Design of Targeted Flurbiprofen Biomimetic Nanoparticles for Management of Arthritis: In Vitro and In Vivo Appraisal

Mohamed, Hagar I.; El-Kamel, Amal H.; Hammad, Ghada O.; Heikal, Lamia

doi:10.3390/pharmaceutics14010140

Cited by 15 publications

(5 citation statements)

References 65 publications

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“…Pure carvedilol exhibited a distinct sharp endothermic peak at 113.03 °C, implying its crystallinity. The thermogram of BSA exhibited a broad enthalpy peak corresponding to heating the protein above its denaturation temperature, which was observed at 73.93 °C [ 19 , 48 , 49 ]. Upon analyzing the DSC profile of the optimized carvedilol-loaded BSA-based nanoparticles, we observed that the characteristic peak of carvedilol disappeared, suggesting that the drug incorporation in an amorphous state within the protein structure of the optimized formulation.…”

Section: Resultsmentioning

confidence: 99%

“…A shift in the peak may also have been caused by the stabilizing effects of carvedilol on BSA. This could imply the successful interaction and the entrapment of carvedilol inside the BSA nanoparticles, which might lead to a change in the molecular confirmation of the protein with the formation of a more organized and stable structure [ 49 ]. These results are supported by earlier studies in which various agents, such as limonene [ 50 ], halothane, and palmitic acid [ 51 ], increased the denaturation temperature of formed BSA complexes.…”

Section: Resultsmentioning

confidence: 99%

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Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance

et al. 2023

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Carvedilol, an anti-hypertensive medication commonly prescribed by healthcare providers, falls under the BCS class II category due to its low-solubility and high-permeability characteristics, resulting in limited dissolution and low absorption when taken orally. Herein, carvedilol was entrapped into bovine serum albumin (BSA)-based nanoparticles using the desolvation method to obtain a controlled release profile. Carvedilol-BSA nanoparticles were prepared and optimized using 32 factorial design. The nanoparticles were characterized for their particle size (Y1), entrapment efficiency (Y2), and time to release 50% of carvedilol (Y3). The optimized formulation was assessed for its in vitro and in vivo performance by solid-state, microscopical, and pharmacokinetic evaluations. The factorial design showed that an increment of BSA concentration demonstrated a significant positive effect on Y1 and Y2 responses with a negative effect on Y3 response. Meanwhile, the carvedilol percentage in BSA nanoparticles represented its obvious positive impact on both Y1 and Y3 responses, along with a negative impact on Y2 response. The optimized nanoformulation entailed BSA at a concentration of 0.5%, whereas the carvedilol percentage was 6%. The DSC thermograms indicated the amorphization of carvedilol inside the nanoparticles, which confirmed its entrapment into the BSA structure. The plasma concentrations of carvedilol released were observable from optimized nanoparticles up to 72 h subsequent to their injection into rats, revealing their longer in vivo circulation time compared to pure carvedilol suspension. This study offers new insight into the significance of BSA-based nanoparticles in sustaining the release of carvedilol and presents a potential value-added in the remediation of hypertension.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance

et al. 2023

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“…This revealed that the presence of RHCl in the F2 formulation did not suppress the anti-inflammatory activity of FBP; rather, it enhanced the inhibition rate by enhancing the solubility and bioavailability of FBP. In one study, flurbiprofen containing hyaluronic acid-coated bovine serum albumin nanoparticles showed improved therapeutic efficacy by reducing joint swelling when tested in an arthritis-induced rat model [ 71 ].…”

Section: Resultsmentioning

confidence: 99%

In Vitro and In Vivo Evaluation of Composite Oral Fast Disintegrating Film: An Innovative Strategy for the Codelivery of Ranitidine HCl and Flurbiprofen

et al. 2023

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Here, we evaluate the feasibility of co-loading plain ranitidine hydrochloride (RHCl) and microencapsulated flurbiprofen (FBP) in a Lycoat® RS780-based oral fast disintegrating film (ODF). These films were developed by the solvent casting method to minimize the adverse effects of FBP and reduce the dosage form burden on patients. Optimized FBP microparticles (M3) with an average size of 21.2 ± 9.2 µm were loaded alone (F1) and in combination with plain RHCl (F2) in the composite ODF. All films were evaluated physicomechanically and physicochemically. These films were resilient, flexible, and disintegrated within thirty seconds. SEM images showed intact FBP microparticles in both formulations and, moreover, did not observe an interaction between the drug and film components. Microencapsulated FBP was released in a controlled manner over 48 h from the proposed formulations, while RHCl was released within 5 min from F2. After in vitro evaluation, formulations were also tested for in vivo anti-inflammatory activity, cytokine (TNF-α and IL-6) levels, and gastroprotective effects in rats. The anti-inflammatory activity and gastroprotective effect of F2 were markedly higher than pure FBP and other synthesized formulations (M3 and F1). The average score of gastric lesions was in the order of pure FBP (15.5 ± 1.32) > M3 (8 ± 2) > F1 (1 ± 0.5) > F2 (0.5 ± 0) > control (0). Additionally, F2 showed a sustained anti-inflammatory effect up to 10 h in the rat paw edema model. Furthermore, F2 also markedly reduced TNF-α and IL-6 levels. Conclusively, the Lycoat® RS780-based composite film could be a promising carrier for the co-loading of microencapsulated FBP with RHCl. In the future, an optimized formulation (F2) could be capable of countering the issues related to multiple drug administration in geriatric patients and evading the gastric irritation associated with FBP.

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“…35 Mohamed et al used this method to load the anti-arthritis drug FLUR onto BSA with good results. 36 In addition, the emulsification method can also be used in combination with other methods to obtain more stable nanoparticles. Yamasaki et al combined the emulsification method with the spray method to load praziquantel into HSA and successfully produced smaller and more uniform drug-loaded nanoparticles with significantly improved oral utilization.…”

Section: Emulsion/solvent Extraction Methodsmentioning

confidence: 99%

“…Mohamed et al. used this method to load the anti‐arthritis drug FLUR onto BSA with good results 36 . In addition, the emulsification method can also be used in combination with other methods to obtain more stable nanoparticles.…”

Section: Preparation Of Nano‐serum Albuminmentioning

confidence: 99%

Research progress of serum albumin in the field of drug delivery

Ji,

Zheng,

et al. 2024

Interdisciplinary Medicine

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As a drug delivery system with wide application potential, serum albumin drug‐carrying nanoparticles have attracted extensive attention in the field of drug delivery in recent years. This review aims to summarize the research progress of serum albumin drug‐loaded nanoparticles in the field of drug delivery. Firstly, the excellent properties of serum albumin as a drug carrier were introduced, several methods of preparing serum albumin nanoparticles were discussed in depth, and their advantages and disadvantages were compared. Then, the design of the nanoparticle albumin drug carrier is discussed, including the control of the size of the nanoparticle, the surface properties and the amount of drug loading, so as to achieve better drug delivery effect. Finally, a series of therapeutic approaches using serum albumin nanoparticles as drug carriers, such as anti‐cancer drug delivery and drug delivery across the blood‐brain barrier, are systematically summarized. In summary, the research of serum albumin drug‐carrying nanoparticles has brought new possibilities and opportunities to the field of drug delivery, and inspired more innovative research and practical applications.

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Design of Targeted Flurbiprofen Biomimetic Nanoparticles for Management of Arthritis: In Vitro and In Vivo Appraisal

Cited by 15 publications

References 65 publications

Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance

Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance

In Vitro and In Vivo Evaluation of Composite Oral Fast Disintegrating Film: An Innovative Strategy for the Codelivery of Ranitidine HCl and Flurbiprofen

Research progress of serum albumin in the field of drug delivery

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