Iontophoresis-Facilitated Delivery of Prednisolone through Throat Skin to the Trachea After Topical Application of its Succinate Salt

Ishii, Hiroshi; Suzuki, Takahiro; Todo, Hiroaki; Kamimura, Mitsuhiro; Sugibayashi, Kenji

doi:10.1007/s11095-010-0337-x

Cited by 6 publications

(3 citation statements)

References 29 publications

(27 reference statements)

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“…In a rat model it was about 8 mm depth for lipophilic steroids (hydrocortisone, fluocinolone acetonide) [15] and 3-4 mm depth for non-steroidal anti-inflammatory drugs [16]. Also, in the rat model, a steroid prodrug (prednisolone sodium succinate) topically applied to the skin over the trachea caused a higher prednisolone concentration at the trachea than in plasma, and the use of iontophoresis resulted in a 12-fold higher prednisolone concentration at the trachea [17].…”

Section: Discussionmentioning

confidence: 99%

Transdermal Application of Steroid to Cervical Trachea for the Cough in Patients with Bronchial Asthma and Cough Variant Asthma-A Pilot Study

Mouri¹,

Mizutani²

2013

J Allergy Ther

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Background: The delivery of steroid to asthmatic patients has been limited to inhalation therapy or systemic therapy. The objective of this study was to evaluate the efficacy of transcutaneous application of steroid over the cervical trachea to asthmatic patients as an alternative route of drug delivery. Methods: Five patients with bronchial asthma (BA), 10 patients with cough-variant asthma (CVA) and 13 patients with cough predominant asthma (CPA) whose symptoms were not adequately controlled despite their current therapy were enrolled in the study. Steroid ointment of mometasone furoate or betamethasone valerate, in the amount of 1/2 fingertip unit once or twice a day for up to 3 months, to the skin over the cervical trachea, was added to the current therapy. Diphenhydramine ointment was also tried by 14 of the study participants. Results: Out of 28 patients receiving the steroid treatment, cough was reduced in 11 patients (39.3%). Cough disappeared completely in 3 cases, improved in 7 cases, and reduced temporarily but worsened again during the course in 1 case. Out of 14 patients receiving diphenhydramine treatment, cough was reduced in 5 patients (35.7%). Conclusions: The existence of responders to topical steroid ointment therapy to the cervical trachea strongly suggests that the trachea is also involved as an airway inflammation site. Though less effective compared to inhaled corticosteroid therapy, the transdermal administration could be regarded as the third route of steroid therapy for asthmatic cough.

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Section: Discussionmentioning

confidence: 99%

Transdermal Application of Steroid to Cervical Trachea for the Cough in Patients with Bronchial Asthma and Cough Variant Asthma-A Pilot Study

Mouri¹,

Mizutani²

2013

J Allergy Ther

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“…In order to overcome the skin barrier posed by SC, a variety of physical or chemical penetration enhancing technologies have been developed and utilized, including but not limited to diverse nanocarrier systems, − chemical penetration enhancers, − skin penetrating peptides, , iontophoresis, − sonophoresis, − electroporation, , microneedle, − elongated microparticles, , and their reasonable combinations. − Among all those enhancement methods, a relatively straightforward physical approach to skin disruption is the microneedle application with a range of device configurations and application strategies. , Microneedles can create plenty of microholes in skin (50–200 μm in diameter) in a minimally invasive manner and then surmount the SC barrier without side effects apart from occasional erythema. , However, solid microneedles that pierce the skin to make it more permeable, such as microneedle roller or stamp, are immediately withdrawn after piercing the skin, therefore the effective penetration time for therapeutics post microneedle application is remarkably restrained since the punctured microholes within skin reduce and then close up in short time (10–20 min) , due to the skin self-contraction. Microneedle patches that are coated with or contain therapeutics or vaccines for dissolution in the skin, despite their sustained or controlled drug release in the skin, can be applied only to small areas of the skin because of the fixed small patch size.…”

Section: Introductionmentioning

confidence: 99%

Skin Delivery of Hydrophilic Biomacromolecules Using Marine Sponge Spicules

Zhang

Liu

et al. 2017

Mol. Pharmaceutics

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We report the development of sponge Haliclona sp. spicules, referred to as SHS, and its topical application in skin delivery of hydrophilic biomacromolecules, a series of fluorescein isothiocyanate-dextrans (FDs). SHS are silicious oxeas which are sharp-edged and rod-shaped (∼120 μm in length and ∼7 μm in diameter). SHS can physically disrupt skin in a dose-dependent manner and retain within the skin over at least 72 h, which allows sustained skin penetration of hydrophilic biomacromolecules. The magnitude of enhancement of FD delivery into skin induced by SHS treatment was dependent on its molecular weight. Specifically, SHS topical application enhanced FD-10 (MW: 10 kDa) penetration into porcine skin in vitro by 33.09 ± 7.16-fold compared to control group (p < 0.01). SHS dramatically increased the accumulation of FD-10 into and across the dermis by 62.32 ± 13.48-fold compared to the control group (p < 0.01). In vivo experiments performed using BALB/c mice also confirmed the effectiveness of SHS topical application; the skin absorption of FD-10 with SHS topical application was 72.14 ± 48.75-fold (p < 0.05) and 15.39 ± 9.91-fold (p < 0.05) higher than those from the PBS and Dermaroller microneedling, respectively. Further, skin irritation study and transepidermal water loss (TEWL) measurement using guinea pig skin in vivo indicated that skin disruption induced by SHS treatment is self-limited and can be recovered with time and efficiently. SHS can offer a safe, effective, and sustained skin delivery of hydrophilic biomacromolecules and presents a promising platform technology for a wide range of cosmetic and medical applications.

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“…The stratum corneum in the outermost layer of the skin restricts the skin penetration of hydrophilic and macromolecular drugs [ 4 , 5 ]. In order to solve this problem, a number of methods to improve transdermal drug transport have been evaluated, including chemical absorption enhancers [ 6 ], iontophoresis [ 7 ], sonophoresis [ 8 ], electroporation [ 9 , 10 ] and microneedle arrays (MN) [ 11 ]. Among these techniques, MN is an effective way to deliver macromolecular and hydrophilic drugs into systemic circulation from the skin.…”

Section: Introductionmentioning

confidence: 99%

Efficient Transdermal Delivery of Alendronate, a Nitrogen-Containing Bisphosphonate, Using Tip-Loaded Self-Dissolving Microneedle Arrays for the Treatment of Osteoporosis

et al. 2017

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To improve the transdermal bioavailability and safety of alendronate (ALN), a nitrogen-containing bisphosphonate, we developed self-dissolving microneedle arrays (MNs), in which ALN is loaded only at the tip portion of micron-scale needles by a dip-coating method (ALN(TIP)–MN). We observed micron-scale pores in rat skin just after application of ALN(TIP)–MN, indicating that transdermal pathways for ALN were created by MN. ALN was rapidly released from the tip of MNs as observed in an in vitro release study. The tip portions of MNs completely dissolved in the rat skin within 5 min after application in vivo. After application of ALN(TIP)–MN in mice, the plasma concentration of ALN rapidly increased, and the bioavailability of ALN was approximately 96%. In addition, the decrease in growth plate was effectively suppressed by this efficient delivery of ALN in a rat model of osteoporosis. Furthermore, no skin irritation was observed after application of ALN(TIP)–MN and subcutaneous injection of ALN, while mild skin irritation was induced by whole-ALN-loaded MN (ALN–MN)—in which ALN is contained in the whole of the micron-scale needles fabricated from hyaluronic acid—and intradermal injection of ALN. These findings indicate that ALN(TIP)–MN is a promising transdermal formulation for the treatment of osteoporosis without skin irritation.

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Iontophoresis-Facilitated Delivery of Prednisolone through Throat Skin to the Trachea After Topical Application of its Succinate Salt

Abstract: The present results suggest the usefulness of topical application of the ionic steroidal prodrugs onto throat skin followed by iontophoresis treatment for directly delivering the steroid to the trachea.

Cited by 6 publications

References 29 publications

Transdermal Application of Steroid to Cervical Trachea for the Cough in Patients with Bronchial Asthma and Cough Variant Asthma-A Pilot Study

Transdermal Application of Steroid to Cervical Trachea for the Cough in Patients with Bronchial Asthma and Cough Variant Asthma-A Pilot Study

Skin Delivery of Hydrophilic Biomacromolecules Using Marine Sponge Spicules

Efficient Transdermal Delivery of Alendronate, a Nitrogen-Containing Bisphosphonate, Using Tip-Loaded Self-Dissolving Microneedle Arrays for the Treatment of Osteoporosis

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