Controlled release alginate-chitosan microspheres of tolmetin sodium prepared by internal gelation technique and characterized by response surface modeling

Elsayed, Mahmoud M. A.

doi:10.1590/s2175-97902020000118414

Cited by 13 publications

(21 citation statements)

References 27 publications

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“…Temperature showed no impact on AZM release after 1 and 3 h, in contrast to the LE percentage [42,69]. The findings of the LE percentage on in vitro release after 1 and 3 h suggest that the best AZM-ZnONPs formula should be made with a high AZM concentration (+1, 0.75%), a medium ZnONP weight (0, 500 mg), and a low temperature (−1, 20 ± 1 • C).…”

Section: In Vitro Release Study Of Azm-znonpsmentioning

confidence: 79%

“…The formulation characteristics of AZM-ZnONPs were examined and optimized using a Box-Behnken experimental design (BBD) for the maximum LE percentage and rapid drug delivery after 1 and 3 h [21,[37][38][39][40][41]. In circumstances involving more than two dependent variables, this design was chosen since it necessitates fewer treatment combinations than other designs [42][43][44]. The BBD is also ratable and has statistical "missing corners," which can help the experimenter avoid combination factor excesses.…”

Section: Experimental Designmentioning

confidence: 99%

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Tailoring of Novel Azithromycin-Loaded Zinc Oxide Nanoparticles for Wound Healing

et al. 2022

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Skin is the largest mechanical barrier against invading pathogens. Following skin injury, the healing process immediately starts to regenerate the damaged tissues and to avoid complications that usually include colonization by pathogenic bacteria, leading to fever and sepsis, which further impairs and complicates the healing process. So, there is an urgent need to develop a novel pharmaceutical material that promotes the healing of infected wounds. The present work aimed to prepare and evaluate the efficacy of novel azithromycin-loaded zinc oxide nanoparticles (AZM-ZnONPs) in the treatment of infected wounds. The Box–Behnken design and response surface methodology were used to evaluate loading efficiency and release characteristics of the prepared NPs. The minimum inhibitory concentration (MIC) of the formulations was determined against Staphylococcus aureus and Escherichia coli. Moreover, the anti-bacterial and wound-healing activities of the AZM-loaded ZnONPs impregnated into hydroxyl propyl methylcellulose (HPMC) gel were evaluated in an excisional wound model in rats. The prepared ZnONPs were loaded with AZM by adsorption. The prepared ZnONPs were fully characterized by XRD, EDAX, SEM, TEM, and FT-IR analysis. Particle size distribution for the prepared ZnO and AZM-ZnONPs were determined and found to be 34 and 39 nm, respectively. The mechanism by which AZM adsorbed on the surface of ZnONPs was the best fit by the Freundlich model with a maximum load capacity of 160.4 mg/g. Anti-microbial studies showed that AZM-ZnONPs were more effective than other controls. Using an experimental infection model in rats, AZM-ZnONPs impregnated into HPMC gel enhanced bacterial clearance and epidermal regeneration, and stimulated tissue formation. In conclusion, AZM -loaded ZnONPs are a promising platform for effective and rapid healing of infected wounds.

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Section: In Vitro Release Study Of Azm-znonpsmentioning

confidence: 79%

Section: Experimental Designmentioning

confidence: 99%

Tailoring of Novel Azithromycin-Loaded Zinc Oxide Nanoparticles for Wound Healing

et al. 2022

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“…LUT-ENPs Size and Polydispersity Index (PDI) For the optimization of different formulation variables three levels of each independent variable were used. The selected levels of EtOH concentrations (X 1 ) were 15(−1), 30(0), and 45% (1) (v/v), whereas the selected levels of SL concentrations were (X 2 ) 2(−1), 4(0), and 6(1) %(w/v) (Table 1) [19,20].…”

Section: Morphology Of the Prepared Lut-enpsmentioning

confidence: 99%

Design and Optimization of Orally Administered Luteolin Nanoethosomes to Enhance Its Anti-Tumor Activity against Hepatocellular Carcinoma

et al. 2021

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Luteolin (LUT) is a natural flavonoid with low oral bioavailability with restricted clinical applications due to its low solubility. LUT shows significant anti-tumor activity in many cancer cells, including hepatocellular carcinoma (HCC). The most recent trend in pharmaceutical innovations is the application of phospholipid vesicles to improve the solubility of such hydrophobic drugs. Ethosomes are one of the most powerful phospholipid vesicles used to achieve that that target. In this study, LUT-loaded ethosomal nanoparticles (LUT-ENPs) were prepared by the cold method. Full factorial design and response surface methodology were used to analyze and optimize the selected formulation variables. Drug entrapment efficiency, vesicle size, zeta potential, Fourier transform infra-red spectroscopy, scanning electron microscopy, and cumulative percent drug released was estimated. The selected LUT-ENPs were subjected to further investigations as estimation of hepatic gene expression levels of GPC3, liver biomarkers, and oxidative stress biomarkers. The prepared LUT-ENPs were semi-spherical in shape with high entrapment efficiency. The prepared LUT-ENPs have a small particle size with high zeta potential values. The in vitro liver biomarkers assay revealed a significant decrease in the hepatic tissue nitric oxide (NO), malondialdehyde (MDA) content, and the expression of the GPC3 gene. Results showed a high increase in the hepatic tissue levels of glutathione (GSH) and superoxide dismutase (SOD). Histopathological examination showed a small number of hepatic adenomas and a significant decrease of neoplastic hepatic lesions after treatment with LUT-ENPs. Our results firmly suggest the distinctive anti-proliferative activity of LUT-ENPs as an oral drug delivery system for the treatment of HCC.

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“…Gefitinib (GFT) is a tyrosine kinase inhibitor drug ( Figure 1 a) used as a first-line treatment for patients with advanced or metastatic non-small cell lung, colon, and breast cancer [ 11 , 12 ]. GFT is a member of the biopharmaceutics classification system (BCS) class II drugs, which exhibit low solubility and high permeability after oral administration [ 13 , 14 ]. GFT shows poor solubility/absorption/bioavailability after oral administration with a dose of 250 mg once daily [ 15 ].…”

Section: Introductionmentioning

confidence: 99%

“…GFT is a dibasic compound with pKa values of 5.4 and 7.2, which shows a pH-dependent solubility in the gastrointestinal fluids (~60% of the drug is absorbed in the gastrointestinal tract (GIT) [ 16 ]. Several systems have been developed for enhancing the solubility of hydrophobic drugs, including medication derivatization, the use of a complexing agent, manipulation of the solid state, the use of a surface-active agent, enlarging the surface area of the drug exposed to dissolution, spray drying, and microencapsulation [ 14 , 17 , 18 , 19 , 20 , 21 ]. Recently, the use of lipid vesicular systems such as ethosomes, niosomes, liposomes, proliposomes, and cubosomes has been developed to enhance the solubility of poorly water-soluble drugs [ 22 ]; these systems not only enhance the solubility of poorly soluble drugs but also sustain the release rate, which enhances the bioavailability for many drugs [ 23 , 24 , 25 , 26 ].…”

Section: Introductionmentioning

confidence: 99%

Anti-Tumor Activity of Orally Administered Gefitinib-Loaded Nanosized Cubosomes against Colon Cancer

et al. 2023

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Gefitinib (GFT) is a tyrosine kinase inhibitor drug used as a first-line treatment for patients with advanced or metastatic non-small cell lung, colon, and breast cancer. GFT exhibits low solubility and hence low oral bioavailability, which restricts its clinical application. One of the most important trends in overcoming such problems is the use of a vesicular system. Cubosomes are considered one of the most important vesicular systems used to improve solubility and oral bioavailability. In this study, GFT cubosomal nanoparticles (GFT-CNPs) were prepared by the emulsification method. The selected formulation variables were analyzed and optimized by full factorial design and response surface methodology. Drug entrapment efficiency (EE%), transmission electron microscopy, particle size, polydispersity index, in vitro release and its kinetics, and the effect of storage studies were estimated. The chosen GFT-CNPs were subjected to further investigations as gene expression levels of tissue inhibitors of metalloproteinases-1 (TIMP-1) and matrix metalloproteinases-7 (MMP-7), colon biomarkers, and histopathological examination of colon tissues. The prepared GFT-CNPs were semi-cubic in shape, with high EE%, smaller vesicle size, and higher zeta potential values. The in vivo data showed a significant decrease in the serum level of embryonic antigen (CEA), carbohydrate antigen 19-9 (CA 19-9), and gene expression level of TIMP-1 and MMP-7. Histopathological examination showed enhancement in cancer tissue and highly decreased focal infiltration in the lamina propria after treatment with GFT-CNPs.

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Controlled release alginate-chitosan microspheres of tolmetin sodium prepared by internal gelation technique and characterized by response surface modeling

Cited by 13 publications

References 27 publications

Tailoring of Novel Azithromycin-Loaded Zinc Oxide Nanoparticles for Wound Healing

Tailoring of Novel Azithromycin-Loaded Zinc Oxide Nanoparticles for Wound Healing

Design and Optimization of Orally Administered Luteolin Nanoethosomes to Enhance Its Anti-Tumor Activity against Hepatocellular Carcinoma

Anti-Tumor Activity of Orally Administered Gefitinib-Loaded Nanosized Cubosomes against Colon Cancer

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