Polymeric micelles in drug delivery: An insight of the techniques for their characterization and assessment in biorelevant conditions

Ghezzi, Martina; Pescina, Silvia; Padula, Cristina; Santi, Patrizia; Favero, Elena Del; Cantù, Laura

doi:10.1016/j.jconrel.2021.02.031

Cited by 579 publications

(357 citation statements)

References 211 publications

Supporting

Mentioning

287

Contrasting

Unclassified

Order By: Relevance

“…The in vitro release of RES from the optimized formulation was performed via the dialysis method [29] at 37 • C. An amount of RES-TPGS lyophilized powder in a 1:5 formulation, corresponding to 2 mg of RES, was reconstituted with 5 mL of phosphate buffer solution (PBS) at pH 7.4 and filled in a dialysis tube (MW CO 12,000 Da, Spectrum TM , Spectra/Pore ® , USA). A corresponding RES raw powder was suspended in the same volume to obtain an equal drug concentration and was tested along with the loaded micelles.…”

Section: In Vitro Release Studiesmentioning

confidence: 99%

Increased Water-Solubility and Maintained Antioxidant Power of Resveratrol by Its Encapsulation in Vitamin E TPGS Micelles: A Potential Nutritional Supplement for Chronic Liver Disease

et al. 2021

View full text Add to dashboard Cite

Children affected by chronic liver disease exhibit impaired neurocognitive development and growth due to the low absorption and digestion of nutrients. Furthermore, malnutrition is an adverse prognostic factor in liver transplantation as it is associated with an increase in morbidity and mortality. D-α-tocopheryl-polyethylene-glycol-succinate (TPGS) is currently administered per os as a vitamin E source to improve children’s survival and well-being; however, TPGS alone does not reverse spinocerebellar degeneration and lipid peroxidation. To potentiate the effects of TPGS, we loaded micelles with resveratrol (RES), a natural polyphenol, with antioxidant and antiinflammatory activities, which has demonstrated protective action in the liver. Firstly, we investigated the suitability of TPGS to encapsulate RES in micelles by means of a phase-solubility study, then RES-TPGS formulations were prepared via solvent casting and solvent diffusion evaporation methods. RES-TPGS colloidal dispersions showed small mean diameters (12 nm), low polydispersity, and quite neutral Zeta potentials. The formulations showed a sustained drug release and a good drug loading capacity, further confirmed by infrared spectroscopy and differential scanning calorimetry. RES-TPGSs exhibited unaltered antioxidant activity compared to pristine RES via the DPPH assay and a significant reduction in toxicity compared to empty TPGS on HaCaT cells. Thus, RES-TPGS micelles may overcome the challenges of current liver disease therapy by providing more protective effects thanks to the antioxidant activity of RES and by reducing the surfactant toxicity on normal cells.

show abstract

Section: In Vitro Release Studiesmentioning

confidence: 99%

Increased Water-Solubility and Maintained Antioxidant Power of Resveratrol by Its Encapsulation in Vitamin E TPGS Micelles: A Potential Nutritional Supplement for Chronic Liver Disease

et al. 2021

View full text Add to dashboard Cite

show abstract

“…However, this is only a hypothetical model that needs to be verified. Further studies are needed to investigate the conformation of these micelles in water (e.g., by using 1 H NMR in D 2 O) [ 52 , 53 ] and to examine the morphology of the self-assembled structures in water (e.g., by using cryogenic TEM or atomic force microscopy) [ 54 , 55 , 56 ].…”

Section: Resultsmentioning

confidence: 99%

“…In fact, the size distributions of both drug-free and PAX-loaded TPGS 2000 - b -PCL nanocarriers showed bimodal size distribution ( Figure S7 ), which may suggest either nanoparticle aggregation or formation of a mixed population, e.g., micelles and polymersomes. However, further studies (e.g., atomic force microscopy and cryogenic TEM) are needed to verify the possibility of presence of mixed morphologies [ 54 , 56 , 62 ].…”

Section: Resultsmentioning

confidence: 99%

“…Although fluorescent spectroscopy techniques are commonly used for determination of CMC, the application of DLS is expected to reduce the chance of error in CMC measurement. Since the measurement of CMC using fluorescent probes, such as pyrene, heavily depends on the partition equilibrium coefficient (kV) of the fluorescent probe to the core of micelle solution, the physical state of the micellar core may affect this partition and thus influence the measured CMC values [ 56 ].…”

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Design and Development of D‒α‒Tocopheryl Polyethylene Glycol Succinate‒block‒Poly(ε-Caprolactone) (TPGS−b−PCL) Nanocarriers for Solubilization and Controlled Release of Paclitaxel

et al. 2021

View full text Add to dashboard Cite

The objective of this study was to synthesize and characterize a set of biodegradable block copolymers based on TPGS-block-poly(ε-caprolactone) (TPGS-b-PCL) and to assess their self-assembled structures as a nanodelivery system for paclitaxel (PAX). The conjugation of PCL to TPGS was hypothesized to increase the stability and the drug solubilization characteristics of TPGS micelles. TPGS-b-PCL copolymer with various PCL/TPGS ratios were synthesized via ring opening bulk polymerization of ε-caprolactone using TPGS, with different molecular weights of PEG (1–5 kDa), as initiators and stannous octoate as a catalyst. The synthesized copolymers were characterized using 1H NMR, GPC, FTIR, XRD, and DSC. Assembly of block copolymers was achieved via the cosolvent evaporation method. The self-assembled structures were characterized for their size, polydispersity, and CMC using dynamic light scattering (DLS) technique. The results from the spectroscopic and thermal analyses confirmed the successful synthesis of the copolymers. Only copolymers that consisted of TPGS with PEG molecular weights ≥ 2000 Da were able to self-assemble and form nanocarriers of ≤200 nm in diameter. Moreover, TPGS2000-b-PCL4000, TPGS3500-b-PCL7000, and TPGS5000-b-PCL15000 micelles enhanced the aqueous solubility of PAX from 0.3 µg/mL up to 88.4 ug/mL in TPGS5000-b-PCL15000. Of the abovementioned micellar formulations, TPGS5000-b-PCL15000 showed the slowest in vitro release of PAX. Specifically, the PAX-loaded TPGS5000-b-PCL15000 micellar formulation showed less than 10% drug release within the first 12 h, and around 36% cumulative drug release within 72 h compared to 61% and 100% PAX release, respectively, from the commercially available formulation (Ebetaxel®) at the same time points. Our results point to a great potential for TPGS-b-PCL micelles to efficiently solubilize and control the release of PAX.

show abstract

“…Amphiphilic block copolymer micelles are widely used as nanocarriers for the encapsulation and delivery of hydrophobic drugs as they seek to avoid possible side effects, decrease drug degradation after administration and enhance the bioavailability of the drug [ 37 , 38 , 39 ]. Curcumin (CUR) is a hydrophobic polyphenol compound that has gained significant attention due to its low cytotoxicity, anticancer effects and anti-inflammatory properties [ 40 , 41 , 42 , 43 ].…”

Section: Introductionmentioning

confidence: 99%

PnBA-b-PNIPAM-b-PDMAEA Thermo-Responsive Triblock Terpolymers and Their Quaternized Analogs as Gene and Drug Delivery Vectors

2021

View full text Add to dashboard Cite

In this work, the ability of thermo-responsive poly [butyl acrylate-b-N-isopropylacrylamide-b-2-(dimethylamino) ethyl acrylate] (PnBA-b-PNIPAM-b-PDMAEA) triblock terpolymer self-assemblies, as well as of their quaternized analogs (PnBA-b-PNIPAM-b-QPDMAEA), to form polyplexes with DNA through electrostatic interactions was examined. Terpolymer/DNA polyplexes were prepared in three different amine over phosphate group ratios (N/P), and linear DNA with a 2000 base pair length was used. In aqueous solutions, the terpolymers formed aggregates of micelles with mixed PNIPAM/(Q)PDMAEA coronas and PnBA cores. The PnBA-b-PNIPAM-b-PDMAEA terpolymers’ micellar aggregates were also examined as carriers for the model hydrophobic drug curcumin (CUR). The complexation ability of the terpolymer with DNA was studied by UV–Vis spectroscopy and fluorescence spectroscopy by investigating ethidium bromide quenching. Fluorescence was also used for the determination of the intrinsic fluorescence of the CUR-loaded micellar aggregates. The structural characteristics of the polyplexes and the CUR-loaded aggregates were investigated by dynamic and electrophoretic light scattering techniques. Polyplexes were found to structurally respond to changes in solution temperature and ionic strength, while the intrinsic fluorescence of encapsulated CUR was increased at temperatures above ambient.

show abstract

Polymeric micelles in drug delivery: An insight of the techniques for their characterization and assessment in biorelevant conditions

Cited by 579 publications

References 211 publications

Increased Water-Solubility and Maintained Antioxidant Power of Resveratrol by Its Encapsulation in Vitamin E TPGS Micelles: A Potential Nutritional Supplement for Chronic Liver Disease

Increased Water-Solubility and Maintained Antioxidant Power of Resveratrol by Its Encapsulation in Vitamin E TPGS Micelles: A Potential Nutritional Supplement for Chronic Liver Disease

Design and Development of D‒α‒Tocopheryl Polyethylene Glycol Succinate‒block‒Poly(ε-Caprolactone) (TPGS−b−PCL) Nanocarriers for Solubilization and Controlled Release of Paclitaxel

PnBA-b-PNIPAM-b-PDMAEA Thermo-Responsive Triblock Terpolymers and Their Quaternized Analogs as Gene and Drug Delivery Vectors

Contact Info

Product

Resources

About