Application of hydrotropy to transdermal formulations: hydrotropic solubilization of polyol fatty acid monoesters in water and enhancement effect on skin permeation of 5-FU

Takahashi, Kyoko; Komai, Megumi; Kinoshita, Natsumi; Nakamura, Emi; Hou, Xiao-Long; Takatani‐Nakase, Tomoka; Kawase, Masaya

doi:10.1111/j.2042-7158.2011.01308.x

Cited by 11 publications

(9 citation statements)

References 20 publications

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“…It is required >30% NaSal to dissolve PGMC in the HEL solution [22]. To determine effect of low dose NaSal on TCI, PGMC was completely dissolved in the HEL solution with the addition of other hydrotropic agent, NaBen, which does not induce immune response in <$>\raster="<$>≦ 58% (w/v) of NaBen as shown in Fig.…”

Section: Methodsmentioning

confidence: 99%

“…g ., propylene glycol and ethanol). These results suggest that the hydrotropic formulation of PGMC is potentially useful for transdermal administration of water-soluble drugs [22]. This prompted us to further use a hydrotropic formulation of PGMC in the development of effective TCI systems.…”

Section: Introductionmentioning

confidence: 99%

“…Previously, we developed transdermal formulations using the hydrotropic phenomenon without pretreatment or disruption of the skin [22]. Hydrotropy refers to increasing the solubility of poorly water-soluble drugs by the addition of hydrotropic salts, such as urea, caffeine, nicotinamide, sodium benzoate (NaBen), and sodium salicylate (NaSal) [23]–[26].…”

Section: Introductionmentioning

confidence: 99%

“…Hydrotropy refers to increasing the solubility of poorly water-soluble drugs by the addition of hydrotropic salts, such as urea, caffeine, nicotinamide, sodium benzoate (NaBen), and sodium salicylate (NaSal) [23]–[26]. We have found that polyol fatty acid esters (POFE) act as absorption enhancers and enable solubilization in water in the presence of hydrotropic agents, which is caused by a change in the interaction between water molecules and the aggregation of hydrotropic salts with POFE [22]. Moreover, we also reported that the hydrotropic formulation of propylene glycol monocaprylate (PGMC), a monoester of polyol fatty acid, and 5-fluorouracil (5-FU), which is an example of a hydrosoluble substance, significantly enhanced the skin penetration of 5-FU as compared with other formulations ( e .…”

Section: Introductionmentioning

confidence: 99%

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Transcutaneous Immunization System Using a Hydrotropic Formulation Induces a Potent Antigen-Specific Antibody Response

et al. 2012

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BackgroundTranscutaneous immunization (TCI) is a novel vaccination strategy, which is expected to have therapeutic applications. However, to develop effective TCI systems, a simple, non-invasive and safe transdermal formulation is required. This study developed a novel TCI system utilizing the co-administration of a liposoluble absorption enhancer, propylene glycol monocaprylate (PGMC) and hydrosoluble protein antigen without pretreatment of any typical adjuvants and disruption of the skin. Novel transdermal formulations were also prepared with sodium salicylate (NaSal) as a hydrotropic agent to improve the solubility of poorly water-soluble substances.Methodology/Principal FindingsThe TCI system, which used a transdermal formulation containing hen lysozyme (HEL) and PGMC, solubilized with NaSal, resulted in a substantial HEL-specific antibody response in an HEL dose-dependent manner even in the absence of potent adjuvants, such as cholera toxin (CT). We also investigated whether NaSal activates antigen-presenting cells in vitro to clarify the mechanisms of antibody production by the hydrotropic formulation. NaSal enhanced the expression of MHC class II molecules and increased the production of IL-12 and TNF-α in dendritic cells, which were stimulated by lipopolysaccharide in vitro, indicating that NaSal had an effective adjuvant-like property. Moreover, the use of NaSal in the TCI system did not induce an HEL-specific, IgE-dependent anaphylactic reaction.Conclusion/SignificanceOur TCI system using a hydrotropic formulation effectively and safely induced the intended immune response, and this system thus represents a new advantageous method that will result in improved TCI strategies.

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Transcutaneous Immunization System Using a Hydrotropic Formulation Induces a Potent Antigen-Specific Antibody Response

et al. 2012

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“…The mean particle size of the solution consisting of PGMC was approximately 14 nm. The hydrotropic transdermal formulation enhanced skin permeation of 5-Fu due to the ability of the hydrotrope to form aggregates 68 .…”

Section: Hydrotropes As Drug Carriersmentioning

confidence: 99%

Untitled

2019

IJPSR

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Drug discovery and development plays a major role in the world and serves mankind. The major criteria to be considered and given importance in drug development is the solubility of a drug. Among all newly discovered chemical entities, about 40% of drugs fail to reach the market due to their poor aqueous solubility or lipophilicity. Poor solubility is not only a problem for formulation development and clinical testing but also an obstacle at the very beginning while screening new compounds for pharmacological activity. Nowadays oral route is considered as the preferred route of drug administration than other routes due to its convenience in terms of ease of administration and economy. The first requirement of drug which is supposed to be given by oral route is good aqueous solubility, as the poor solubility leads to low absorption, inadequate and variable bioavailability and also gastrointestinal mucosal toxicity. To prevent these crisis, several solubility enhancement techniques have been employed to enhance the solubility of poorly soluble drugs and hydrotropic solubilization is one of them. Besides, the advantage of certain properties like high selectivity, non-inflammability, environmentally friendly, easy availability and cost-effectiveness of hydrotropes makes this technique superior to other solubilization techniques. In the present review, an attempt has been made to discuss the hydrotropic solubilization technique and highlight the applications with this approach.

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Correlation of hydrotropic solubilization by urea with logD of drug molecules and utilization of this effect for topical formulations

Herbig

Evers

2013

European Journal of Pharmaceutics and Biopharmaceutics

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Application of hydrotropy to transdermal formulations: hydrotropic solubilization of polyol fatty acid monoesters in water and enhancement effect on skin permeation of 5-FU

Cited by 11 publications

References 20 publications

Transcutaneous Immunization System Using a Hydrotropic Formulation Induces a Potent Antigen-Specific Antibody Response

Transcutaneous Immunization System Using a Hydrotropic Formulation Induces a Potent Antigen-Specific Antibody Response

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Correlation of hydrotropic solubilization by urea with logD of drug molecules and utilization of this effect for topical formulations

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