Preparation and Release of pH-Sensitive β-Cyclodextrin Derivative Micelles Loaded with Paclitaxel

In this paper, a new amphiphilic mono-6-β-cyclodextrin octadecylimine (6-β-CD-N-ODMA) copolymer was synthesized based on β-cyclodextrin and octadecylamine, which can self-assemble to form polymeric micelles. Drug-loaded micelles (a new drug carrier) were obtained using 6-β-CD-N-ODMA and paclitaxel (...

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Veröffentlicht in:Polymers 2022-06, Vol.14 (12), p.2482
Hauptverfasser: Zhao, Meirong, Jiang, Weiwei, Xie, Xinrong, Jaiswal, Yogini, Williams, Leonard, Wei, Mei, Mo, Ying, Guan, Yifu, Yang, Hua
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container_end_page
container_issue 12
container_start_page 2482
container_title Polymers
container_volume 14
creator Zhao, Meirong
Jiang, Weiwei
Xie, Xinrong
Jaiswal, Yogini
Williams, Leonard
Wei, Mei
Mo, Ying
Guan, Yifu
Yang, Hua
description In this paper, a new amphiphilic mono-6-β-cyclodextrin octadecylimine (6-β-CD-N-ODMA) copolymer was synthesized based on β-cyclodextrin and octadecylamine, which can self-assemble to form polymeric micelles. Drug-loaded micelles (a new drug carrier) were obtained using 6-β-CD-N-ODMA and paclitaxel (PTX) by the dialysis method. Orthogonal experiments were used to optimize the preparation method of the drug-loaded micelles. The drug-loading content of the carrier prepared by the optimized method was 1.97%. The physicochemical properties of blank micelles and drug-loaded micelles were evaluated by the fluorescence probe method, infrared spectra, dynamic light scattering, and scanning electron microscopy. The release properties of the carrier were investigated. The carrier has good pH sensitivity and the cumulative release rate after 96 h was 88% in PBS (pH = 5.0). The Ritger–Peppas equation is the optimal model for PTX released at pH 5.0, implying that the hydrolysis effect of 6-β-CD-N-ODMA is the main reason for PTX release. The results indicate that the developed carrier can increase the solubility of PTX and possess potential for increased clinical efficacy of PTX.
doi_str_mv 10.3390/polym14122482
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Drug-loaded micelles (a new drug carrier) were obtained using 6-β-CD-N-ODMA and paclitaxel (PTX) by the dialysis method. Orthogonal experiments were used to optimize the preparation method of the drug-loaded micelles. The drug-loading content of the carrier prepared by the optimized method was 1.97%. The physicochemical properties of blank micelles and drug-loaded micelles were evaluated by the fluorescence probe method, infrared spectra, dynamic light scattering, and scanning electron microscopy. The release properties of the carrier were investigated. The carrier has good pH sensitivity and the cumulative release rate after 96 h was 88% in PBS (pH = 5.0). The Ritger–Peppas equation is the optimal model for PTX released at pH 5.0, implying that the hydrolysis effect of 6-β-CD-N-ODMA is the main reason for PTX release. The results indicate that the developed carrier can increase the solubility of PTX and possess potential for increased clinical efficacy of PTX.</description><identifier>ISSN: 2073-4360</identifier><identifier>EISSN: 2073-4360</identifier><identifier>DOI: 10.3390/polym14122482</identifier><identifier>PMID: 35746058</identifier><language>eng</language><publisher>Basel: MDPI AG</publisher><subject>Cancer therapies ; Copolymers ; Cyclodextrins ; Dosage and administration ; Drug carriers ; Drug delivery systems ; Drugs ; Efficiency ; Fluorescent indicators ; Hemodialysis ; Infrared spectra ; Methods ; Micelles ; Optimization ; Paclitaxel ; Photon correlation spectroscopy ; Vehicles</subject><ispartof>Polymers, 2022-06, Vol.14 (12), p.2482</ispartof><rights>COPYRIGHT 2022 MDPI AG</rights><rights>2022 by the authors. Licensee MDPI, Basel, Switzerland. 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Drug-loaded micelles (a new drug carrier) were obtained using 6-β-CD-N-ODMA and paclitaxel (PTX) by the dialysis method. Orthogonal experiments were used to optimize the preparation method of the drug-loaded micelles. The drug-loading content of the carrier prepared by the optimized method was 1.97%. The physicochemical properties of blank micelles and drug-loaded micelles were evaluated by the fluorescence probe method, infrared spectra, dynamic light scattering, and scanning electron microscopy. The release properties of the carrier were investigated. The carrier has good pH sensitivity and the cumulative release rate after 96 h was 88% in PBS (pH = 5.0). The Ritger–Peppas equation is the optimal model for PTX released at pH 5.0, implying that the hydrolysis effect of 6-β-CD-N-ODMA is the main reason for PTX release. 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The results indicate that the developed carrier can increase the solubility of PTX and possess potential for increased clinical efficacy of PTX.</abstract><cop>Basel</cop><pub>MDPI AG</pub><pmid>35746058</pmid><doi>10.3390/polym14122482</doi><orcidid>https://orcid.org/0000-0003-0886-5204</orcidid><oa>free_for_read</oa></addata></record>
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subjects Cancer therapies
Copolymers
Cyclodextrins
Dosage and administration
Drug carriers
Drug delivery systems
Drugs
Efficiency
Fluorescent indicators
Hemodialysis
Infrared spectra
Methods
Micelles
Optimization
Paclitaxel
Photon correlation spectroscopy
Vehicles
title Preparation and Release of pH-Sensitive β-Cyclodextrin Derivative Micelles Loaded with Paclitaxel
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