Pharmacokinetic and pharmacodynamic studies following percutaneous absorption of erythropoietin micropiles to rats

Ito, Yoshiaki; Shiroyama, K; Yoshimitsu, Jun-Ichiro; Ohashi, Yoshinori; Sugioka, Nobuyuki; Takada, Kanji

doi:10.1016/j.jconrel.2007.05.028

Cited by 15 publications

(6 citation statements)

References 25 publications

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“…Moreover, we reported rat experiment with pen-type micropiles. 18) Although BA values in rat were not evaluated, BA was calculated approximately 40% with pen-type micropiles using data in i.v. experiment and corresponded with SDMA chip in this study.…”

Section: Discussionmentioning

confidence: 99%

“…When microneedle arrays are inserted into the skin, conduits are created for the penetration of drug across stratum corneum (SC). Once a drug penetrates the SC, it can diffuse rapidly through the deeper tissue and permeate into the underlying capillaries for systemic absorption.Our previous studies suggest that macromolecules such as insulin, 15,16) erythropoietin (EPO), 17,18) interferon, 19) and recombinant human growth hormone 20) are well absorbed through rat skin by self-dissolving micropile preparations about 2-3 mm in length with an outer diameter of 0.3-0.4 mm. In addition, a self-dissolving micropile array (SDMA), comprising 10 lines and 10 columns, was formed on a 1.0-cm 2 chip, where water-soluble thread-forming polymers such as chondroitin sulfate and dextran were used as the base and insulin was formulated as a model peptide drug.…”

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confidence: 99%

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Self-Dissolving Micropile Array Chip as Percutaneous Delivery System of Protein Drug

Ito

Hasegawa

Fukushima

et al. 2010

Biological & Pharmaceutical Bulletin

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Transdermal drug delivery systems (TDDS) have been challenged to increase the permeation rate of drugs through the skin and experimental strategies have included the use of chemical enhancers and physical methods. Of these, chemical enhancers have contributed most to the development of TDDS. Approximately 20 products of TDDS were launched on the US market by the end of 2008. Thus the penetration of small molecules through the skin can be enhanced by chemical enhancers.1) However, triggering of skin irritation and other safety concerns limit their use. As examples of physical absorption enhancement methods, iontophoresis, electroporation, and ultrasound have been investigated.2-6) Iontophoresis uses an electric field to drive ionized molecules across the skin by electrophoresis and nonionized molecules by electroosmosis. Despite concerns about skin irritation, iontophoresis may be useful for delivery of some peptides including insulin. 7) In particular, TDDS of lidocaine by iontophoresis was launched onto the US market in 2004. Also, transient enhancement of skin permeability of both small drugs and macromolecules has been shown by electroporation and ultrasound. 8,9) Recent advances in microfabrication technology have made it possible to prepare microneedles that have a possible application as novel TDDS. Since the first publication by Henry et al. 10) in 1998, microfabrication techniques for the production of silicon, metal, glass and polymer microneedle arrays with micrometer dimensions have been reported. [11][12][13][14] The microneedles are either solid or hollow and possess a geometrical shape. Microneedle TDDS are roughly defined by a micron-sized needle preparation through and by which drug is percutaneously administered. Microneedle TDDS are classified as follows: (1) extremely small needles through which drug solution can be injected into the skin; (2) metallic and/or silastic microneedles on whose surface drug is coated; and (3) metallic and/or silastic microneedles with which conduits (micropores) are made on the skin and drug solution is applied after removing the microneedles. Fully to understand the function of microneedles, the physiology of the skin must be considered. There are no blood vessels in the epidermis. Deeper, there are blood capillaries in the dermis, which forms the bulk of skin volume and contains living cells and nerves. When microneedle arrays are inserted into the skin, conduits are created for the penetration of drug across stratum corneum (SC). Once a drug penetrates the SC, it can diffuse rapidly through the deeper tissue and permeate into the underlying capillaries for systemic absorption.Our previous studies suggest that macromolecules such as insulin, 15,16) erythropoietin (EPO), 17,18) interferon, 19) and recombinant human growth hormone 20) are well absorbed through rat skin by self-dissolving micropile preparations about 2-3 mm in length with an outer diameter of 0.3-0.4 mm. In addition, a self-dissolving micropile array (SDMA), comprising 10 lines and 10 columns, was...

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Section: Discussionmentioning

confidence: 99%

mentioning

confidence: 99%

Self-Dissolving Micropile Array Chip as Percutaneous Delivery System of Protein Drug

Ito

Hasegawa

Fukushima

et al. 2010

Biological & Pharmaceutical Bulletin

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“…The blood samples withdrawn as above were transferred to a series of graduated centrifuge tube containing 1 mL of 10% w/v EDTA solution. [17] The samples were centrifuged immediately at 3000rpm for 15 min in cooling centrifuge machine to collect plasma. [18] The plasma was separated and transferred into other set of sample tubes and stored at –20°C until assayed.…”

Section: Methodsmentioning

confidence: 99%

Formulation, In Vitro and In Vivo Pharmacokinetics of Anti-HIV Vaginal Bioadhesive Gel

Chatterjee

2011

Journal of Young Pharmacists

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Inexpensive and female-controlled pre-exposure prophylaxis strategies to prevent mucosal transmission of the virus, is urgently needed with the rising prevalence of human immunodeficiency virus (HIV-1 and HIV2) infections in women. Zidovudine-loaded bioadhesive vaginal gel may become one of the very useful strategies, as it can be used not only for controlled release but also for enhancing bioavailability. Drug delivery through vaginal gel is a promising area for continued research with the aim of achieving controlled release with enhanced bioavailability over longer periods of time. The aim of the study was to develop a newer prolong releasing Zidovudine (AZT) bioadhesive vaginal gel to treat HIV infections with increased patient convenience. AZT-loaded bioadhesive vaginal gel was prepared successfully by using cold mechanical method. F3 formulation containing carbopol–HPMC (1:3) was selected and evaluated in order to achieve objectives of this study. In vitro drug release study of F3 showed in 24 h drug released following case I Fickian (n ≤ 0.5) transport mechanism, and in vivo drug release was found much better (Tmax), (Cmax), and bioavailability (F) comparison with oral pour drug solution. It was also showed good extrudability, spreadability, and bioadhesive strength. A generalized protocol, for the further research, in this area will surely expected to yield significant outcome with improved drug delivery system.

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“…and the usefulness were suggested with insulin (Ito et al, 2006a(Ito et al, , 2008a, erythropoietin (EPO) (Ito et al, 2006b(Ito et al, , 2007, interferon (Ito et al, 2008b) and recombinant human growth hormone (Ito et al, 2008c). They were well absorbed through rat skin by dissolving microneedle preparations about 2-3 mm in length with an outer diameter of 0.3-0.4 mm.…”

Section: Introductionmentioning

confidence: 99%

Incidence of low bioavailability of leuprolide acetate after percutaneous administration to rats by dissolving microneedles

Ito

Murano

Hamasaki

et al. 2011

International Journal of Pharmaceutics

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Pharmacokinetic and pharmacodynamic studies following percutaneous absorption of erythropoietin micropiles to rats

Cited by 15 publications

References 25 publications

Self-Dissolving Micropile Array Chip as Percutaneous Delivery System of Protein Drug

Self-Dissolving Micropile Array Chip as Percutaneous Delivery System of Protein Drug

Formulation, In Vitro and In Vivo Pharmacokinetics of Anti-HIV Vaginal Bioadhesive Gel

Incidence of low bioavailability of leuprolide acetate after percutaneous administration to rats by dissolving microneedles

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