Review of Pharmaceutical Applications of N-Methyl-2-Pyrrolidone

Jouyban, Abolghasem; Fakhree, Mohammad Amin Abolghassemi; Shayanfar, Ali

doi:10.18433/j3p306

Cited by 160 publications

(126 citation statements)

References 66 publications

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“…This can be explained by the physicochemical characteristics of n-methyl-pyrrolidone, which contains a nonpolar carbon that can weaken the structure of hydrogen bonding in water, allowing it to act also as a cosolvent, thereby increasing drug solubilization. 24 Incorporation of the drug in the formulations did not alter the nanometric size, with a uniform distribution of droplet sizes being maintained (Table 2). Table 3 shows the physicochemical characteristics of the study formulations and verifies the structural changes resulting from the different incorporation processes.…”

Section: Resultsmentioning

confidence: 96%

“…23 Further, n-methyl-pyrrolidone is used as a solubilizing agent in pharmaceutical formulations for oral and parenteral use and as a penetration enhancer for lipophilic drugs. 24 These characteristics make n-methyl-pyrrolidone an ideal candidate, and recently they have been exploited in applications testing the efficacy of n-methyl-pyrrolidone in transdermal nanosystems containing granisetron hydrochloride, 25 and in formulations designed for topical use, such as lidocaine, 26 estradiol, 27 bupranolol, 28 and insulin. 29 In formulations intended for topical administration, the aqueous phase and surfactants affect skin permeability by hydration of the stratum corneum and breakdown of the lipoprotein matrix, resulting in decreased resistance to drug diffusion.…”

Section: Resultsmentioning

confidence: 99%

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Nanoemulsion containing dapsone for topical administration: a study of in vitro release and epidermal permeation

Borges¹,

Simon²,

Sena³

et al. 2013

IJN

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Background: Topical administration of dapsone can be an alternative route for treatment of leprosy and can also provide new therapeutic applications for an established drug. However, the physicochemical properties of dapsone make it difficult to incorporate into conventional formulations. The current study was directed toward developing a stable nanoemulsion that contains dapsone which can be adapted for topical use. Methods: Nanoemulsions were prepared using isopropyl myristate or n-methyl-pyrrolidone as the oil phase, and characterized according to their mean droplet size, conductivity, refractive index, pH, drug content, and stability. The in vitro release of dapsone and its ability to permeate the epidermis were also evaluated. Results: Physicochemical characterization demonstrated that nanosystems were formed, which had a uniform droplet distribution and a pH compatible with the skin surface. Use of n-methyl-pyrrolidone provided a greater nanoemulsion region and higher solubilization of dapsone, and increased the in vitro release rate when compared with a nanoemulsion prepared using isopropyl myristate. However, use of isopropyl myristate promoted an increase in in vitro epidermal permeation that followed the Higuchi model. This demonstrates the ability of a nanosystem to influence permeation of dapsone through the skin barrier. Furthermore, the nanoemulsions developed and evaluated here had ideal physicochemical stability over a 3-month period. Conclusion: Incorporation of dapsone into a nanoemulsion may be a promising system for enabling topical delivery of dapsone, while minimizing skin permeation, for the treatment of acne. The method developed here used isopropyl myristate as the oil phase, and promoted permeation of dapsone through the skin barrier for the treatment of leprosy upon use of n-methylpyrrolidone as the oil phase.

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Section: Resultsmentioning

confidence: 96%

Section: Resultsmentioning

confidence: 99%

Nanoemulsion containing dapsone for topical administration: a study of in vitro release and epidermal permeation

Borges¹,

Simon²,

Sena³

et al. 2013

IJN

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show abstract

“…Die Substanz ist hygroskopisch, vollständig mit Wasser mischbar und in den meisten anderen Lösemitteln lös-lich [3]. NMP ist beständig gegen Wasser und wird an der Luft nur langsam oxidiert [1,4]. Natürliche Vorkommen von NMP sind nicht bekannt [3].…”

Section: Stoffeigenschaften Und Anwendungunclassified

“…Eine Exposition am Arbeitsplatz oder auch in der Allgemeinbevölkerung kann sich aus der Verwendung als Lösemittel zum Entfernen von Farben und Graffiti ergeben, in Innenräumen aus dem Einsatz in Farben und Tinten sowie in Auslegeware und Teppichen. Schließlich wird NMP auch in Kosmetika als Lösemittel und oberflächenaktive Substanz und in manchen Pharmazeutika als Lösevermitt-ler verwendet [1,4,5].…”

Section: Stoffeigenschaften Und Anwendungunclassified

Richtwerte für 1-Methyl-2-pyrrolidon in der Innenraumluft

Umweltbundesamtes¹

2014

Bundesgesundheitsbl.

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“…cosolvency, is the most common and feasible technique to enhance the aqueous solubility of drugs. The common cosolvents which, are used in the pharmaceutical industry are ethanol, propylene glycol, glycerine, glycofural, polyethylene glycols (mainly 200, 300 and 400), N,N-dimethyl acetamide, dimethyl sulfoxide, 2-propanol, dimethyl isosorbide, N-methyl 2-pyrrolidone (NMP) and room temperature ionic liquids (Rubino, 1990;Mizucci et al, 2008;Jouyban et al, 2010a). Their applications and possible side effects have been discussed in the literature (Spiegel and Noseworthy, 1963;Tsai et al, 1986;Patel et al, 1986;Golightly et al, 1988;Rubino, 1990).…”

Section: Solubility Increasingmentioning

confidence: 99%