Polymeric micelles for potentiated antiulcer and anticancer activities of naringin

Mohamed, Elham Abdelmonem; Hashim, Irhan Ibrahim Abu; Yusif, Rehab Mohammad; Shaaban, Ahmed A.; El‐Sheakh, Ahmed R.; Hamed, Mohamed F.; Badria, Farid A.

doi:10.2147/ijn.s154325

Cited by 59 publications

(45 citation statements)

References 78 publications

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“…Swelling of tablets coated with EUD-L combined with 5% and 10% w/w of each release retardant was studied according to the method previously adopted. 30,31 Swelling studies were carried out to screen the effects of the natural release retardant and concentration as well as the release medium pH on the coat swelling; hence, the drug release at the three media was used.…”

Section: Swelling Studiesmentioning

confidence: 99%

“…Slides were prepared using the manual immunohistochemistry stainer following the previously reported procedure. 49,50 Sections were deparaffinized with graded xylene and dehydrated in ethanol. Antigen retrieval was accomplished using citrate buffer pH 6.0.…”

Section: Immunohistochemical Localization Of Tnf-αmentioning

confidence: 99%

“…Naringin has polyhydroxy groups; thus O-H bond stretching resulted in a strong band in the range of 3000-3500 cm −1 . 50,52 Other characteristic bands of naringin included aromatic -OH at 1516 cm −1 , phenolic -OH at 1207 and 1362 cm −1 , and carbonyl group at 1644 cm −1 . Similar data have been reported.…”

Section: Study Of Drug-polymer Interactionmentioning

confidence: 99%

“…It has been reported that the mean time for a formulation to reach colon can be estimated as 5 hrs since the average residence time in stomach is 2 hrs, and that in small intestine is 3 hrs. 30,31 Accordingly, several studies have reported that cumulative percentage release after 5 hrs (CR 5h ) less than 20% can refer to gastric and intestinal protection against considerable drug release, and hence colon targeting can be expected. 30,66,67 Therefore, CR 5h was used to compare the coated tablets with respect to their ability to retard naringin release particularly at PB 6.8 and possibly target it to colon.…”

Section: In Vitro Release Studymentioning

confidence: 99%

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<p>Colon Targeting of Naringin for Enhanced Cytoprotection Against Indomethacin-Induced Colitis in Rabbits</p>

Naggar¹,

Mohamed²,

Borg³

et al. 2020

DDDT

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Background: Naringin is a promising anti-inflammatory drug against various disorders including ulcerative colitis. However, its oral bioavailability is low (8%) possibly due to cleavage at the upper gut. Consequently, colon targeting would be necessary for drug protection at the upper gut, enhanced oral bioavailability and potentiated cytoprotection against colitis. Methodology: This study involved the formulation of compression-coated tablets of naringin employing mixtures of pH-sensitive Eudragit L100-55 (EUD-L100-55) and different time-dependent polymers including ethyl cellulose (EC), sodium alginate (ALG) and sodium carboxymethyl cellulose (SCMC). Drug-polymer interaction during release was assessed using Fourier transform-infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Tablets were evaluated in vitro. Surface morphology of the optimized tablets either before or after exposure to the different release media was examined employing scanning electron microscopy (SEM). Cytoprotection potential of the optimized tablets against indomethacin-induced colitis in rabbits was screened and compared to core tablets through a histopathological examination of colon, measurement of serum perinuclear antineutrophil cytoplasmic antibodies (pANCA) and immunohistochemical localization of tumor necrosis factor-alpha (TNF-α). Results: FT-IR and DSC results may indicate drug-polymers interaction during release. Release retardation could be related to polymer swelling that was in the order of SCMC > ALG > EC. SEM examination indicated more porous coats at the buffers relative to the acidic medium. Colon targeting was expected in case of coats of 5% ALG, 5% SCMC and 10% EC (w/w) in combination with EUD-L100-55; thus, they were selected for in vivo evaluation. Effective cytoprotection of selected tablets against indomethacin-induced colitis was indicated by a significant (P<0.05) reduction in mucosal damage, serum levels of pANCA and TNF-α expression compared to untreated colitis and core-pretreated groups. Compared to EC, higher cytoprotection potential of ALG-and SCMC-based tablets was reflected by lower concentration (5% w/w) to provide cytoprotection against indomethacin-induced colitis.

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Section: Swelling Studiesmentioning

confidence: 99%

Section: Immunohistochemical Localization Of Tnf-αmentioning

confidence: 99%

Section: Study Of Drug-polymer Interactionmentioning

confidence: 99%

Section: In Vitro Release Studymentioning

confidence: 99%

See 2 more Smart Citations

<p>Colon Targeting of Naringin for Enhanced Cytoprotection Against Indomethacin-Induced Colitis in Rabbits</p>

Naggar¹,

Mohamed²,

Borg³

et al. 2020

DDDT

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“…us, alcohol is commonly used to induce experimental gastric ulcer models in animals [9]. Most of the existing antiulcer drugs mainly work via the manner of acid suppression and indirectly promote the self-healing of gastric mucosa, but show limited efficacy [10]. Lots of clinical and experimental studies have demonstrated that utilization of herbal medicines could be a valuable alternative to cure the gastric ulcer with few adverse effects [11].…”

Section: Introductionmentioning

confidence: 99%

Gastroprotective Activity of the Total Flavones from Abelmoschus manihot (L.) Medic Flowers

Zhang

Chu

et al. 2020

Evidence-Based Complementary and Alternative Medicine

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Background. Abelmoschus manihot (L.) Medic flower is a medicinal plant for the treatment of diseases in China. e present study was carried out to scientifically validate the gastroprotective activity and clarify the possible mechanism of the total flavones from Abelmoschus manihot (L.) Medic flowers (TFA). Methods. Gastric ulcer was induced in mice by oral administration of ethanol. e gastroprotective activity of TFA was evaluated by the gastric ulcer index and histological examinations. e gastric tissue was collected in the form of homogenate. e level of malondialdehyde (MDA) and glutathione (GSH), the activity of superoxide dismutase (SOD), and protein content were measured. Western blotting for the expression of Bax, Bcl-2, TNF-α, and NF-κB(p65) was also carried out. e effect of TFA was compared with that of standard antiulcer drug omeprazole (100 mg/kg). Results. is gastroprotective effect of TFA could be attributed to the increase in the activity of SOD and GSH and decrease in the levels of MDA and also decrease in the levels of Bax, TNF-α, and NF-κB(p65) expressions and increase in the Bcl-2 expression level. Conclusion.e findings of this study demonstrated that TFA could significantly attenuate ethanol-induced gastric injury via antioxidative, anti-inflammatory, and antiapoptotic effects.

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Investigation of the properties of chitosan–Pluronic based nanogel drug delivery systems utilizing various Pluronic types

Nguyen,

Nguyen

et al. 2024

Polymer Engineering & Sci

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This research aimed to create self‐assembled nanogel particles using chitosan grafted with various types of Pluronic to encapsulate curcumin, a hydrophobic biological agent. The study explored the properties of CS–Pluronic nanogels using Pluronic types L61, P123, F127, and F68, each varying in hydrophilic–lipophilic balance (HLB) index. Findings indicated that the critical micelle concentration (CMC) of Pluronics and CS–Pluronic copolymers did not depend on the HLB values but were influenced by the structural characteristics of each Pluronic type. The efficiency of curcumin encapsulation within the nanogels correlated with the CMC values of the CS–Pluronic copolymers, where lower CMC values resulted in higher encapsulation efficiencies. The curcumin‐loaded nanogels were spherical, positively charged, and had an average diameter under 200 nm. Controlled, pH‐dependent release of curcumin was observed in vitro studies conducted at 37°C in PBS at pH levels of 7.4 and 5.0, with a faster release in acidic conditions. Biocompatibility testing indicated that nanogel biocompatibility was influenced by the HLB value of Pluronic, with lower HLB values associated with reduced biocompatibility. Cytotoxicity testing revealed that curcumin‐loaded nanogels had increased cytotoxicity on MCF‐7 cells compared to free curcumin. CS–P123 emerged as the most effective carrier, meeting biocompatibility and stability requirements during storage.Highlights CS–Pluronic serves as an effective hydrophobic drug delivery system. The capacity of CS–Pluronic to encapsulate hydrophobic drugs is determined by its CMC value rather than its HLB index. CS–Pluronic is a copolymer known for its excellent biocompatibility. CS–Pluronic increases the toxicity of curcumin in nanogels compared to free curcumin.

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Polymeric micelles for potentiated antiulcer and anticancer activities of naringin

Cited by 59 publications

References 78 publications

<p>Colon Targeting of Naringin for Enhanced Cytoprotection Against Indomethacin-Induced Colitis in Rabbits</p>

<p>Colon Targeting of Naringin for Enhanced Cytoprotection Against Indomethacin-Induced Colitis in Rabbits</p>

Gastroprotective Activity of the Total Flavones from Abelmoschus manihot (L.) Medic Flowers

Investigation of the properties of chitosan–Pluronic based nanogel drug delivery systems utilizing various Pluronic types

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