Fabrication and Characterization of Thiolated Chitosan Microneedle Patch for Transdermal Delivery of Tacrolimus.

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Abstrakt

Tytuł:: Fabrication and Characterization of Thiolated Chitosan Microneedle Patch for Transdermal Delivery of Tacrolimus.
Autorzy:: Ahmad Z; Riphah Institute of Pharmaceutical Sciences (RIPS), Riphah International University, Lahore Campus, Lahore, Pakistan.
Khan MI; Riphah Institute of Pharmaceutical Sciences (RIPS), Riphah International University, Lahore Campus, Lahore, Pakistan.
Siddique MI; Institute of Pharmaceutical Sciences, University of Veterinary and Animal Sciences, Lahore, Pakistan.
Sarwar HS; Riphah Institute of Pharmaceutical Sciences (RIPS), Riphah International University, Lahore Campus, Lahore, Pakistan.; Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, 45320, Pakistan.
Shahnaz G; Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, 45320, Pakistan.
Hussain SZ; Department of Chemistry and Chemical Engineering, SBA School of Science and Engineering (SBA-SSE), Lahore University of Management Sciences (LUMS), Lahore, 54792, Pakistan.
Bukhari NI; College of Pharmacy, University of the Punjab, Lahore, Pakistan.
Hussain I; Department of Chemistry and Chemical Engineering, SBA School of Science and Engineering (SBA-SSE), Lahore University of Management Sciences (LUMS), Lahore, 54792, Pakistan.
Sohail MF; Riphah Institute of Pharmaceutical Sciences (RIPS), Riphah International University, Lahore Campus, Lahore, Pakistan. .; Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, 45320, Pakistan. .; Department of Chemistry and Chemical Engineering, SBA School of Science and Engineering (SBA-SSE), Lahore University of Management Sciences (LUMS), Lahore, 54792, Pakistan. .
Źródło:: AAPS PharmSciTech [AAPS PharmSciTech] 2020 Jan 16; Vol. 21 (2), pp. 68. Date of Electronic Publication: 2020 Jan 16.
Typ publikacji:: Journal Article
Język:: English
Imprint Name(s):: Publication: New York : Springer
Original Publication: Arlington, VA : American Association of Pharmaceutical Scientists, c2000-
MeSH Terms:: Transdermal Patch*
Chitosan/*chemistry
Immunosuppressive Agents/*administration & dosage
Tacrolimus/*administration & dosage
Animals ; Diffusion Chambers, Culture ; Disulfides/chemistry ; Drug Delivery Systems ; Equipment Design ; Microinjections ; Needles ; Rats ; Skin/metabolism ; Sulfhydryl Compounds ; Tensile Strength
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Contributed Indexing:: Keywords: microneedle patch; tacrolimus; thiolated chitosan; transdermal delivery
Substance Nomenclature:: 0 (Disulfides)
0 (Immunosuppressive Agents)
0 (Sulfhydryl Compounds)
9012-76-4 (Chitosan)
WM0HAQ4WNM (Tacrolimus)
Entry Date(s):: Date Created: 20200118 Date Completed: 20200406 Latest Revision: 20210325
Update Code:: 20231215
DOI:: 10.1208/s12249-019-1611-9
PMID:: 31950394
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Microneedle patch is a prominent strategy with minimal invasion and painless application to improve skin penetration of drug molecules. Herein, we report microneedle patch (MNP) as an alternative to the oral route for the systemic delivery of tacrolimus (TM), an immunosuppressant drug. Thiolated chitosan (TCS) based microneedle patch was fabricated and characterized in vitro and in vivo for its mechanical strength, skin penetration, drug release, and skin irritation. The MNP having 225 needles with 575 μm showed good mechanical properties in terms of tensile strength and percentage elongation. The skin penetration showed 84% penetration with no breakage. Histology of the mice skin after insertion showed the penetration of needles into the dermis. In vitro release and ex vivo permeation studies through Franz diffusion cell showed the sustained release (82.5%) of TM from the MNP with significantly higher (p < 0.05) skin permeation as compared with controls, respectively. Moreover, in vivo biocompatibility in rats showed the safety of the material and patch. Thus, the TCS microneedle patch has the potential to be developed as a transdermal delivery system for tacrolimus with improved bioavailability and sustained release over a longer period.

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