Targeted Delivery of Miconazole Employing LL37 Fragment Mutant Peptide CKR12-Poly (Lactic-Co-Glycolic) Acid Polymeric Micelles

We previously reported that conjugates of antimicrobial peptide fragment analogues and poly (lactic-co-glycolic) acid (PLGA) enhance antimicrobial activity and that the conjugated micelle structure is an effective tool for antimicrobial drug delivery. In recent years, the delivery of antimicrobial p...

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Autores principales:	Takeshi Mori, Miyako Yoshida, Mai Hazekawa, Daisuke Ishibashi, Yoshiro Hatanaka, Rie Kakehashi, Makoto Nakagawa, Toshihiro Nagao, Miki Yoshii, Honami Kojima, Rio Uno, Takahiro Uchida
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	antimicrobial peptide scanning electron microscopy transmission electron microscopy micelle drug delivery drug targeting Biology (General) QH301-705.5 Chemistry QD1-999
Acceso en línea:	https://doaj.org/article/c9afa08c405a45fc975c8d026515e4e0
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spelling	oai:doaj.org-article:c9afa08c405a45fc975c8d026515e4e02021-11-11T17:27:13ZTargeted Delivery of Miconazole Employing LL37 Fragment Mutant Peptide CKR12-Poly (Lactic-Co-Glycolic) Acid Polymeric Micelles10.3390/ijms2221120561422-00671661-6596https://doaj.org/article/c9afa08c405a45fc975c8d026515e4e02021-11-01T00:00:00Zhttps://www.mdpi.com/1422-0067/22/21/12056https://doaj.org/toc/1661-6596https://doaj.org/toc/1422-0067We previously reported that conjugates of antimicrobial peptide fragment analogues and poly (lactic-co-glycolic) acid (PLGA) enhance antimicrobial activity and that the conjugated micelle structure is an effective tool for antimicrobial drug delivery. In recent years, the delivery of antimicrobial peptides to targets for antimicrobial activity has attracted attention. In this study, we targeted <i>Candida albicans</i>, a causative organism of catheter-related bloodstream infections, which is refractory to antimicrobial agents and is currently a problem in medical practice. We evaluated the antifungal activity of CKR12 (a mutant fragment of the human cathelicidin peptide, LL-37)-PLGA-miconazole (MCZ) micelles using nanotechnology with MCZ delivery. The prepared CKR12-PLGA-MCZ micelles were characterised by measuring dynamic light scattering, zeta potential, dilution stability, and drug release. CKR12-PLGA-MCZ micelles showed higher antifungal activity than CKR12-PLGA micelles and MCZ solution. Furthermore, scanning and transmission electron microscopy suggested that CKR12-PLGA-MCZ micelles disrupted both cell wall and cell membrane of <i>C. albicans</i>. Our results revealed a synergistic effect of antifungal activity using a combination of antimicrobial peptide fragment analogues and MCZ, and that MCZ is a promising tool for the delivery to target microorganisms.Takeshi MoriMiyako YoshidaMai HazekawaDaisuke IshibashiYoshiro HatanakaRie KakehashiMakoto NakagawaToshihiro NagaoMiki YoshiiHonami KojimaRio UnoTakahiro UchidaMDPI AGarticleantimicrobial peptidescanning electron microscopytransmission electron microscopymicelledrug deliverydrug targetingBiology (General)QH301-705.5ChemistryQD1-999ENInternational Journal of Molecular Sciences, Vol 22, Iss 12056, p 12056 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	antimicrobial peptide scanning electron microscopy transmission electron microscopy micelle drug delivery drug targeting Biology (General) QH301-705.5 Chemistry QD1-999
spellingShingle	antimicrobial peptide scanning electron microscopy transmission electron microscopy micelle drug delivery drug targeting Biology (General) QH301-705.5 Chemistry QD1-999 Takeshi Mori Miyako Yoshida Mai Hazekawa Daisuke Ishibashi Yoshiro Hatanaka Rie Kakehashi Makoto Nakagawa Toshihiro Nagao Miki Yoshii Honami Kojima Rio Uno Takahiro Uchida Targeted Delivery of Miconazole Employing LL37 Fragment Mutant Peptide CKR12-Poly (Lactic-Co-Glycolic) Acid Polymeric Micelles
description	We previously reported that conjugates of antimicrobial peptide fragment analogues and poly (lactic-co-glycolic) acid (PLGA) enhance antimicrobial activity and that the conjugated micelle structure is an effective tool for antimicrobial drug delivery. In recent years, the delivery of antimicrobial peptides to targets for antimicrobial activity has attracted attention. In this study, we targeted <i>Candida albicans</i>, a causative organism of catheter-related bloodstream infections, which is refractory to antimicrobial agents and is currently a problem in medical practice. We evaluated the antifungal activity of CKR12 (a mutant fragment of the human cathelicidin peptide, LL-37)-PLGA-miconazole (MCZ) micelles using nanotechnology with MCZ delivery. The prepared CKR12-PLGA-MCZ micelles were characterised by measuring dynamic light scattering, zeta potential, dilution stability, and drug release. CKR12-PLGA-MCZ micelles showed higher antifungal activity than CKR12-PLGA micelles and MCZ solution. Furthermore, scanning and transmission electron microscopy suggested that CKR12-PLGA-MCZ micelles disrupted both cell wall and cell membrane of <i>C. albicans</i>. Our results revealed a synergistic effect of antifungal activity using a combination of antimicrobial peptide fragment analogues and MCZ, and that MCZ is a promising tool for the delivery to target microorganisms.
format	article
author	Takeshi Mori Miyako Yoshida Mai Hazekawa Daisuke Ishibashi Yoshiro Hatanaka Rie Kakehashi Makoto Nakagawa Toshihiro Nagao Miki Yoshii Honami Kojima Rio Uno Takahiro Uchida
author_facet	Takeshi Mori Miyako Yoshida Mai Hazekawa Daisuke Ishibashi Yoshiro Hatanaka Rie Kakehashi Makoto Nakagawa Toshihiro Nagao Miki Yoshii Honami Kojima Rio Uno Takahiro Uchida
author_sort	Takeshi Mori
title	Targeted Delivery of Miconazole Employing LL37 Fragment Mutant Peptide CKR12-Poly (Lactic-Co-Glycolic) Acid Polymeric Micelles
title_short	Targeted Delivery of Miconazole Employing LL37 Fragment Mutant Peptide CKR12-Poly (Lactic-Co-Glycolic) Acid Polymeric Micelles
title_full	Targeted Delivery of Miconazole Employing LL37 Fragment Mutant Peptide CKR12-Poly (Lactic-Co-Glycolic) Acid Polymeric Micelles
title_fullStr	Targeted Delivery of Miconazole Employing LL37 Fragment Mutant Peptide CKR12-Poly (Lactic-Co-Glycolic) Acid Polymeric Micelles
title_full_unstemmed	Targeted Delivery of Miconazole Employing LL37 Fragment Mutant Peptide CKR12-Poly (Lactic-Co-Glycolic) Acid Polymeric Micelles
title_sort	targeted delivery of miconazole employing ll37 fragment mutant peptide ckr12-poly (lactic-co-glycolic) acid polymeric micelles
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/c9afa08c405a45fc975c8d026515e4e0
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Targeted Delivery of Miconazole Employing LL37 Fragment Mutant Peptide CKR12-Poly (Lactic-Co-Glycolic) Acid Polymeric Micelles

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