but also can be effective in some disorders such as androgenic alopecia and male pattern baldness. Several serious side effects for systemic administration of flutamide can be overcome by emulgel dosage form. Absorption enhancers can promote permeation of flutamide through skin. Percutaneous absorption of Flutamide emulgels with different concentrations of Transcutol P and Precirol ATO5 was studied. Methods: Various emulgel formulations using different concentration of Transcutol P and Precirol ATO5 with 0.5 to 5 % w/w were prepared. Percutaneous absorption was tested with standard Franz Diffusion Cell equipment using full thickness rat skin. Drug concentrations in the samples were analyzed by High-Performance Liquid Chromatography (HPLC) equipped with UV-Vis detector at 305 nm. Results: The percutaneous absorption of flutamide emulgels formulated with enhancers was higher than control formulations. Enhancement ratio increased from 1.218 to 3.670 and 1.346 to3.900 for Precirol ATO5 and Transcutol P, respectively. Area under the Curve (AUC) increased by increase the enhancers’ concentration and a significant upsurge was seen in the concentration 1% for both enhancers. Conclusion: The flutamide emulgel containing 1% Transcutol P showed more appropriate percutaneous absorption through the skin compared to others.

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“…The stress tests reveal the intrinsic stability of the active ingredients and can be useful in developing a suitable formulation with satisfactory quality and shelf life [ 55 ]. Several accelerated stability tests have been suggested for the prediction of long-term stability, such as storage at elevated temperatures [ 56 ], under an accelerated or different type of light exposure [ 57 , 58 ], and under oxidative stress [ 55 , 59 ]. Honokiol is known to act as an antioxidant because of high radical-scavenging activities determined by the presence of two hydroxyl groups at the ortho - and para -positions [ 60 ].…”

Section: Discussionmentioning

confidence: 99%

Honokiol-Loaded Nanoemulsion for Glioblastoma Treatment: Statistical Optimization, Physicochemical Characterization, and an In Vitro Toxicity Assay

et al. 2023

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Background: Glioblastoma (GBM) is an extremely invasive and heterogenous malignant brain tumor. Despite advances in current anticancer therapy, treatment options for glioblastoma remain limited, and tumor recurrence is inevitable. Therefore, alternative therapies or new active compounds that can be used as adjuvant therapy are needed. This study aimed to develop, optimize, and characterize honokiol-loaded nanoemulsions intended for intravenous administration in glioblastoma therapy. Methods: Honokiol-loaded nanoemulsion was developed by incorporating honokiol into Lipofundin MCT/LCT 20% using a horizontal shaker. The Box–Behnken design, coupled with response surface methodology, was used to optimize the incorporation process. The effect of the developed formulation on glioblastoma cell viability was determined using the MTT test. Long-term and short-term stress tests were performed to evaluate the effect of honokiol on the stability of the oil-in-water system and the effect of different stress factors on the stability of honokiol, respectively. Its physicochemical properties, such as MDD, PDI, ZP, OSM, pH, and loading efficiency (LE%), were determined. Results: The optimized honokiol-loaded nanoemulsion was characterized by an MDD of 201.4 (0.7) nm with a PDI of 0.07 (0.02) and a ZP of −28.5 (0.9) mV. The LE% of honokiol was above 95%, and pH and OSM were sufficient for intravenous administration. The developed formulation was characterized by good stability and a satisfactory toxicity effect of the glioblastoma cell lines. Conclusions: The honokiol-loaded nanoemulsion is a promising pharmaceutical formulation for further development in the adjuvant therapy of glioblastoma.

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Comparative Stability of Two Anti-Hyperpigmentation Agents: Kojic Acid as a Natural Metabolite and Its Di-Palmitate Ester, Under Oxidative Stress; Application to Pharmaceutical Formulation Design

Cited by 4 publications

References 17 publications

Nanoemulsion Containing Kojic Dipalmitate and Rosehip Oil: A Promising Formulation to Treat Melasma

Nanoemulsion Containing Kojic Dipalmitate and Rosehip Oil: A Promising Formulation to Treat Melasma

Effects of Transcutol P and Precirol ATO-5 on Percutaneous Absorption of Flutamide from Emulgels

Honokiol-Loaded Nanoemulsion for Glioblastoma Treatment: Statistical Optimization, Physicochemical Characterization, and an In Vitro Toxicity Assay

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