Functional Polyion Complex Micelles for Potential Targeted Hydrophobic Drug Delivery
Abstract
:1. Introduction
2. Materials and Methods
2.1. Chemicals and Reagents
2.2. Synthesis of PHEMA-b-PLLys Block Copolymer
2.2.1. Synthesis of Poly(2-Hydroxyethyl Methacrylate) with Protected Amine End-Group (PHEMA-N-Boc)
2.2.2. Synthesis of Poly(2-Hydroxyethyl Methacrylate) Macroinitiator (PHEMA-NH2)
2.2.3. Synthesis of PHEMA-b-PZLLys Block Copolymer
2.2.4. Primary Amine Groups Deprotection
2.3. Synthesis of LBA-PEG-b-PLAsp Functional Block Copolymer
2.3.1. Synthesis of HO-PEG-b-PBzLAsp Block Copolymer
2.3.2. End-Functionalization with LBA and Carboxyl Groups Deprotection
2.4. Characterization Methods
2.5. Polyion Complex (PIC) Micelles Preparation
2.6. Critical Micelle Concentration (CMC) Estimation
2.7. Drug Loading and In Vitro Drug Release
2.8. Antioxidant Activity Estimation via DPPH• Radical Scavenging Assay
3. Results and Discussion
3.1. Synthesis and Characterization of Functional Oppositely Charged Hybrid Block Copolymers
3.2. Formation of Polyion Complex Micelles from the Synthesized Oppositely Charged Hybrid Block Copolymers
3.3. Hydrophobic Drug Loading into the Polyion Complex Micelles
3.4. In Vitro Drug Release and Antioxidant Activity Measurements
4. Conclusions
Supplementary Materials
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
Sample Availability
References
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Macroinitiators | Hybrid Diblock Copolymers | |||||||
---|---|---|---|---|---|---|---|---|
Code | DPna | Mna (g mol−1) | ÐMb | Code | t-DPn c | DPna | Mna (g mol−1) | ÐMb |
PHEMA-NH2 | 26 | 3400 | 1.23 | PHEMA-b-PZLLys | 35 | 37 | 13,100 | 1.38 |
HO-PEG-NH2 | 68 | 3000 | 1.12 | HO-PEG-b-PLBzAsp | 35 | 30 | 9150 | 1.30 |
Empty PIC Micelles | Drug Loaded PIC Micelles | ||||||||
---|---|---|---|---|---|---|---|---|---|
Code | d a (nm) | PdI a | ζ a (mV) | d a (nm) | PdI a | ζ a (mV) | DLE b (%) | DLC b (%) | IC50 c (μg mL−1) |
PIC 1:5 | 95.85 ± 1.21 | 0.295 | −21.64 ± 2.10 | 109.99 ± 0.92 | 0.077 | −19.24 ± 2.00 | 71 | 6.4 | 19.94 |
PIC 1:1 | 90.02 ± 3.45 | 0.318 | −4.41 ± 1.58 | 101.81 ± 1.83 | 0.077 | −2.06 ± 2.35 | 66 | 6.5 | 25.43 |
PIC 5:1 | 79.14 ± 1.68 | 0.109 | 10.93 ± 1.31 | 89.35 ± 0.18 | 0.079 | 9.79 ± 1.73 | 60 | 5.5 | 20.02 |
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Kalinova, R.; Dimitrov, I. Functional Polyion Complex Micelles for Potential Targeted Hydrophobic Drug Delivery. Molecules 2022, 27, 2178. https://doi.org/10.3390/molecules27072178
Kalinova R, Dimitrov I. Functional Polyion Complex Micelles for Potential Targeted Hydrophobic Drug Delivery. Molecules. 2022; 27(7):2178. https://doi.org/10.3390/molecules27072178
Chicago/Turabian StyleKalinova, Radostina, and Ivaylo Dimitrov. 2022. "Functional Polyion Complex Micelles for Potential Targeted Hydrophobic Drug Delivery" Molecules 27, no. 7: 2178. https://doi.org/10.3390/molecules27072178