Propitious maneuvering for delivery of the phytopharmaceutical “apocynin” to induced fulminant hepatitis in BALB/c mice: In vitro and in vivo assessments

Anter, Hend Mohamed; Aman, Reham Mokhtar; Shaaban, Ahmed A.; Hashim, Irhan Ibrahim Abu; Meshali,

doi:10.1016/j.ijpharm.2022.122165

Cited by 6 publications

(12 citation statements)

References 85 publications

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“…These results were in unison with earlier reports [72]. MTX release from uncoated (F2) and FA-CS coated (F10 and F11) displayed a biphasic behavior, an initial burst release in different media for the first 2 h followed by sustained release up to 8 h. The initial burst release could be accredited to MTX molecules existing near the surface of the NPs [36] or loosely attached in the NPs [63], along with the accelerated diffusion of release medium into NPs due to their large surface area [16]. Furthermore, MTX encapsulated in the inner core of the polymeric matrix was responsible for the sustained release behavior from 2 to 8 h because of the biodegradation of the polymeric matrix and slow drug diffusion from such matrix [63].…”

Section: In Vitro Release Studies and Kinetics Analysissupporting

confidence: 91%

“…The freshly prepared optimized FA-CS coated MTX NPs (F10) suspension was packed in screw-capped amber glass vials and stored at refrigerated (4 ± 1°C) and ambient conditions (25 ± 2°C/40 ± 5% relative humidity) [35] for three months to inspect the impact of the storage temperature on physical appearance, PS, PDI, ζP, and EE% that were determined at time zero and then monthly [36].…”

Section: Storage Stability Studymentioning

confidence: 99%

“…FA spectrum (I) showed the bands at 3415, 1694, and 1604 cm -1 due to N-H stretching vibration, stretching vibration of C=O of the carboxylic group, and N-H group bending, respectively [43]. The spectrum of CS (II) exhibited characteristic peaks at 3451, 1656, 1595, 1158, 1074, and 1030 cm -1 attributed to the overlap between N─H and O─H bands because of intramolecular hydrogen bonds, C=O stretching vibrations of amide I, N-H bending vibrations of amide II, C-O-C bond asymmetric vibration, and C-O stretching vibration, respectively [36]. The spectrum of FA-CS conjugate (III) revealed significant changes compared to that of FA and CS.…”

Section: Synthesis and Characterization Of Fa-cs Conjugatementioning

confidence: 99%

“…The spectrum of MTX (I) revealed absorption peaks at 3420, 2955, 1647, 1603, 1497, 1406, and 1208 cm -1 corresponding to N-H stretching vibration, C-H stretching, C=O functional group from amide I, amide II band resulting from NH 2 bending along with C-N stretching, aryl system, C-O group, together with C=O moiety and amide III bands, respectively [74]. PLGA spectrum (II) exhibited the characteristic peaks at 3528 and 1747 cm -1 attained to the stretching vibration of -OH and C=O, respectively, of its monomers, lactide and glycolide [36]. The symmetric stretching of -CH, -CH 2 , and -CH 3 was distinguished by two absorption bands at 2883 and 2955 cm -1 , while the asymmetric stretching of -CH 3 and -CH 2 were characterized by distinct peaks at 1398 and 1459 cm -1…”

Section: Fourier Transform Infrared Spectroscopy (Ftir)mentioning

confidence: 99%

“…PVA spectrum (III) displayed discriminative bands at 3422, 2940, 1736, 1098, and 850 cm -1 due to stretching vibrations of -OH, C-H, C=O, C-O, and C-C groups of PVA, respectively [36,76]. The spectrum of FA-CS (IV) showed the distinguished peak at 3451cm -1 attributed to the overlapping between NH-and OH-groups of FA and CS [26], together with amide (CONH-) peak at 1654 cm -1 that was attributed to the interaction between the amino group of CS with the carboxylate group of FA [44,45] and NH bending in the second amine group at 1570 cm -1 [26,47,48].…”

Section: Fourier Transform Infrared Spectroscopy (Ftir)mentioning

confidence: 99%

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Surface-Decorated Nanocarrier as a Targeted Drug Delivery Cargo to Folate Receptor-Overexpressing Cells for Enhancing Anti-cancer and Anti-inflammatory Activity

Girgis

2023

J. Pharm. Res. Int.

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Aims: Folate receptor (FR) is overexpressed in most cancer cells and activated macrophages entailed in rheumatoid arthritis (RA). The aim of the current study was the fabrication of FR-targeted nanocarrier loaded with methotrexate (MTX) to magnify its therapeutic efficacy and limit its toxicity. Methodology: Folic acid-chitosan (FA-CS) conjugate was synthesized and characterized. MTX loaded poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) were prepared, optimized and coated with different concentrations of FA-CS conjugate. The selected FA-CS coated MTX NPs formulation (F10) was evaluated via in vitro and in vivo studies. Results: F10 had satisfactory encapsulation efficiency (76.2%), homogenous particle size (278.6 nm) and positive zeta potential (34.0 mV) and displayed biphasic drug release pattern in different pH media. Further characterization of F10 cinched MTX incorporation in the polymeric matrix of the targeted nanocarrier. In vitro cytotoxicity assay to FR-positive and FR-negative cancer cells revealed the improved anticancer effect of F10 to FR-positive cancer cells, which was absent in FR-negative cells, compared to free MTX or uncoated MTX NPs (F2). F10 showed appropriate storage stability at refrigerated temperature up to 3 months. Moreover, oral administration of F10 in the treatment of complete Freund’s adjuvant (CFA)-induced RA in BALB/c mice conferred prodigious therapeutic outcomes and declined systemic toxicity compared to oral treatment with conventional pure MTX or commercial MTX tablets. Conclusion: The fabricated targeted nanocarrier could enhance the anticancer activity of MTX to FR-overexpressing cancer cells and could be a promising novel approach for oral administration of MTX in the treatment of RA or other inflammatory conditions associated with FR-overexpressing activated macrophages.

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Section: In Vitro Release Studies and Kinetics Analysissupporting

confidence: 91%

Section: Storage Stability Studymentioning

confidence: 99%

Section: Synthesis and Characterization Of Fa-cs Conjugatementioning

confidence: 99%

Section: Fourier Transform Infrared Spectroscopy (Ftir)mentioning

confidence: 99%

Section: Fourier Transform Infrared Spectroscopy (Ftir)mentioning

confidence: 99%

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Surface-Decorated Nanocarrier as a Targeted Drug Delivery Cargo to Folate Receptor-Overexpressing Cells for Enhancing Anti-cancer and Anti-inflammatory Activity

Girgis

2023

J. Pharm. Res. Int.

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In vitro–in vivo assessments of apocynin-hybrid nanoparticle-based gel as an effective nanophytomedicine for treatment of rheumatoid arthritis

Aman

Zaghloul

Elsaed

et al. 2023

Drug Deliv. and Transl. Res.

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Apocynin (APO), a well-known bioactive plant-based phenolic phytochemical with renowned anti-inflammatory and antioxidant pharmacological activities, has recently emerged as a specific nicotinamide adenine dinucleotide phosphate-oxidase (NADPH) oxidase inhibitor. As far as we know, no information has been issued yet regarding its topical application as a nanostructured-based delivery system. Herein, APO-loaded Compritol® 888 ATO (lipid)/chitosan (polymer) hybrid nanoparticles (APO-loaded CPT/CS hybrid NPs) were successfully developed, characterized, and optimized, adopting a fully randomized design (32) with two independent active parameters (IAPs), namely, CPT amount (XA) and Pluronic® F-68 (PF-68) concentration (XB), at three levels. Further in vitro–ex vivo investigation of the optimized formulation was performed before its incorporation into a gel base matrix to prolong its residence time with consequent therapeutic efficacy enhancement. Subsequently, scrupulous ex vivo–in vivo evaluations of APO-hybrid NPs-based gel (containing the optimized formulation) to scout out its momentous activity as a topical nanostructured system for beneficial remedy of rheumatoid arthritis (RA) were performed. Imperatively, the results support an anticipated effectual therapeutic activity of the APO-hybrid NPs-based gel formulation against Complete Freund’s Adjuvant-induced rheumatoid arthritis (CFA-induced RA) in rats. In conclusion, APO-hybrid NPs-based gel could be considered a promising topical nanostructured system to break new ground for phytopharmaceutical medical involvement in inflammatory-dependent ailments. Graphical Abstract

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Formulation of lipid polymer hybrid nanoparticles of the phytochemical Fisetin and its in vivo assessment against severe acute pancreatitis

Awadeen,

Boughdady,

Zaghloul

et al. 2023

Sci Rep

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Fisetin (FST) is a naturally occurring flavonol that has recently emerged as a bioactive phytochemical with an impressive array of biological activities. To the author knowledge, boosting the activity of FST against severe acute pancreatitis (SAP) through a nanostructured delivery system (Nanophytomedicine) has not been achieved before. Thereupon, FST-loaded lipid polymer hybrid nanoparticles (FST-loaded LPHNPs) were prepared through conjoined ultrasonication and double emulsion (w/o/w) techniques. Comprehensive in vitro and in vivo evaluations were conducted. The optimized nanoparticle formula displayed a high entrapment efficiency % of 61.76 ± 1.254%, high loading capacity % of 32.18 ± 0.734, low particle size of 125.39 ± 0.924 nm, low particle size distribution of 0.357 ± 0.012, high zeta potential of + 30.16 ± 1.416 mV, and high mucoadhesive strength of 35.64 ± 0.548%. In addition, it exhibited a sustained in vitro release pattern of FST. In the in vivo study, oral pre-treatment of FST-loaded LPHNPs protected against l-arginine induced SAP and multiple organ injuries in rats compared to both FST alone and plain LPHNPs, as well as the untreated group, proven by both biochemical studies, that included both amylase and lipase activities, and histochemical studies of pancreas, liver, kidney and lungs. Therefore, the study could conclude the potential efficacy of the novel phytopharmaceutical delivery system of FST as a prophylactic regimen for SAP and consequently, associated multiple organ injuries.

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Propitious maneuvering for delivery of the phytopharmaceutical “apocynin” to induced fulminant hepatitis in BALB/c mice: In vitro and in vivo assessments

Cited by 6 publications

References 85 publications

Surface-Decorated Nanocarrier as a Targeted Drug Delivery Cargo to Folate Receptor-Overexpressing Cells for Enhancing Anti-cancer and Anti-inflammatory Activity

Surface-Decorated Nanocarrier as a Targeted Drug Delivery Cargo to Folate Receptor-Overexpressing Cells for Enhancing Anti-cancer and Anti-inflammatory Activity

In vitro–in vivo assessments of apocynin-hybrid nanoparticle-based gel as an effective nanophytomedicine for treatment of rheumatoid arthritis

Formulation of lipid polymer hybrid nanoparticles of the phytochemical Fisetin and its in vivo assessment against severe acute pancreatitis

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