In Vitro Release of 5-Fluorouracil and Methotrexate from Different Thermosensitive Chitosan Hydrogel Systems

Mohammed, Ahmed M.; Osman, Shaaban K.; Saleh, Khaled; Samy, Ahmed M.

doi:10.1208/s12249-020-01672-6

Cited by 33 publications

(23 citation statements)

References 42 publications

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“…The thermogram of 5-FU (fig. 1) showed a characteristic sharp peak of pure 5-FU around 280.04 °C, mainly related to 5-FU melting point temperature (Tm) [23,24]. Peak around 148.58 ο C in the thermogram of cholesterol as shown in fig.…”

Section: Thermal Behavior Xrd and Ftir Of 5-fu And Lipidsmentioning

confidence: 99%

Pre-Formulation Study on 5-Fluorouracil and Certain Lipids for Solid Lipid Nanoparticles Preparation

et al. 2022

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Objective: The study's objective involved compatibility studies to investigate the possible interactions between 5-fluorouracil (5-FU) and four different lipids, and the most appropriate lipid was chosen. Differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier Transform Infrared spectroscopy (FT-IR) are used for the compatibility study between 5-FU and several excipients as cholesterol, compritol®, stearic acid, and glycerol monostearate (GMS). Methods: The physical mixture between 5-FU and each lipid was made by mixing of a certain amount of drug with the same amount of lipid. Drug lipid blended mixtures were made by solvent evaporation casting method. 5-FU alone, physical mixture and blended mixture were measured using Differential scanning calorimetry (DSC) to investigate melting peak of drug and effect of each lipid on this melting point, X-ray diffraction (XRD) to observe the crystalline or amorphous state of drug and Fourier Transform Infrared (FT-IR) to determine any chemical interaction between drug and these lipids by observing any shift happened to characteristic peaks related to the drug. Results: 5-FU Tm (280.04 °C) peak appeared in drug-lipid physical mixtures with minor changes in position while this peak disappeared in 5-FU-compritol® and 5-FU-cholesterol blended mixture, indicating that the drug is molecular dispersed. XRD result showed that the crystalline structure of 5-FU was present in physical mixtures with four lipids, while in the 5-FU-compritol® blended mixture, the crystalline state of the drug was disappeared, confirming the DSC result. The FT-IR spectrum of the 5-FU-physical mixtures with four lipids showed that all characteristic peaks of the drug appeared with minor changes. In the case of 5-FU-blended mixtures with mentioned lipids, no chemical interaction occurred between the drug and mentioned lipids except in the drug-stearic acid blended mixture, the N-H peak at 3136.25 cm-1 was disappeared due to amide ester formation. Conclusion: The most appropriate lipids suitable for the preparation of 5-FU solid lipid nanoparticles were GMS and cholesterol.

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Section: Thermal Behavior Xrd and Ftir Of 5-fu And Lipidsmentioning

confidence: 99%

Pre-Formulation Study on 5-Fluorouracil and Certain Lipids for Solid Lipid Nanoparticles Preparation

et al. 2022

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“…DSC thermograms of MTX, E100 and MTX-NPs are demonstrated in Figure 5a. DSC thermogram of MTX indicated a sharp endothermic peak at 122 °C, which corresponds to the melting peak of MTX [59]. E100 showed an endothermic peak at 54.78 °C matching to the transition temperature (Tg) of polymer.…”

Section: Dsc Analysismentioning

confidence: 99%

Development and In Vitro/In Vivo Evaluation of pH-Sensitive Polymeric Nanoparticles Loaded Hydrogel for the Management of Psoriasis

et al. 2021

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Methotrexate (MTX), the gold standard against psoriasis, poses severe problems when administered systemically viz increased toxicity, poor solubility and adverse reactions. Hence, a topical formulation of MTX for the management of psoriasis can be an effective approach. The present study aimed to develop an MTX based nanoparticle-loaded chitosan hydrogel for evaluating its potential efficacy in an imiquimod-induced psoriatic mice model. MTX-NPs loaded hydrogel was prepared and optimized using the o/w emulsion solvent evaporation method. Particle size, zeta potential, entrapment efficiency, in vitro drug release, ex vivo permeation, skin irritation and deposition studies were performed. Psoriatic Area and Severity Index (PASI) score/histopathological examinations were conducted to check the antipsoriatic potential of MTX-NPs loaded hydrogel using an imiquimod (IMQ)-induced psoriatic model. Optimized MTX-NPs showed a particle size of 256.4 ± 2.17 nm and encapsulation efficiency of 86 ± 0.03%. MTX-NPs loaded hydrogel displayed a 73 ± 1.21% sustained drug release in 48 h. Ex vivo permeation study showed only 19.95 ± 1.04 µg/cm2 of drug permeated though skin in 24 h, while epidermis retained 81.33% of the drug. A significant decrease in PASI score with improvement to normalcy of mice skin was observed. The developed MTX-NPs hydrogel displayed negligible signs of mild hyperkeratosis and parakeratosis, while histopathological studies showed healing signs of mice skin. So, the MTX-NPs loaded hydrogel can be a promising delivery system against psoriasis.

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“…The materials commonly used in thermosensitive hydrogels are generally divided into two categories: synthetic and natural. Synthetic materials include poloxamers [35][36][37][38], poly N-isopropylacrylamides [39][40][41][42], and polyethylene glycol [43][44][45]; naturally formed materials include chitosan [46][47][48][49] and cellulose [50][51][52].…”

Section: Common Temperature Sensitive Materials and Gelation Mechanismmentioning

confidence: 99%

Thermosensitive Hydrogels and Advances in Their Application in Disease Therapy

et al. 2022

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Thermosensitive hydrogels, having unique sol–gel transition properties, have recently received special research attention. These hydrogels exhibit a phase transition near body temperature. This feature is the key to their applications in human medicine. In addition, hydrogels can quickly gel at the application site with simple temperature stimulation and without additional organic solvents, cross-linking agents, or external equipment, and the loaded drugs can be retained locally to improve the local drug concentration and avoid unexpected toxicity or side effects caused by systemic administration. All of these features have led to thermosensitive hydrogels being some of the most promising and practical drug delivery systems. In this paper, we review thermosensitive hydrogel materials with biomedical application potential, including natural and synthetic materials. We describe their structural characteristics and gelation mechanism and briefly summarize the mechanism of drug release from thermosensitive hydrogels. Our focus in this review was to summarize the application of thermosensitive hydrogels in disease treatment, including the postoperative recurrence of tumors, the delivery of vaccines, the prevention of postoperative adhesions, the treatment of nervous system diseases via nasal brain targeting, wound healing, and osteoarthritis treatment.

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In Vitro Release of 5-Fluorouracil and Methotrexate from Different Thermosensitive Chitosan Hydrogel Systems

Cited by 33 publications

References 42 publications

Pre-Formulation Study on 5-Fluorouracil and Certain Lipids for Solid Lipid Nanoparticles Preparation

Pre-Formulation Study on 5-Fluorouracil and Certain Lipids for Solid Lipid Nanoparticles Preparation

Development and In Vitro/In Vivo Evaluation of pH-Sensitive Polymeric Nanoparticles Loaded Hydrogel for the Management of Psoriasis

Thermosensitive Hydrogels and Advances in Their Application in Disease Therapy

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