Study on Mixed Solvency Concept in Formulation Development of Aqueous Injection of Poorly Water Soluble Drug

Solanki, Shailendra Singh; Soni, Love Kumar; Maheshwari, R. K.

doi:10.1155/2013/678132

Cited by 14 publications

(37 citation statements)

References 11 publications

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“…Solubility was determined in triplicate. [17][18][19][20] Figure 5]. Drug was estimated spectrophotometrically in mixed solvent system and distilled water to observe any interference between drug and excipients by taking respective reagents blank at appropriate wavelength during study.…”

Section: Solubility Determinationmentioning

confidence: 99%

“…The aseptic room was fumigated using a mixture of 40% formaldehyde and potassium permanganate and the UV lights were switched on for 30 min before formulation of injections and the filling of injections into vials. [17][18][19][20] …”

Section: Preparation Of Aseptic Areamentioning

confidence: 99%

“…Finally, the stoppers were rinsed with freshly prepared sterile distilled water and dried in vacuum oven under aseptic condition. [18][19][20] …”

Section: Treatment Of Packing Materialsmentioning

confidence: 99%

“…The solutions were analyzed spectrophotometrically at 274 nm for drug content after appropriate dilutions with distilled water using the same vehicle as blank after appropriate dilution. [17][18][19][20] Aseptic filtration and packaging…”

Section: Preparation Of Aqueous Injectionmentioning

confidence: 99%

“…Therefore, the authors have proposed a mixed-solvency approach for poorly water-soluble drugs. [17][18][19][20] In this research, aceclofenac was used as model drug (poorly water soluble drug), it is white crystalline powder, practically insoluble in water, freely soluble in acetone, soluble in ethanol (96%) [ Figure 1]. [21] The solubilization power of the cosolvents, two solid solubilizers, i.e., urea and sodium citrate system and mixed solvent system were evaluated.…”

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Solanki

2017

AJP

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Context: Water solubility is an important molecular property for successful drug development as it is a key factor governing drug access to biological membranes. The solubilization of poorly water soluble drug by facilitated mixed solvency is presented. Aim: The aim was to develop the injection formulations of the model poorly water-soluble drug. Settings and Design: Trial and error based experimental study. Materials and Methods: Mixed solvency approach was used to solubilize the hydrophobic drug. Mixed solvent system prepared using water-soluble hydrotropes (such as sodium citrate and urea) and water-miscible cosolvents, such as polyethylene glycol (PEG) 200, PEG 300, PEG 400, PEG 600, glycerin, propylene glycol, and ethanol. Drug was characterized using ultraviolet, Fourier Transform infrared (FT-IR), and Raman spectroscopy. Solubilizing power (Φ) and the Gibbs free energy of transfer (ΔG 0 tr) were determined. Various properties of solution such as pH, viscosity, specific gravity, and refractive index were also studied. Results: Desired solubility of drug achieved in a mixed solvent blend AF5, which was more than 200 fold as compared to the solubility in distilled water 0.152 mg/ml. Drug content was found to be more than 98%. FT-IR and Raman spectroscopy results may support intermolecular hydrogen bonding between drug and mixed solvent system. Developed formulation was physically and chemically stable. Conclusion: This technique proved a synergistic enhancement in solubility of a poorly water soluble drug due to mixed solvent effect and produces a stable formulation. Mixed solvency concept may reduce the individual concentration of solubilizers and so reduce their toxicity associated with them.

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Section: Solubility Determinationmentioning

confidence: 99%

Section: Preparation Of Aseptic Areamentioning

confidence: 99%

“…Finally, the stoppers were rinsed with freshly prepared sterile distilled water and dried in vacuum oven under aseptic condition. [18][19][20] …”

Section: Treatment Of Packing Materialsmentioning

confidence: 99%

Section: Preparation Of Aqueous Injectionmentioning

confidence: 99%

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2017

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7-formyl-10-methylisoellipticine, a novel ellipticine derivative, induces mitochondrial reactive oxygen species (ROS) and shows anti-leukaemic activity in mice

et al. 2015

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Acute myeloid leukaemia (AML) is the most common type of leukaemia in adults and is associated with high relapse rates. Current treatment options have made significant progress but the 5 year survival for AML remains low and therefore, there is an urgent need to develop novel therapeutics. Ellipticines, a class of cancer chemotherapeutic agents, have had limited success clinically due to low solubility and toxic side effects. Isoellipticines, novel isomers of ellipticine, have been designed to overcome these limitations. One particular isoellipticine, 7-formyl-10-methylisoellipticine, has previously showed strong ability to inhibit the growth of leukaemia cell lines. In this study the anti-leukaemia effect of this compound was investigated in detail on an AML cell line, MV4-11. Over a period of 24 h 7-formyl-10-methyl isoellipticine at a concentration of 5 μM can kill up to 40 % of MV4-11 cells. Our research suggests that the cytotoxicity of 7-formyl-10-methylisoellipticine is partially mediated by an induction of mitochondrial reactive oxygen species (ROS). Furthermore, 7-formyl-10-methylisoellipticine demonstrated promising anti-tumour activity in an AML xenograft mouse model without causing toxicity, implying the potential of isoellipticines as novel chemotherapeutic agents in the treatment of leukaemia.

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