Self-Assembled Block Copolymer Nanoaggregates for Drug Delivery Applications

Kuperkar, Ketan; Tiwari, Sanjay; Bahadur, Pratap

doi:10.1016/b978-0-12-819659-5.00015-x

Cited by 15 publications

(18 citation statements)

References 89 publications

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“…Tetronics are broadly used in various applications such as anti‐foaming and wetting agents, thickeners, dispersants, and emulsifiers for diverse industrial drives 29,30 . Tetronics are regularly useful in biomedical domains such as genetic immunization, drug delivery, and membrane biochemistry 31‐36 . Despite of this numerous and potential pharmaceutical applications, there are presently no studies reporting the antibacterial activity of tetronic derivatives.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, antimicrobial and anticancer activities of Tetronic 1107 Schiff bases

Alasmary

Kenawy

El‐Deeb

et al. 2022

Polymers for Advanced Techs

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As a result of the serious issues connected to the bacterial infections, there is an imperious need to improve strong and ecofriendly antimicrobial polymers to overcome the limitations of conventional antimicrobial agents. In this trend, poloxamines (Tetronics) which are X‐shaped poly(ethylene oxide)–poly(propylene oxide) diblocks linked to a focal ethylenediamine group; were successfully modified to produce Tetronic Schiff base for enhancing the biological activities of Tetronic 1107. Modification of tetronic 1107 (T1107) was proceeded throughout chloroacetylation of T1107 followed by amination using p‐phenylenediamine then the latter was treated with different aldehydes to yield Tetronic Schiff bases. Characterization of Tetronic Schiff bases was carried out by 1H‐NMR, Fourier‐transform infrared spectroscopy, X‐ray diffraction, elemental analysis and thermogravimetric analysis (TGA) analyses. The antimicrobial activities of four tested compounds coded (EK1, EK2, EK3, and EK4) were quantified using Microtiter‐assay methods. The obtained data revealed potential antimicrobial activities for tested compounds against all tested microbes with priority against Pseudomonas aeruginosa, Escherichia coli and Staphylococcus aureus. Sample coded EK4 exhibited the most effective treatment against P. aeruginosa, Candida albicans, S. aureus and E. Coli with minimal inhibitory concentration values of 6, 16, 12.5, and 1.5 μM, respectively. Furthermore, the safety results confirmed that EK4 and EK1 were the safest treatment with IC50 values of 76.01 and 62.67 μM, respectively. In addition, all tested compounds showed significant anticancer effects against MDA‐MB‐231cell line, while EK3 was effective treatment against A549 cell line with IC50 values of 39.63 μM. Meanwhile, both EK2 and EK4 showed the highest selectivity index (SI) values against MDA‐MB‐231 cell line with values 2.5 and 3.07, respectively. Interestingly, EK4 showed the maximum SI values on A549 and Hep‐G2 cell lines with values 1.62 and 1.52, respectively.

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Section: Introductionmentioning

confidence: 99%

Synthesis, antimicrobial and anticancer activities of Tetronic 1107 Schiff bases

Alasmary

Kenawy

El‐Deeb

et al. 2022

Polymers for Advanced Techs

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“…Polyamines, commercially available as Tetronic ® , are formed by blocks of copolymers consisting of poly (ethylene oxide) (PEO) and poly (propylene oxide) (PPO) units arranged in a four-armed star shape with different hydrophilic-lipophilic balance (HBL), and molecular weight [10,11], being very attractive as drug delivery systems due to the capacity to form nanometric structures as micelles or worm-like micelles, for example, [12][13][14]. Structurally, Tetronics are similar to Pluronics ® [15][16][17]. PEO-PPO-PEO copolymer block micelles (Pluronic) incorporating doxorubicin (SP1049C) are used in clinical studies as anticancer agents [18].…”

Section: Introductionmentioning

confidence: 99%

New Machine Learning Approach for the Optimization of Nano-Hybrid Formulations

et al. 2022

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Nano-hybrid systems are products of interactions between organic and inorganic materials designed and planned to develop drug delivery platforms that can be self-assembled. Poloxamine, commercially available as Tetronic®, is formed by blocks of copolymers consisting of poly (ethylene oxide) (PEO) and poly (propylene oxide) (PPO) units arranged in a four-armed star shape. Structurally, Tetronics are similar to Pluronics®, with an additional feature as they are also pH-dependent due to their central ethylenediamine unit. Laponite is a synthetic clay arranged in the form of discs with a diameter of approximately 25 nm and a thickness of 1 nm. Both compounds are biocompatible and considered as candidates for the formation of carrier systems. The objective is to explore associations between a Tetronic (T1304) and LAP (Laponite) at concentrations of 1–20% (w/w) and 0–3% (w/w), respectively. Response surface methodology (RMS) and two types of machine learning (multilayer perceptron (MLP) and support vector machine (SVM)) were used to evaluate the physical behavior of the systems and the β-Lapachone (β-Lap) solubility in the systems. β-Lap (model drug with low solubility in water) has antiviral, antiparasitic, antitumor, and anti-inflammatory properties. The results show an adequate machine learning approach to predict the physical behavior of nanocarrier systems with and without the presence of LAP. Additionally, the analysis performed with SVM showed better results (R2 > 0.97) in terms of data adjustment in the evaluation of β-Lap solubility. Furthermore, this work presents a new methodology for classifying phase behavior using ML. The new methodology allows the creation of a phase behavior surface for different concentrations of T1304 and LAP at different pHs and temperatures. The machine learning strategies used were excellent in assisting in the optimized development of new nano-hybrid platforms.

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“…The progress of drug delivery technology has created a rich landscape of enterprising and promising polymer-based candidates for the demanding treatment of critical diseases [1,2]. Amphiphilic block copolymers (AmBCs) are now ubiquitous in drug delivery formulations, endowing drugs with favorable properties [3], such as water solubilization, enhanced stability and systemic circulation, increased uptake rate of target cells/tissues, reduced enzyme degradation and controlled release of the drug [4,5].…”

Section: Introductionmentioning

confidence: 99%

Poly(2-oxazoline)-Based Amphiphilic Gradient Copolymers as Nanocarriers for Losartan: Insights into Drug–Polymer Interactions

2021

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The current study is focused on the development of highly stable drug nanocarriers by encapsulating losartan potassium (LSR) into an amphiphilic biocompatible poly(2-methyl-2-oxazoline)-grad-poly(2-phenyl-2-oxazoline) (PMeOxz72-grad-PPhOxz28) gradient copolymer (GC). Based on dynamic light scattering (DLS), the PMeOxz72-grad-PPhOxz28 (where the subscripts denote %wt composition of the components) GC formed micelles and aggregates of 13 nm and 96 nm in aqueous milieu. The presence of hydrophobic LSR molecules altered the structural characteristics of the GC, modulating the organization of the polymeric components and revealing the formation of hyper micellar nanostructures in addition to micelles. The 2D-NOESY experiments evidenced intermolecular interactions between the phenyl ring of LSR with the phenyl group of PPhOxz and eminent correlations between the butyl chain of LSR with the phenyl group of PPhOxz and methylene group of PMeOxz, respectively. Additionally, NMR studies as a function of temperature demonstrated that the presence of hydrophilic PMeOxz segments in the gradient core of PMeOxz72-grad-PPhOxz28 nanoassemblies induced an increased fluidity of the core matrix, especially upon heating, thus causing water penetration, resulting in increased proton mobility. Lastly, the ultrasound release profile of LSR signified that a great amount of the encapsulated LSR is tightly bound to the PMeOxz72-grad-PPhOxz28 nanoassemblies.

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Self-Assembled Block Copolymer Nanoaggregates for Drug Delivery Applications

Cited by 15 publications

References 89 publications

Synthesis, antimicrobial and anticancer activities of Tetronic 1107 Schiff bases

Synthesis, antimicrobial and anticancer activities of Tetronic 1107 Schiff bases

New Machine Learning Approach for the Optimization of Nano-Hybrid Formulations

Poly(2-oxazoline)-Based Amphiphilic Gradient Copolymers as Nanocarriers for Losartan: Insights into Drug–Polymer Interactions

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