The effects of electrically assisted methods on transdermal delivery of nalbuphine benzoate and sebacoyl dinalbuphine ester from solutions and hydrogels

Huang, Jeng Fen; Sung, K. C.; Hu, Oliver Yoa Pu; Wang, Jhi Joung; Lin, Yi; Fang, Jia You

doi:10.1016/j.ijpharm.2005.03.015

Cited by 14 publications

(14 citation statements)

References 21 publications

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“…At the level of saturation, concentration of VH was so high that the solution turned viscous. As high viscosity hinders the movement of ions this might also be a contributing factor in reducing the permeation rate (38).…”

Section: Resultsmentioning

confidence: 99%

Screening of Venlafaxine Hydrochloride for Transdermal Delivery: Passive Diffusion and Iontophoresis

Singh

Ghosh²,

Dave³

et al. 2008

AAPS PharmSciTech

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Abstract. The objective of the study was to investigate in vitro transdermal delivery of venlafaxine hydrochloride across the pigskin by passive diffusion and iontophoresis. For passive diffusion, experiments were carried out in Franz diffusion cell whereas for iontophoretic permeation, the diffusion cell was modified to contain both the donor and return electrode on the same side of skin. Anodal iontophoresis was carried out using a current density of 0.5 mA/cm 2 . Donor concentrations used were 585.5 mg/ml (saturated solution) and 100 mg/ml. Experiments initially performed to determine the transport efficiency of venlafaxine ions showed promising results. Iontophoresis increased the permeation rate at both concentration levels over their passive counterparts (P<0.01), but surprisingly higher steadystate flux was obtained from lower donor drug load (P<0.01). The favorable pH of the unsaturated solutions is suggested to be the cause for this effect. Mild synergistic effect was observed when iontophoresis was carried out incorporating peppermint oil in the donor but the same was not found in passive diffusion. Highest steady-state flux obtained in the experiment was 3.279 μmol/cm 2 /h when peppermint oil (0.1%) was included in the donor. As the maintenance requirement of venlafaxine hydrochloride is approximately 9.956 μmol/h, the results suggested that the drug is a promising candidate for iontophoretic delivery.

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Section: Resultsmentioning

confidence: 99%

Screening of Venlafaxine Hydrochloride for Transdermal Delivery: Passive Diffusion and Iontophoresis

Singh

Ghosh²,

Dave³

et al. 2008

AAPS PharmSciTech

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“…The second driving force possibly comes from the expansion of the matrix PAAM hydrogel pore size from 4.18 ± 1.30 m (E = 0 V) to 9.3 ± 4.8 m (E = 0.1 V), as visualized in Figures 1(c) and (d), respectively. In addition, the electric field can increase the permeation of the hydrophilic drug, SA, through the liophilic stratum corneum in the pigskin by the creation of transient micropores in the skin which provide the transport pathway of the drug (Gusbeth & Weaver, 2000;Murdan, 2003;Huang et al, 2005). Figure 7 were fitted to equation (6) and the scaling exponent n of cross-linked PAAM (PAAM_0.016) was determined to be n ≈ 0.34-0.54.…”

Section: Effect Of Electric Field Strengthmentioning

confidence: 99%

“…When an electric field is applied to an aqueous medium, the electrolysis in the buffer solution produces positive and negative buffer ions. The negative buffer ions are generated at cathode electrode, resulting in the deprotonation and the neutralization of positive charged groups on the PAAM and consequently gel de-swelling at cathode (Gusbeth & Weaver, 2000;Huang et al, 2005). Tanaka et al (1982) also reported that the de-swelling of partially hydrolyzed PAAM hydrogel occurred continuously along the gel axis when an electric field of 1.25 V was applied, and the de-swelling increased with voltage.…”

Section: Data Ofmentioning

confidence: 99%

Electric field assisted transdermal drug delivery from salicylic acid-loaded polyacrylamide hydrogels

Niamlang

Sirivat

2009

Drug Delivery

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“…In order to maintain the blood nalbuphine concentration to improve the patient compliance and therapeutic effectiveness in pain management, nalbuphine prodrugs had been synthesized for transdermal aims (Fig. (6)) [40][41][42][43]. Nalbuphine prodrugs were synthesized by using the method reported previously [44].…”

Section: Nalbuphinementioning

confidence: 99%

“…Besides the straight-chain prodrugs, nalbuphine benzoate and sebacoyl dinalbuphine ester were designed to perform the in vitro skin absorption for delivering nalbuphine [43]. The passive permeation studies demonstrated that nalbuphine benzoate had higher permeation rates than the parent drug.…”

Section: Nalbuphinementioning

confidence: 99%

Prodrug Strategy for Enhancing Drug Delivery via Skin

Fang¹,

Leu²

2006

CDDT

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Skin as a route for drug delivery has been extensively investigated. However, because of the predominant barrier function of stratum corneum in skin, the clinical application is limited. One strategy to solve this problem of drug permeation via skin is the use of prodrugs. Prodrugs are inactive compounds which are metabolized either chemically or enzymatically in a controlled or predictable manner to its parent active drug. Prodrugs can enhance dermal/transdermal drug delivery via different mechanisms, including increased skin partitioning, increased aqueous solubility, and reduced crystallization, etc. Besides the prodrug itself, the optimization of vehicle is important as well. The prodrug partitioning between skin and vehicle as well as prodrug-vehicle interaction may influence the enhancing efficacy on skin permeation. This review explores the synthesis and enhancing mechanisms of prodrugs for topical drug delivery. The prodrugs categorized by the therapeutic use of the parent drugs, including anticancer drugs, analgesics, anti-inflammatory drugs and vitamins, are systemically introduced in this review.

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The effects of electrically assisted methods on transdermal delivery of nalbuphine benzoate and sebacoyl dinalbuphine ester from solutions and hydrogels

Cited by 14 publications

References 21 publications

Screening of Venlafaxine Hydrochloride for Transdermal Delivery: Passive Diffusion and Iontophoresis

Screening of Venlafaxine Hydrochloride for Transdermal Delivery: Passive Diffusion and Iontophoresis

Electric field assisted transdermal drug delivery from salicylic acid-loaded polyacrylamide hydrogels

Prodrug Strategy for Enhancing Drug Delivery via Skin

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