Synthesis and Formulation of Thermosensitive Drug Carrier for Temperature Triggered Delivery of Naproxen Sodium

Gasztych, Monika; Gola, Agnieszka; Kobryń, Justyna; Musiał, Witold

doi:10.3390/molecules21111473

Cited by 8 publications

(4 citation statements)

References 29 publications

(39 reference statements)

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“…The release profiles obtained in former experiments had a growing pattern similar to the logarithmic graph, similarly to the former experiments [ 24 ]. The lowest degree of release at 22 ± 0.5 °C of the active substance was found in AK2, and it may have been ascribed to the type of used crosslinker and comonomer.…”

Section: Discussionsupporting

confidence: 75%

Application of Polymerization Activator in the Course of Synthesis of N-Isopropylacrylamide Derivatives for Thermally Triggered Release of Naproxen Sodium

2018

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Poly-N-isopropylacrylamide (polyNIPA) is an extensively studied polymer in the field of controlled drug delivery. PolyNIPA contains carbonyl and amide groups along a hydrophobic chain. In an aqueous environment, crosslinked polyNIPA forms a gel characterized by a reversible volume phase transition temperature (VPTT), in response to changes in the external environment excited by the temperature factor. NIPA-based polymers were synthesized by a surfactant-free precipitation polymerization (SFPP) method at a temperature of 70 °C using the free radical initiator potassium persulfate (KPS) and at 35 °C using redox initiator system KPS with N,N,N’,N’-tetramethylethylenediamine (TEMED). The synthesized products were evaluated via dynamic light scattering (DLS), nuclear magnetic resonance (NMR) and Fourier-transform infrared spectroscopy (FTIR). The chemical structure, molecular mass, and hydrodynamic diameter of obtained particles, as well as the effects of synthesized polymers on the release of the active substance, naproxen sodium (NS), from hydroxypropyl methyl cellulose (HPMC)-based hydrogels were assessed. The use of the TEMED activator affected the particle size, as well as the release kinetics of NS. The insertion of TEMED into reactant mixtures may be applied to modify the release kinetics of NS from hydrogel preparations.

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Section: Discussionsupporting

confidence: 75%

Application of Polymerization Activator in the Course of Synthesis of N-Isopropylacrylamide Derivatives for Thermally Triggered Release of Naproxen Sodium

2018

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“…[ 30 ]. The influence of the formulation based on N -isopropylacrylamide and hydroxypropyl methylcellulose thermosensitive hydrogel for the naproxen sodium release was investigated [ 31 , 32 , 33 , 34 ]. Release tests showed that modification of the cross-linker type influenced the properties of synthesized polymeric particles obtained via surfactant free precipitation polymerization [ 32 ].…”

Section: Introductionmentioning

confidence: 99%

Semi-Crystalline Copolymer Hydrogels as Smart Drug Carriers: In Vitro Thermo-Responsive Naproxen Release Study

Ilić‐Stojanović

Nikolić

et al. 2021

Pharmaceutics

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In this study, poly(N-isopropylacrylamide-co-2-hydroxypropyl methacrylate) hydrogels were synthesized using free radical initiated copolymerization method. Four hydrogels with different cross-linker concentrations were prepared. Semi-crystalline, cross-linked copolymer networks were confirmed by FTIR, SEM and XRD analysis. Variation of swelling behaviour was monitored gravimetrically and thermo-responsiveness has been noticed. An application of synthesized thermo-responsive hydrogels as carriers for the modulated release of anti-inflammatory model drug was investigated. Moreover, naproxen loading into these hydrogels was also determined using FTIR, SEM and XRD techniques and release was analyzed using HPLC method at simulated physiological conditions. Swelling kinetic and mechanism of water transport, as well as diffusion of naproxen through the hydrogels were analyzed. Thus, the aim of this work was to study various compositions of obtained hydrogels and their possibility of application as a thermo-responsive carrier for prolonged naproxen release in order to evaluate as a potential candidate for drug carrier in future pharmaceutical applications.

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“…The hydrodynamic diameter of the particles was examined via DLS (dynamic light scattering) what enabled, in limited field, evaluation of polydispersity of prepared samples of rehydrated dispersions of liposomal fraction according to procedures performed formerly in our department [51]. The measurement of hydrodynamic diameter of the particles was carried out using the Zetaseizer Nano ZS ZEN3600 analyzer from Malvern (UK).…”

Section: Methodsmentioning

confidence: 99%

Selected Physicochemical Properties of Lyophilized Hydrogel with Liposomal Fraction of Calcium Dobesilate

Pilch

Musiał

2018

Materials

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Lyophilization is the process of drying and improving the stability of various pharmaceutical preparations. In this work we evaluated the properties of 11 hydrophilic gels calcium dobesilate with liposomes based on soybean lecithin, subjected to the freeze-drying procedure. Liposomes were produced by using method thin lipid film. Lyophilization was carried out under conditions of temperature equal (−30 °C) and pressure 0.37 mbar. We evaluated the preparations with dynamic light scattering (DLS) method, optical microscopy and Fourier-transform infrared spectroscopy (FTIR). In this work we presented the average results for the particle diameter in the sample and PDI (polydispersity index) value for the samples that produced the results. When testing using the DLS method on a Malvern Zetaseizer, results for 7 samples were not obtained. Two of next four samples were characterized by an increased size of the liposome particle resulting from a lower concentration of ethanol compared to the rest of them. Three samples under the microscope did not show any differences. It was possible only to see single crystals probably of undissolved calcium dobesilate. Some clusters were observed in the 4 samples, and when they appeared they were very small. The aggregates and irregular liposomes present in the rest of the samples may have been formed due to the destabilizing activity of ethanol towards lipid membranes. In the FTIR spectrum for MC, the peak was observed at the wavenumber of ca. 2900 cm−1 and of about 1050 cm−1. In case of pure calcium dobesilate we observed low pick at the wavenumber of about 3400 cm−1. The spectrum has a low peak at the wavenumber of 1450 cm−1 and intense peaks ranging from approx. 1000 cm−1 to approx. 1200 cm−1. Decay of the lecithin peak in formulations with liposomes at 1725 cm−1 wavelength may indicate the occurrence of the hydrolysis reaction in the system. Probably there was a hydrolysis of the ester bond connecting the rest of the phosphoric acid and the choline with the glycerol residue.

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Synthesis and Formulation of Thermosensitive Drug Carrier for Temperature Triggered Delivery of Naproxen Sodium

Cited by 8 publications

References 29 publications

Application of Polymerization Activator in the Course of Synthesis of N-Isopropylacrylamide Derivatives for Thermally Triggered Release of Naproxen Sodium

Application of Polymerization Activator in the Course of Synthesis of N-Isopropylacrylamide Derivatives for Thermally Triggered Release of Naproxen Sodium

Semi-Crystalline Copolymer Hydrogels as Smart Drug Carriers: In Vitro Thermo-Responsive Naproxen Release Study

Selected Physicochemical Properties of Lyophilized Hydrogel with Liposomal Fraction of Calcium Dobesilate

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