Characterization of Solid Maltose Microneedles and their Use for Transdermal Delivery

Kolli, Chandra Sekhar; Banga, Ajay K.

doi:10.1007/s11095-007-9350-0

Cited by 188 publications

(134 citation statements)

References 20 publications

Supporting

Mentioning

123

Contrasting

Unclassified

Order By: Relevance

“…21) Kolli and Banga reported that micropiles with a length of 500 mm are applied to the skin and pressed using a finger with a pressure of approximately 0.35-0.5 N, the whole micropile is not inserted into the skin. 22) The usefulness of SDMP was studied with macromolecular compounds such as insulin, 23) low molecular weight heparin (LMWH) 24) and erythropoietin (EPO) 25) from both pharmacokinetic and pharmacodynamic aspects. From these studies, SDMPs were shown to be an effective TDDS for the percutaneous absorption of hydrophilic macromolecular drugs.…”

mentioning

confidence: 99%

Permeation Enhancement of Ascorbic Acid by Self-Dissolving Micropile Array Tip through Rat Skin

Ito¹,

Maeda²,

Fukushima³

et al. 2010

Chem. Pharm. Bull.

View full text Add to dashboard Cite

Ascorbic acid (AA, vitamin C) is a hydrophilic vitamin that cannot be produced endogenously in rats and primates including human and is widely used for the protection of the aging of the skin due to the exposure to the UV light and for the acceleration of the synthesis of collagen in the skin. [1][2][3][4] AA was shown to be absorbed from the gastrointestinal tract by an active transport system, though limited amount of AA was transported by this system. 5) In addition, after AA was absorbed, AA was rapidly eliminated from the body by the oxidative metabolism through both enzymatic and nonenzymatic processes.2) Therefore, even if we intake excess amount of AA, sufficient amount of AA is not absorbed into the systemic circulation and is not delivered to its target tissue, skin.2) To conquer this problem, percutaneous delivery of AA has been challenged. The advantage of percutaneous delivery of AA is (1) to obtain high concentration of AA in the skin and (2) to escape the hepatic first-pass effect before reaching to the systemic circulation. However, when AA is percutaneously administered, the penetration of AA to the dermal tissue is difficult because of the high barrier function of the skin. To increase the permeability of AA, derivatives such asascorbic acid 2-sulfate 8) and disodium isostearyl 2-o-L-ascorbyl phosphate, 9,10) has been developed. Also Gopinath et al. designed ascorbyl palmitate vesicles (Aspasomes) for the transdermal delivery of ascorbic acid.11) Furthermore, recent advances in pharmaceutical technology have promoted the research on the permeability enhancement of AA using physical absorption enhancing method like iontophoresis 12) and microemulsion technologies.11,13) Iontophoresis uses an electric field to drive ionized molecules across the skin by electrophoresis and non-ionized molecules by electro osmosis. 14)Despite concerns about skin irritation, iontophoresis may be useful to deliver some peptides and small proteins.15) On the other hand, microneedles are also one of the physical methods for the percutaneous absorption of drugs. With microneedles, small microconduits are formed on the skin. Recent advance in microfabrication technology has made it possible to prepare microneedles that have a possibility of novel transdermal drug delivery system (TDDS). Since the first publication by Henry et al.,16) microfabrication techniques for the production of silicon, metal, glass and polymer microneedle arrays with micrometer dimensions have been developed. 17-20) The microneedles are either solid or hollow and posses a geometrical shape. Microneedle TDDS is roughly defined by a micron size needle preparation for percutaneous administration. Microneedle TDDSs are classified as follows; (1) extremely small needle through which drug solution can be injected into the skin, (2) metallic and/or silastic microneedles on which surface drug is coated, and (3) metallic and/or silastic microneedles by which microconduits are made on the skin and drug solution is applied after removing the microneedles. H...

show abstract

mentioning

confidence: 99%

Permeation Enhancement of Ascorbic Acid by Self-Dissolving Micropile Array Tip through Rat Skin

Ito¹,

Maeda²,

Fukushima³

et al. 2010

Chem. Pharm. Bull.

View full text Add to dashboard Cite

show abstract

“…Therefore, to reach an effective blood concentration, the therapeutic efficacy of drug should be improved by increasing drug administration. [21] Kolli and Banga [22] show that the plasma drug concentration reaches its maximum when using microneedles as compared to passive 95 delivery.…”

mentioning

confidence: 99%

Transdermal drug delivery by coated microneedles: geometry effects on drug concentration in blood

Al-Qallaf

Das

Davidson

2009

Asia-Pacific J Chem Eng

View full text Add to dashboard Cite

Drug administration through transdermal delivery is restricted by the top layer of skin, the stratum corneum. One possible solution to overcome the barrier function of the stratum corneum is to employ microneedle arrays. However, detailed theoretical models relating drug‐coated microneedles and their geometry to the drug concentration in the blood are limited. This article aims to address this issue by examining the blood concentration profiles for a model drug, insulin, that has been administered via coated microneedles. A mathematical model is introduced and applied to predict theoretical blood concentrations. Furthermore, the insulin concentration in blood is calculated for a range of different microneedle shapes and dimensions to identify the most effective geometry. The results indicate that the optimum microneedle geometry in terms of maximizing insulin concentration was a rocket‐shaped needle with a constant tip angle of 90°. Also, it has been found that the number of microneedles in an array is the most significant factor in determining maximum insulin concentration in the blood (Cb, max). Penetration depth of the microneedle, centre‐to‐centre spacing and microneedle thickness had a less significant effect on the maximum insulin concentration in the blood. It is envisaged that the current study will help in designing microneedles of optimum size and shape for transdermal drug delivery. Copyright © 2009 Curtin University of Technology and John Wiley & Sons, Ltd.

show abstract

“…Therefore even in the case of metallic micropiles, the length was designed to be Ͼ500 mm. 28) When micropiles with a length of 500 mm are applied to the skin, it was pressed using a finger with a pressure of approximately 0.35-0.5 N. 29) In our study, the SDMA chip was administered to both rat and dog abdominal skin using the pressure of the fingers. The skin was at first pulled up with two fingers.…”

Section: Discussionmentioning

confidence: 93%

“…A coin was pressed against one side of the skin fold, and SDMA was inserted on the other side of skin by pressing with a finger. Both pressing force was adjusted to 0.3-0.5 N. 29) Using this method, SDMA was easily inserted into the skin and a good absorption enhancing effect was obtained in both rat and dog experiments.…”

Section: Discussionmentioning

confidence: 99%

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

Ito

Hasegawa

Fukushima

et al. 2010

Biological & Pharmaceutical Bulletin

View full text Add to dashboard Cite

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...

show abstract

Characterization of Solid Maltose Microneedles and their Use for Transdermal Delivery

Abstract: Maltose microneedles were characterized and shown to create microchannels in the skin, which were also characterized and shown to improve the transdermal delivery of NH.

Cited by 188 publications

References 20 publications

Permeation Enhancement of Ascorbic Acid by Self-Dissolving Micropile Array Tip through Rat Skin

Permeation Enhancement of Ascorbic Acid by Self-Dissolving Micropile Array Tip through Rat Skin

Transdermal drug delivery by coated microneedles: geometry effects on drug concentration in blood

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

Contact Info

Product

Resources

About