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Brucks, Richard; Nanavaty, Maulik; Jung, Donald; Siegel, Frederick P.

doi:10.1023/a:1015938522673

Cited by 48 publications

(7 citation statements)

References 7 publications

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“…Synthesis of Lactam N-Acetic Acid EsterssThe 5-and 6-membered lactams (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14) were prepared with acetate esters at the 1-position (Table 1). The bromoacetate esters were prepared by reaction of the appropriate alcohol with bromoacetyl bromide, and this crude bromoacetate ester was used to alkylate the sodium salt of the various lactams.…”

Section: Methodsmentioning

confidence: 99%

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Synthesis and in Vitro Transdermal Penetration Enhancing Activity of Lactam N-Acetic Acid Esters

Michniak¹,

Player²,

Sowell³

1996

Journal of Pharmaceutical Sciences

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A homologous series of N-acetic acid esters of 2-pyrrolidinone and 2-piperidinone has been prepared and evaluated for its ability to enhance the skin content and flux of hydrocortisone 21-acetate in hairless mouse skin in vitro. Enhancement ratios (ER) were determined for flux (J), 24-hour diffusion cell receptor cell concentrations (Q24), and 24-h full-thickness mouse skin steroid content (SC) and compared to control values (no enhancer present). In addition, in an attempt to abrogate toxicity, these dermal penetration enhancers were designed to have the potential for biodegradation by dermal esterases. 2-Oxopyrrolidine-alpha acetic acid dodecyl ester (5) showed the highest enhancement ratios for J (ER 67.33) and Q24 (ER 180.66). 2-Oxopiperidine-alpha-acetic acid decyl ester (10) showed a high Q24 (ER 162.07) but a lower J (ER 12.67). 2-Oxopyrrolidine-alpha-acetic acid decyl ester (3) showed the highest enhancement ratio for SC (ER 8.7). The ER Q24 for 3, 5 and 10, as well as other lactam N-acetic acid esters in this work, were significantly higher than the ER found using Azone as enhancer.

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Section: Methodsmentioning

confidence: 99%

“…Many methods have been used to decrease skin resistance to the passage of drugs. These include the prodrug approach, 2 iontophoresis, 3 phonophoresis, 4 and dermal penetration enhancers. 5 This last approach is most convenient; however, these compounds must be highly effective, show no irritancy or toxicity, and be stable and pharmacologically inert.…”

mentioning

confidence: 99%

Synthesis and in Vitro Transdermal Penetration Enhancing Activity of Lactam N-Acetic Acid Esters

Michniak¹,

Player²,

Sowell³

1996

Journal of Pharmaceutical Sciences

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“…[11] Simonin also demonstrated, using a theoretical analysis, that convective reduction of the boundary layer above the skin by stirring of the donor compartment could decrease the overall resistance of the membrane by about 10%. [68] Convection has also been cited as a possible mechanism in other HFS studies,[91] while it has not been implicated in several others. [6, 12, 92, 93]…”

Section: Mechanisms Of Skin Permeability Enhancement In Sonophoresismentioning

confidence: 99%

“…[5, 11, 92] Conversely, and not surprisingly, in studies that observed much larger temperature increases (in excess of 10 °C), thermal effects were found to play a role in increasing permeant transport, although a temperature increase alone could not explain the full enhancement observed with the HFS treatment (1 MHz, 1 W/cm 2 ). [91] Meidan et al even concluded that heating is the main mechanism of action with HFS. [87] A study of sonophoresis, at an intermediate frequency of 150 kHz (2 W/cm 2 ), also concluded that thermal effects may be a significant mechanism of increased flux of hydrophilic permeants.…”

Section: Mechanisms Of Skin Permeability Enhancement In Sonophoresismentioning

confidence: 99%

Ultrasound-mediated transdermal drug delivery: Mechanisms, scope, and emerging trends

Polat

Hart

Langer

et al. 2011

Journal of Controlled Release

357

290

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The use of ultrasound for the delivery of drugs to, or through, the skin is commonly known as sonophoresis or phonophoresis. The use of therapeutic and high frequencies of ultrasound (≥ 0.7 MHz) for sonophoresis (HFS) dates back to as early as the 1950s, while low-frequency sonophoresis (LFS, 20 – 100 kHz) has only been investigated significantly during the past two decades. Although HFS and LFS are similar because they both utilize ultrasound to increase the skin penetration of permeants, the mechanisms associated with each physical enhancer are different. Specifically, the location of cavitation and the extent to which each process can increase skin permeability are quite dissimilar. Although the applications of both technologies are different, they each have strengths that could allow them to improve current methods of local, regional, and systemic drug delivery. In this review, we will discuss the mechanisms associated with both HFS and LFS, specifically concentrating on the key mechanistic differences between these two skin treatment methods. Background on the relevant physics associated with ultrasound transmitted through aqueous media will also be discussed, along with implications of these phenomena on sonophoresis. Finally, a thorough review of the literature is included, dating back to the first published reports of sonophoresis, including a discussion of emerging trends in the field.

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“…Phonophoresis is the use of ultrasound to enhance percutaneous absorption of a drug (15)(16)(17)(18). Phonophoresis provides an advantage as it bypasses the hepatic first-pass metabolism and avoids the side effects in absorption that occur with oral administration (18)(19)(20).…”

Section: Introductionmentioning

confidence: 99%

Comparison of the Efficacy of Phonophoresis and Conventional Ultrasound Therapy in Patients with Primary Knee Osteoarthritis

Oktayoglu¹,

Gür²,

Yardımeden³

et al. 2014

Erciyes Med J

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Objective: To compare the efficacy of phonophoresis (PH) versus ultrasound (US) in patients with primary knee osteoarthritis (OA). Materials and Methods: Forty patients were divided into two groups as PH and US. Acoustic gel containing no pharmacological agent was applied in the US group, whereas a gel containing 1.16% diclofenac diethylamonium was applied in the PH group for 10 sessions. The Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) pain subscale and Visual Analogue Scale (VAS) were used for the assessment of pain. The WOMAC physical function subscale, Lequesne functional index and Stanford Health Assessment Questionnaire (HAQ) were used for the assessment of physical activities. Patients were assessed for a 3 month follow-up period. Results: In the PH group, painless walking duration improved at all follow-up times except for week 2 (p<0.05). Painless walking distance and VAS scores also improved at all follow-up times (p<0.05). In the US group, VAS scores during walking and flexion of the knee, WOMAC pain and physical function scores and total WOMAC scores improved significantly at all follow-up times (p<0.05). Conclusion: Both therapeutic modalities were found effective. We suggest neither therapy is superior to the other but PH can improve painless walking duration more successfully than US.

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Untitled

Cited by 48 publications

References 7 publications

Synthesis and in Vitro Transdermal Penetration Enhancing Activity of Lactam N-Acetic Acid Esters

Synthesis and in Vitro Transdermal Penetration Enhancing Activity of Lactam N-Acetic Acid Esters

Ultrasound-mediated transdermal drug delivery: Mechanisms, scope, and emerging trends

Comparison of the Efficacy of Phonophoresis and Conventional Ultrasound Therapy in Patients with Primary Knee Osteoarthritis

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