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• W2588896088 abstract "Transdermal drug delivery has recently received increasing attention in the faceof growing challenges to deliver peptide and protein drugs. Controlled transdermaldelivery is an important route for the delivery of peptides and proteins that canmaintain the therapeutic effectiveness of the drug by minimizing enzymaticdegradation which is a major concern in other noninvasive routes of delivery suchas the oral route. Although the advantages of transdermal delivery are verydesirable, the natural obstacle to drug entry imposed by the skin's barrier functionmakes it one of the most difficult route of administration.Iontophoresis and electroporation have been reported to be useful as permeationenhancing techniques in the transdermal delivery of protein and peptide drugs. Theobjective of present study is to use the above enhancement techniques to delivercyclosporin A (CSA) to treat psoriasis.The in vitro experiments were performed using hairless rat skin as the model withFranz diffusion cells for iontophoresis and custom made diffusion cells forelectroporation. The donor drug solution of CSA consisted of an aqueous solutionof CSA - polymer solid dispersion, coevaporate, and/or a hydroethanolic solutionof CSA PBS was used as the receiver solution. ³H labelled CSA and ¹⁴C labelledethanol were used to facilitate analysis using a liquid scintillation counter. Thecontrol experiment consisted of passive diffusion study. Silver/silver chloride electrodes were used in all studies. In the iontophoresis experiments a constantDC current (0.5 mA/cm²) was used. In the electroporation experiments differentdelivery parameters were studied: (1) applied electrode voltage (Uelectrode), (2) decaytime constant (τ), (3) the number of pulses delivered - single or multiple, and { 4) thetime of diffusive contact with drug after electroporation ('contact duration').Compared to the passive diffusion, iontophoresis did not result in a significantincrease in the amount of CSA delivered transdermally with both the CSA-polymerdonor and hydroethanolic drug solutions.With the use of electroporation there was a significant increase in thetransdermal delivery, compared to passive transport. With the CSA-polymercoevaporate donor solution the increase in delivery was only about 6 fold higherwhereas with the hydroethanolic solution the increase was about 60 times highercompared to passive diffusion. The 'contact duration• was an important fader anda 4-hour 'contact duration' was found to be the optimum time period required foreffective transdermal delivery. Use of single pulse (τ=5.6 ms) electroporationresulted in a significant increase {p<0.05) in the delivery of CSA in skin {CSA.n)and EtOH in receiver (EtOHreceiver). With multiple pulse (τ=10 ms. 25 pulses) theincrease in CSAskin was more pronounced with a 60 fold increase than comparedto the passive delivery. However there was no significant increase in the other twoquantities viz. CSAreceiver, and EtCHreceiver." @default.
• W2588896088 created "2017-02-24" @default.
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• W2588896088 date "1997-04-01" @default.
• W2588896088 modified "2023-09-25" @default.
• W2588896088 title "Transdermal delivery of cyclosporin A by electrically enhanced permeation techniques" @default.
• W2588896088 hasPublicationYear "1997" @default.
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