Study of Controlled Release of PMMA‐g‐PEG Copolymer and Derivatives Incorporated with the Indomethacin Drug

Azevedo, Maria L. S.; Silveira, Benila Maria; Novack, Kátia Monteiro; Barboza, Ana Paula Moreira; Neves, Bernardo R. A.; Santos, Viviane Martins Rebello dos

doi:10.1002/masy.201800145

Cited by 6 publications

(5 citation statements)

References 12 publications

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“…The weight loss of water in HL micelles is far below the other two counterparts (phase I), implying the sharp decrease of micellar shell hydration with increasing drug loading . Besides, the weight loss of IMC in the hydrophilic PEO shell (phase II) and within the micellar PPO core (phase III) occurs, for which a higher temperature is needed to break the drug–polymer interaction in the hydrophobic micellar core . Moreover, the gradual increase of IMC weight loss in LL, ML, and HL micelles verifies the increase of drug loading.…”

Section: Resultsmentioning

confidence: 86%

“…7 Besides, the weight loss of IMC in the hydrophilic PEO shell (phase II) and within the micellar PPO core (phase III) occurs, for which a higher temperature is needed to break the drug−polymer interaction in the hydrophobic micellar core. 40 Moreover, the gradual increase of IMC weight loss in LL, ML, and HL micelles verifies the increase of drug loading. Finally, the phase IV indicates the weight loss of F127.…”

Section: Resultsmentioning

confidence: 87%

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Insight into Drug Loading Regulated Micellar Rigidity by Nuclear Magnetic Resonance

Sun

Zhou

et al. 2022

ACS Nano

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The rigidity of polymeric micelles plays an important role in their biological behaviors. However, how drug loading affects the rigidity of polymeric micelles remains elusive. Herein, the indomethacin (IMC)-loaded Pluronic F127 micelle is used as a model system to illustrate the impact of drug loading on the rigidity and biological behaviors of polymeric micelles. Against expectations, micelles with moderate drug loading show higher cellular uptake and more severe cytotoxicity as compared to both high and low drug loading counterparts. Extensive oneand two-dimensional nuclear magnetic resonance (NMR) measurements are employed to reveal that the higher drug loading induces stronger interaction between IMC and hydrophilic block to boost the micellar rigidity; consequently, the moderate drug loading imparts micelles with appropriate rigidity for satisfactory cellular uptake and cytotoxicity. In summary, NMR spectroscopy is an important tool to gain insight into drug loading regulated micellar rigidity, which is helpful to understand their biological behaviors.

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Section: Resultsmentioning

confidence: 86%

Section: Resultsmentioning

confidence: 87%

Insight into Drug Loading Regulated Micellar Rigidity by Nuclear Magnetic Resonance

Sun

Zhou

et al. 2022

ACS Nano

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“…SEM analyses were performed on JEOL equipment JSM6510 and the sample preparation was carried out in a Quorum evaporator. The surface analysis of the samples was performed after they were coated with carbon [8,10].…”

Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

“…The resulting depletion of ergosterol and concomitant accumulation of 14-a-methylated precursors interferes with the bulk function of ergosterol in fungal membranes and alters both the fluidity of the membrane and the activity of several membrane-bound enzymes (e.g., chitin synthase). The net effect is an inhibition of fungal growth and replication [8].…”

Section: Introductionmentioning

confidence: 99%

Controlled Release and Cell Viability of Ketoconazole Incorporated in PEG 4000 Derivatives

Inácio,

Nascimento,

Barboza

et al. 2023

Polymers

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In recent years, polymeric materials have been gaining prominence in studies of controlled release systems to obtain improvements in drug administration. These systems present several advantages compared with conventional release systems, such as constant maintenance in the blood concentration of a given drug, greater bioavailability, reduction of adverse effects, and fewer dosages required, thus providing a higher patient compliance to treatment. Given the above, the present work aimed to synthesize polymeric matrices derived from polyethylene glycol (PEG) capable of promoting the controlled release of the drug ketoconazole in order to minimize its adverse effects. PEG 4000 is a widely used polymer due to its excellent properties such as hydrophilicity, biocompatibility, and non-toxic effects. In this work, PEG 4000 and derivatives were incorporated with ketoconazole. The morphology of polymeric films was observed by AFM and showed changes on the film organization after drug incorporation. In SEM, it was possible to notice spheres that formed in some incorporated polymers. The zeta potential of PEG 4000 and its derivatives was determined and suggested that the microparticle surfaces showed a low electrostatic charge. Regarding the controlled release, all the incorporated polymers obtained a controlled release profile at pH 7.3. The release kinetics of ketoconazole in the samples of PEG 4000 and its derivatives followed first order for PEG 4000 HYDR INCORP and Higuchi for the other samples. Cytotoxicity was determined and PEG 4000 and its derivatives were not cytotoxic.

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“…Synthesis of PEG 4000 derivatives [14][15][16] PEG 4000 was subjected to 4 types of chemical modifications in order to functional groups inserted in its polymer chain facilitate the process of incorporation of indomethacin and, consequently, its release ( Figure 1).…”

Section: General Considerationsmentioning

confidence: 99%

Novel Peg 4000 Derivatives and Its Use in Controlled Release of Drug Indomethacin

Nascimento¹,

Lopes²,

Teodolino³

et al. 2020

Quim. Nova

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The insertion of functional groups in polymer compounds may facilitate their interaction with different drugs. PEG polymers are widely used for their low melting point, low toxicity, drug compatibility, and hydrophilicity. They are used as pharmaceutical excipients for the formulation of conventional or modified released drugs and are designed to be upgraded as drug-modulating controllers at specific sites in the body. Indomethacin has been used in the controlled release of drugs because it is a drug that have good interaction with different polymers. The drug is a non-steroidal anti-inflammatory drug used in the treatment of rheumatoid arthritis, osteoarthritis, spondylitis, and other disorders. In this work, PEG 4000 had its chain modified by organic reactions and their derivatives were emulsified to form microparticles using polyvinyl alcohol as an emulsifier. Posteriorly were also incorporated with indomethacin. The samples were characterized to prove the influence of indomethacin on the morphology and thermal behavior of this polymer. The controlled release was performed in the time from 0 to 240 min using the Ultraviolet Spectroscopy to quantify indomethacin released from the polymer matrix for these 4 hours. Releases over the time were satisfactory as concentrations increased over time, which we can conclude that the structural modification of PEG 4000 was beneficial in the release of the indomethacin drug.

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Study of Controlled Release of PMMA‐g‐PEG Copolymer and Derivatives Incorporated with the Indomethacin Drug

Cited by 6 publications

References 12 publications

Insight into Drug Loading Regulated Micellar Rigidity by Nuclear Magnetic Resonance

Insight into Drug Loading Regulated Micellar Rigidity by Nuclear Magnetic Resonance

Controlled Release and Cell Viability of Ketoconazole Incorporated in PEG 4000 Derivatives

Novel Peg 4000 Derivatives and Its Use in Controlled Release of Drug Indomethacin

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