Valproic Acid and Sodium Valproate: Comprehensive Profile

Alsarra, Ibrahim A.; Al-Omar, Mohamed A.; Belal, F.

doi:10.1016/s0099-5428(05)32008-9

Cited by 26 publications

(11 citation statements)

References 56 publications

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“…The FTIR spectrum of SV exhibited characteristic vibrations in the region of 2937–2848 cm −1 associated with aliphatic C-H stretching. The vibrational peaks detected at 1544–1404 cm −1 were attributed to COO- stretching, respectively [ 63 , 64 ].…”

Section: Resultsmentioning

confidence: 99%

“…DSC thermograms of SV, Span 60, Cremophor RH, plain spanlastics and the optimized spanlastic formula are illustrated in Figure 8 . The DSC thermogram of SV showed a characteristic endothermic peak at 99.3 °C which revealed the crystallinity of SV [ 63 , 64 , 67 ]. The DSC thermogram of Span 60 exhibited an endothermic peak at 54.4 °C that corresponds to its transition temperature [ 68 ].…”

Section: Resultsmentioning

confidence: 99%

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Formulation of Sodium Valproate Nanospanlastics as a Promising Approach for Drug Repurposing in the Treatment of Androgenic Alopecia

et al. 2020

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Sodium valproate (SV) is an antiepileptic drug that is widely used in the treatment of ‎different seizure disorders. The topical SV has a hair regenerative potential through activating the Wnt/β-catenin pathway and anagen phase induction‎. The aim of the current investigation was to fabricate nanospanlastics of SV for improving its dermal delivery by providing ‎prolonged drug effect and increasing its permeability ‎for treatment of androgenic alopecia (AGA). SV-loaded nanospanlastics were formulated according to 23 factorial design by ethanol injection method using a non-ionic surfactant (Span 60) and edge activators (EAs), such as Tween 80 and Cremophor RH 40, to explore the influence of different independent variables on entrapment efficiency (EE%) and percentage drug released after 12 h (Q12h) in order to choose the optimized formula using Design-Expert software. The optimized formula (F8) appeared as spherical deformable vesicles with EE% of 90.32 ± 2.18% and Q12h of 90.27 ± 1.98%. F8 exhibited significant improvement of ex vivo permeation than free SV. The clinical study exhibited no comparable difference between F8 and marketed minoxidil lotion. However, F8 demonstrates less adverse effects than minoxidil lotion. Nanospanlastics could be a safe and effective method for improving the topical delivery of SV in the management of AGA.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Formulation of Sodium Valproate Nanospanlastics as a Promising Approach for Drug Repurposing in the Treatment of Androgenic Alopecia

et al. 2020

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“…Thus, we might obtain a higher or similar level of cell inhibition in melanoma cells with 48 h pretreatment, while 12 h pretreatment might result in less efficacy in terms of potential temporal effects. In addition, we administrated VPA once in the ETO→VPA sequential combined treatment since VPA is stable in solution under 40 °C [ 20 ]. We, therefore, considered there would be a negligible difference in efficacy when VPA is given at regular intervals.…”

Section: Discussionmentioning

confidence: 99%

Synergistic Effect of Simultaneous versus Sequential Combined Treatment of Histone Deacetylase Inhibitor Valproic Acid with Etoposide on Melanoma Cells

Shyu

Liu

Chuang

2021

IJMS

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Melanoma is the most lethal form of skin cancer, which is intrinsically resistant to conventional chemotherapy. Combination therapy has been developed to overcome this challenge and show synergistic anticancer effects on melanoma. Notably, the histone deacetylase inhibitor, valproic acid (VPA), has been indicated as a potential sensitizer of chemotherapy drugs on various metastatic cancers, including advanced melanoma. In this study, we explored whether VPA could serve as an effective sensitizer of chemotherapy drug etoposide (ETO) on B16-F10 and SK-MEL-2-Luc melanoma cell lines in response to drug-induced DNA damages. Our results demonstrated that the VPA-ETO simultaneous combined treatment and ETO pretreated sequential combined treatment generated higher inhibitory effectivities than the individual treatment of each drug. We found the VPA-ETO simultaneous combined treatment contributed to the synergistic inhibitory effect by the augmented DNA double-strand breaks, accompanied by a compromised homologous recombination activity. In comparison, the ETO pretreated sequential combined treatment led to synergistic inhibitory effect via enhanced apoptosis. Surprisingly, the enhanced homologous recombination activity and G2/M phase arrest resulted in the antagonistic effect in both cells under VPA pretreated sequential combined treatment. In summary, our findings suggested that sequential order and effective dose of drug administration in VPA-ETO combination therapy could induce different cellular responses in melanoma cells. Such understanding might help potentiate the effectiveness of melanoma treatment and highlight the importance of sequential order and effective dose in combination therapy.

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“…During the second phase, the evaporation rate decreases; this can be attributed to the dissolution of sodium valproate in valproic acid as the solubility of sodium valproate might increase with temperature, which increases the viscosity of the solution, or due to the precipitation of sodium valproate that was dissolved in valproic acid, which forms a physical barrier for evaporation. During the third phase (around 290 C), the evaporation rate of valproic acid increases since at such a high temperature, which greatly exceeds the boiling point of valproic acid (219.5 C) (Alsarra et al 2005), the valproic acid molecules acquire enough energy much to overcome any physical interaction with sodium valproate. The residue at the end of the thermogravimetric analysis was observed to dissolve rapidly in water indicating the presence of residual sodium valproate since it is readily soluble in water.…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

“…Valproic acid is clear, colorless to pale yellow, slightly viscous liquid, and sparingly soluble in water, whereas sodium valproate is a white crystalline, hygroscopic, and highly soluble in water and alcohol (Alsarra et al 2005). It was noticed that on the addition of divalproex sodium to water, the coordination complex readily dissociates into sodium valproate and valproic acid.…”

Section: Introductionmentioning

confidence: 99%

On the plasticizing properties of divalproex sodium: physicochemical and spectroscopic characterization studies

Khatri

Desai

Minko

2018

Pharmaceutical Development and Technology

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The objective of the research was to demonstrate the plasticization properties of divalproex sodium, due to its component-valproic acid, on ethyl cellulose, which could prove beneficial for film fabrications or hot melt extrusion based formulations. Films containing 10-50% w/w (DVS/EC) as dry weight were prepared using solvent evaporation method and characterized using texture analyzer, hybrid rheometer, differential scanning calorimetry, thermogravimetry, X-ray diffractometry, polarized microscopy, FTIR, and Raman spectroscopy. It was found that there was a decrease in average peak load, melt viscosity, and glass transition temperature (T g) while increase in elongation, with increase in concentration of DVS in the films. These results demonstrate the plasticization tendency of DVS on EC, which was attributed to the presence of valproic acid (fatty acid) in DVS. XRD studies showed amorphous nature of the films; however, polarized microscopy revealed the presence of scattered undissolved sodium valproate crystals. The presence of a single T g established complete miscibility between valproic acid and EC. Films showed reasonable physical stability (similar T g) at 45 C/75% RH for 2 weeks (open condition), attributable to the similar solubility parameters of DVS and EC. FTIR and Raman spectroscopy results proved the presence of hydrogen bonding between DVS and EC.

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Valproic Acid and Sodium Valproate: Comprehensive Profile

Cited by 26 publications

References 56 publications

Formulation of Sodium Valproate Nanospanlastics as a Promising Approach for Drug Repurposing in the Treatment of Androgenic Alopecia

Formulation of Sodium Valproate Nanospanlastics as a Promising Approach for Drug Repurposing in the Treatment of Androgenic Alopecia

Synergistic Effect of Simultaneous versus Sequential Combined Treatment of Histone Deacetylase Inhibitor Valproic Acid with Etoposide on Melanoma Cells

On the plasticizing properties of divalproex sodium: physicochemical and spectroscopic characterization studies

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