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Transdermal Delivery of Glimepiride: A Novel Approach Using Nanomicelle-Embedded Microneedles

Glimepiride (GM) is a hydrophobic drug that dissolves slowly and yields inconsistent clinical responses after oral administration. Transdermal drug delivery (TDD) is an appropriate alternative to oral administration. Microneedles (MNs) offer a promising delivery system that penetrates the skin, whil...

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Autores principales: Pervez, Sadia, Nasir, Fazli, Hidayatullah, Talaya, Khattak, Muzna Ali, Alasmari, Fawaz, Zainab, Syeda Rabqa, Gohar, Shazma, Tahir, Arbab, Maryam, Gul e
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10459310/
https://www.ncbi.nlm.nih.gov/pubmed/37631233
http://dx.doi.org/10.3390/pharmaceutics15082019
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author Pervez, Sadia
Nasir, Fazli
Hidayatullah, Talaya
Khattak, Muzna Ali
Alasmari, Fawaz
Zainab, Syeda Rabqa
Gohar, Shazma
Tahir, Arbab
Maryam, Gul e
author_facet Pervez, Sadia
Nasir, Fazli
Hidayatullah, Talaya
Khattak, Muzna Ali
Alasmari, Fawaz
Zainab, Syeda Rabqa
Gohar, Shazma
Tahir, Arbab
Maryam, Gul e
author_sort Pervez, Sadia
collection PubMed
description Glimepiride (GM) is a hydrophobic drug that dissolves slowly and yields inconsistent clinical responses after oral administration. Transdermal drug delivery (TDD) is an appropriate alternative to oral administration. Microneedles (MNs) offer a promising delivery system that penetrates the skin, while polymeric micelles can enhance the solubility; hence, the combination of both results in high drug bioavailability. This study aims to improve glimepiride’s solubility, dissolution rate, and bioavailability by incorporating nanomicelles into MNs for TDD. The nanomicelles formulated with 10% Soluplus(®) (SP) and 40% GM had a mean particle size of 82.6 ± 0.54, PDI of 0.1 ± 0.01, −16.2 ± 0.18 zeta potential, and achieved a 250-fold increase in solubility. The fabricated pyramid shaped GM-dissolving MNs were thermally stable and had no formulation incompatibility, as confirmed by thermal and FTIR analysis. The in vitro dissolution profile revealed that the GM release from nanomicelles and nanomicelle-loaded DMN was concentration-independent following non-Fickian transport mechanism. Improved pharmacokinetic parameters were obtained with dose of 240 µg as compared to 1 mg of GM oral tablet, in healthy human volunteers. The observed C(max), T(max) and MRT were 1.56 μg/mL ± 0.06, 4 h, and 40.04 h ± 3.37, respectively. The safety profile assessment indicated that microneedles are safe with no adverse effects on skin or health. This study provides an alternative delivery system for the administration of glimepiride, resulting in improved bioavailability, enhanced patient compliance, and reduced dosing frequency.
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spelling pubmed-104593102023-08-27 Transdermal Delivery of Glimepiride: A Novel Approach Using Nanomicelle-Embedded Microneedles Pervez, Sadia Nasir, Fazli Hidayatullah, Talaya Khattak, Muzna Ali Alasmari, Fawaz Zainab, Syeda Rabqa Gohar, Shazma Tahir, Arbab Maryam, Gul e Pharmaceutics Article Glimepiride (GM) is a hydrophobic drug that dissolves slowly and yields inconsistent clinical responses after oral administration. Transdermal drug delivery (TDD) is an appropriate alternative to oral administration. Microneedles (MNs) offer a promising delivery system that penetrates the skin, while polymeric micelles can enhance the solubility; hence, the combination of both results in high drug bioavailability. This study aims to improve glimepiride’s solubility, dissolution rate, and bioavailability by incorporating nanomicelles into MNs for TDD. The nanomicelles formulated with 10% Soluplus(®) (SP) and 40% GM had a mean particle size of 82.6 ± 0.54, PDI of 0.1 ± 0.01, −16.2 ± 0.18 zeta potential, and achieved a 250-fold increase in solubility. The fabricated pyramid shaped GM-dissolving MNs were thermally stable and had no formulation incompatibility, as confirmed by thermal and FTIR analysis. The in vitro dissolution profile revealed that the GM release from nanomicelles and nanomicelle-loaded DMN was concentration-independent following non-Fickian transport mechanism. Improved pharmacokinetic parameters were obtained with dose of 240 µg as compared to 1 mg of GM oral tablet, in healthy human volunteers. The observed C(max), T(max) and MRT were 1.56 μg/mL ± 0.06, 4 h, and 40.04 h ± 3.37, respectively. The safety profile assessment indicated that microneedles are safe with no adverse effects on skin or health. This study provides an alternative delivery system for the administration of glimepiride, resulting in improved bioavailability, enhanced patient compliance, and reduced dosing frequency. MDPI 2023-07-26 /pmc/articles/PMC10459310/ /pubmed/37631233 http://dx.doi.org/10.3390/pharmaceutics15082019 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Pervez, Sadia
Nasir, Fazli
Hidayatullah, Talaya
Khattak, Muzna Ali
Alasmari, Fawaz
Zainab, Syeda Rabqa
Gohar, Shazma
Tahir, Arbab
Maryam, Gul e
Transdermal Delivery of Glimepiride: A Novel Approach Using Nanomicelle-Embedded Microneedles
title Transdermal Delivery of Glimepiride: A Novel Approach Using Nanomicelle-Embedded Microneedles
title_full Transdermal Delivery of Glimepiride: A Novel Approach Using Nanomicelle-Embedded Microneedles
title_fullStr Transdermal Delivery of Glimepiride: A Novel Approach Using Nanomicelle-Embedded Microneedles
title_full_unstemmed Transdermal Delivery of Glimepiride: A Novel Approach Using Nanomicelle-Embedded Microneedles
title_short Transdermal Delivery of Glimepiride: A Novel Approach Using Nanomicelle-Embedded Microneedles
title_sort transdermal delivery of glimepiride: a novel approach using nanomicelle-embedded microneedles
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10459310/
https://www.ncbi.nlm.nih.gov/pubmed/37631233
http://dx.doi.org/10.3390/pharmaceutics15082019
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